Pharmaceutical phyto API in modern medicine.
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Barely three months into the new year and we are happy to announce a monumental milestone reached - 150 million downloads.
\n\nThis achievement solidifies IntechOpen’s place as a pioneer in Open Access publishing and the home to some of the most relevant scientific research available through Open Access.
\n\nWe are so proud to have worked with so many bright minds throughout the years who have helped us spread knowledge through the power of Open Access and we look forward to continuing to support some of the greatest thinkers of our day.
\n\nThank you for making IntechOpen your place of learning, sharing, and discovery, and here’s to 150 million more!
\n\n\n\n\n'}],latestNews:[{slug:"webinar-introduction-to-open-science-wednesday-18-may-1-pm-cest-20220518",title:"Webinar: Introduction to Open Science | Wednesday 18 May, 1 PM CEST"},{slug:"step-in-the-right-direction-intechopen-launches-a-portfolio-of-open-science-journals-20220414",title:"Step in the Right Direction: IntechOpen Launches a Portfolio of Open Science Journals"},{slug:"let-s-meet-at-london-book-fair-5-7-april-2022-olympia-london-20220321",title:"Let’s meet at London Book Fair, 5-7 April 2022, Olympia London"},{slug:"50-books-published-as-part-of-intechopen-and-knowledge-unlatched-ku-collaboration-20220316",title:"50 Books published as part of IntechOpen and Knowledge Unlatched (KU) Collaboration"},{slug:"intechopen-joins-the-united-nations-sustainable-development-goals-publishers-compact-20221702",title:"IntechOpen joins the United Nations Sustainable Development Goals Publishers Compact"},{slug:"intechopen-signs-exclusive-representation-agreement-with-lsr-libros-servicios-y-representaciones-s-a-de-c-v-20211123",title:"IntechOpen Signs Exclusive Representation Agreement with LSR Libros Servicios y Representaciones S.A. de C.V"},{slug:"intechopen-expands-partnership-with-research4life-20211110",title:"IntechOpen Expands Partnership with Research4Life"},{slug:"introducing-intechopen-book-series-a-new-publishing-format-for-oa-books-20210915",title:"Introducing IntechOpen Book Series - A New Publishing Format for OA Books"}]},book:{item:{type:"book",id:"5820",leadTitle:null,fullTitle:"Green Chemical Processing and Synthesis",title:"Green Chemical",subtitle:"Processing and Synthesis",reviewType:"peer-reviewed",abstract:'Sustainable development and alternative energy constituted urgent needs in the last decade. Renewable chemicals, energy and bio-resource use became challenging topics in the sustainable, renewable and green sciences. This encourages and turns primordial needs the works in certain fields as developing of new and green catalysts for chemical transformations, in the domains of energy, environmental, pharmaceutical, agro-alimentary and cosmetically applications; evaluation of bio-resources compounds largely available for many applications in energy or as additives to fuels and other applications, reduction and conversion of greenhouse gas as well as developing new synthesis routes by avoiding the use of toxic and environmentally damage materials. In this book, the recent sustainable and green process is presented in three sections: "Greenhouse Gas Conversion Efficiency in Microwave", "Biomass Green Process" and "Green Synthesis and Catalysis".',isbn:"978-953-51-3260-8",printIsbn:"978-953-51-3259-2",pdfIsbn:"978-953-51-4761-9",doi:"10.5772/65562",price:119,priceEur:129,priceUsd:155,slug:"green-chemical-processing-and-synthesis",numberOfPages:160,isOpenForSubmission:!1,isInWos:1,isInBkci:!1,hash:"c0ab0c8e1f6a1af3ee04ff657ce75e1d",bookSignature:"Iyad Karame and Hassan Srour",publishedDate:"July 5th 2017",coverURL:"https://cdn.intechopen.com/books/images_new/5820.jpg",numberOfDownloads:11683,numberOfWosCitations:13,numberOfCrossrefCitations:9,numberOfCrossrefCitationsByBook:2,numberOfDimensionsCitations:25,numberOfDimensionsCitationsByBook:2,hasAltmetrics:1,numberOfTotalCitations:47,isAvailableForWebshopOrdering:!0,dateEndFirstStepPublish:"October 5th 2016",dateEndSecondStepPublish:"October 26th 2016",dateEndThirdStepPublish:"January 22nd 2017",dateEndFourthStepPublish:"April 22nd 2017",dateEndFifthStepPublish:"June 21st 2017",currentStepOfPublishingProcess:5,indexedIn:"1,2,3,4,5,6,7",editedByType:"Edited by",kuFlag:!1,featuredMarkup:null,editors:[{id:"145512",title:"Prof.",name:"Iyad",middleName:null,surname:"Karamé",slug:"iyad-karame",fullName:"Iyad Karamé",profilePictureURL:"https://mts.intechopen.com/storage/users/145512/images/3352_n.jpg",biography:"Iyad Karamé, PhD.\nHe is a professor at the Faculty of sciences in the Lebanese University in Beirut. Director of the Organometallic Catalysis and Materials Laboratory, in the department of Chemistry. He got his PhD degree from Claude Bernard-Lyon 1 university in France in January 2004. He was an assistant professor and researcher (ATER) at the Ecole Normale Supérieure de Lyon, France, for one year (2004-2005). A researcher at the Leibniz Institut für Katalyse in Rostock (Germany) (2005-2006) and then at the Laboratory of Organometallic Chemistry of surface, CPE-Lyon till 2008. His principal axis of research are Organometallic Catalysis, Green Chemistry, CO2 chemistry and Synthesis of chelating macrocyles for the complexation of metals.",institutionString:null,position:null,outsideEditionCount:0,totalCites:0,totalAuthoredChapters:"1",totalChapterViews:"0",totalEditedBooks:"4",institution:{name:"Lebanese University",institutionURL:null,country:{name:"Lebanon"}}}],equalEditorOne:null,equalEditorTwo:null,equalEditorThree:null,coeditorOne:{id:"195431",title:"Dr.",name:"Hassan",middleName:null,surname:"Srour",slug:"hassan-srour",fullName:"Hassan Srour",profilePictureURL:"https://mts.intechopen.com/storage/users/195431/images/4969_n.jpg",biography:"Got his PhD degree from University of Claude Bernard Lyon 1 in France in October 2013. His principal axes of research are organic synthesis, polymer electrolytes, organometallic catalysis for different applications (energy storage systems and CO2 valorization). He is an editor of different books published by INTECHOPEN such as: “Recent Advances of Organocatalysis”, Green chemical processing and synthesis and Carbon Dioxide (CO2) Chemistry, Capture and Oil Recovery.",institutionString:null,position:null,outsideEditionCount:0,totalCites:0,totalAuthoredChapters:"0",totalChapterViews:"0",totalEditedBooks:"0",institution:null},coeditorTwo:null,coeditorThree:null,coeditorFour:null,coeditorFive:null,topics:[{id:"496",title:"Environmental Chemistry",slug:"organic-chemistry-environmental-chemistry"}],chapters:[{id:"54677",title:"Enhancing the Greenhouse Gas Conversion Efficiency in Microwave Discharges by Power Modulation",doi:"10.5772/67875",slug:"enhancing-the-greenhouse-gas-conversion-efficiency-in-microwave-discharges-by-power-modulation",totalDownloads:1434,totalCrossrefCites:1,totalDimensionsCites:2,hasAltmetrics:0,abstract:"Scientific interest to the plasma-assisted greenhouse gas conversion continuously increases nowadays, as a part of the global Green Energy activities. Among the plasma sources suitable for conversion of CO2 and other greenhouse gases, the non-equilibrium (low-temperature) discharges where the electron temperature is considerably higher than the gas temperature, represent special interest. The flowing gas discharges sustained by microwave radiation are proven to be especially suitable for molecular gas conversion due to high degree of non-equilibrium they possess. In this Chapter the optimization of CO2 conversion efficiency in microwave discharges working in pulsed regime is considered. The pulsed energy delivery represents new approach for maximization of CO2 conversion solely based on the discharge “fine-tuning”, i. e. without the additional power expenses. In our work several discharge parameters along the gas flow direction in the discharge have been studied using various diagnostic techniques, such as optical actinometry, laser-induced fluorescence, and gas chromatography. The results show that CO2 conversion efficiency can be essentially increased solely based on the plasma pulse frequency tuning. The obtained results are explained by the relation between the plasma pulse parameters and the characteristic time of the relevant energy transfer processes in the discharge.",signatures:"Nikolay Britun, Guoxing Chen, Tiago Silva, Thomas Godfroid, Marie‐\nPaule Delplancke‐Ogletree and Rony Snyders",downloadPdfUrl:"/chapter/pdf-download/54677",previewPdfUrl:"/chapter/pdf-preview/54677",authors:[{id:"176901",title:"Dr.",name:"Nikolay",surname:"Britun",slug:"nikolay-britun",fullName:"Nikolay Britun"},{id:"176903",title:"Dr.",name:"Thomas",surname:"Godfroid",slug:"thomas-godfroid",fullName:"Thomas Godfroid"},{id:"176904",title:"Prof.",name:"Rony",surname:"Snyders",slug:"rony-snyders",fullName:"Rony Snyders"},{id:"199224",title:"Dr.",name:"Tiago",surname:"Silva",slug:"tiago-silva",fullName:"Tiago Silva"},{id:"199226",title:"Mr.",name:"Guoxing",surname:"Chen",slug:"guoxing-chen",fullName:"Guoxing Chen"}],corrections:null},{id:"54707",title:"Role of Plasma Catalysis in the Microwave Plasma‐Assisted Conversion of CO2",doi:"10.5772/67874",slug:"role-of-plasma-catalysis-in-the-microwave-plasma-assisted-conversion-of-co2",totalDownloads:1462,totalCrossrefCites:3,totalDimensionsCites:7,hasAltmetrics:0,abstract:"Climate change and global warming caused by the increasing emissions of greenhouse gases (such as CO2) recently attract attention of the scientific community. The combination of plasma and catalysis is of great interest for turning plasma chemistry in applications related to pollution and energy issues. In this chapter, our recent research efforts related to optimization of the conversion of CO2 and CO2/H2O mixtures in a pulsed surface‐wave sustained microwave discharge are presented. The effects of different plasma operating conditions and catalyst preparation methods on the CO2 conversion and its energy efficiency are discussed. It is demonstrated that, compared to the plasma‐only case, the CO2 conversion and energy efficiency can be enhanced by a factor of ∼2.1 by selecting the appropriate conditions. The catalyst characterization shows that Ar plasma treatment results in a higher density of oxygen vacancies and a comparatively uniform distribution of NiO on the TiO2 surface, which strongly influence CO2 conversion and energy efficiencies of this process. The dissociative electron attachment of CO2 at the catalyst surface enhanced by the oxygen vacancies and plasma electrons may explain the increase of conversion and energy efficiencies in this case. A mechanism of plasma‐catalytic conversion of CO2 at the catalyst surface in CO2 and CO2/H2O mixtures is proposed.",signatures:"Guoxing Chen, Nikolay Britun, Thomas Godfroid, Marie‐Paule\nDelplancke‐Ogletree and Rony Snyders",downloadPdfUrl:"/chapter/pdf-download/54707",previewPdfUrl:"/chapter/pdf-preview/54707",authors:[{id:"176901",title:"Dr.",name:"Nikolay",surname:"Britun",slug:"nikolay-britun",fullName:"Nikolay Britun"},{id:"176903",title:"Dr.",name:"Thomas",surname:"Godfroid",slug:"thomas-godfroid",fullName:"Thomas Godfroid"},{id:"176904",title:"Prof.",name:"Rony",surname:"Snyders",slug:"rony-snyders",fullName:"Rony Snyders"},{id:"199226",title:"Mr.",name:"Guoxing",surname:"Chen",slug:"guoxing-chen",fullName:"Guoxing Chen"},{id:"199227",title:"Prof.",name:"Marie-Paule",surname:"Delplancke-Ogletree",slug:"marie-paule-delplancke-ogletree",fullName:"Marie-Paule Delplancke-Ogletree"}],corrections:null},{id:"54503",title:"Catalytic Conversions of Biomass-Derived Furaldehydes Toward Biofuels",doi:"10.5772/67805",slug:"catalytic-conversions-of-biomass-derived-furaldehydes-toward-biofuels",totalDownloads:1848,totalCrossrefCites:3,totalDimensionsCites:4,hasAltmetrics:0,abstract:"Upgrading of biomass resources toward high-energy compounds (biofuel) is a crucial technology for sustainable development because utilizations of biomass resources can contribute to the low CO2 emission on the basis of carbon neutral concept. In this chapter, recent advances on catalytic hydrogenation and hydrogenolysis of biomass-derived furaldehydes, dehydration products of saccharides, for example, called as hydroxymethylfuran (HMF) and furfural, toward biofuels over heterogeneous catalytic system are introduced. Some approaches on mechanistic study and reactor design are also mentioned in this chapter.",signatures:"Shun Nishimura and Kohki Ebitani",downloadPdfUrl:"/chapter/pdf-download/54503",previewPdfUrl:"/chapter/pdf-preview/54503",authors:[{id:"197425",title:"Prof.",name:"Kohki",surname:"Ebitani",slug:"kohki-ebitani",fullName:"Kohki Ebitani"},{id:"204890",title:"Dr.",name:"Shun",surname:"Nishimura",slug:"shun-nishimura",fullName:"Shun Nishimura"}],corrections:null},{id:"54708",title:"Green Synthesis of Oligomer Calixarenes",doi:"10.5772/67804",slug:"green-synthesis-of-oligomer-calixarenes",totalDownloads:2768,totalCrossrefCites:0,totalDimensionsCites:0,hasAltmetrics:0,abstract:"The synthesis of calixarenes can be conventionally done by heating at high temperature for a few hours and using various solvents in large quantities. The greener synthesis can be done with microwave-assisted synthesis and the solvent-free method, where both of these methods can reduce reaction time, energy use, solvent, and waste, with a higher percentage yield than that from the conventional synthesis method, making the synthesis of cyclic oligomer calixarenes and their derivatives more environmentally friendly.",signatures:"Ratnaningsih Eko Sardjono and Rahmi Rachmawati",downloadPdfUrl:"/chapter/pdf-download/54708",previewPdfUrl:"/chapter/pdf-preview/54708",authors:[{id:"199158",title:"Dr.",name:"Ratnaningsih",surname:"Sardjono",slug:"ratnaningsih-sardjono",fullName:"Ratnaningsih Sardjono"},{id:"199162",title:"M.Sc.",name:"Rahmi",surname:"Rachmawati",slug:"rahmi-rachmawati",fullName:"Rahmi Rachmawati"}],corrections:null},{id:"55121",title:"Environment-Friendly Approach in the Synthesis of Metal/ Polymeric Nanocomposite Particles and Their Catalytic Activities on the Reduction of p-Nitrophenol to p-Aminophenol",doi:"10.5772/intechopen.68388",slug:"environment-friendly-approach-in-the-synthesis-of-metal-polymeric-nanocomposite-particles-and-their-",totalDownloads:1830,totalCrossrefCites:1,totalDimensionsCites:4,hasAltmetrics:0,abstract:"In this chapter, an environment‐friendly approach in synthesizing Au and Au@Ag metal nanoparticles using a microgel is demonstrated. Poly(N‐isopropyl acrylamide)/polyethyleneimine microgel was used as a multifunctional template to reduce metal ions to metal nanoparticles, stabilize and immobilize these metal nanoparticles, and regulate their accessibility within the template. Such multifunctional roles of microgel template were possible due to their unique properties (i.e., amino groups reducing capability, electrostatic and steric stabilizing properties, and swelling/deswelling properties). Characterizations of these metal/polymeric composite particles were also performed, such as scanning electron microscope (SEM), transmission electron microscope (TEM), Zeta‐potential, UV‐vis spectroscopy, X-ray Diffraction (XRD), and X‐ray photoelectron spectroscopy (XPS). To test the catalytic activities of both gold and gold@silver nanoparticles in the microgel template, a model reaction (i.e., reduction of p‐nitrophenol to p‐aminophenol) was performed. Results showed that bimetallic gold@silver gave 10 times higher catalytic activity compared to monometallic gold nanoparticles. With the simple one‐step synthesis, a highly scalable process is possible.",signatures:"Noel Peter Bengzon Tan and Cheng Hao Lee",downloadPdfUrl:"/chapter/pdf-download/55121",previewPdfUrl:"/chapter/pdf-preview/55121",authors:[{id:"197243",title:"Dr.",name:"Noel Peter",surname:"Tan",slug:"noel-peter-tan",fullName:"Noel Peter Tan"},{id:"197363",title:"Dr.",name:"Cheng Hao",surname:"Lee",slug:"cheng-hao-lee",fullName:"Cheng Hao Lee"}],corrections:null},{id:"55675",title:"Environmental-Friendly Catalytic Oxidation Processes Based on Hierarchical Titanium Silicate Zeolites at SINOPEC",doi:"10.5772/intechopen.68389",slug:"environmental-friendly-catalytic-oxidation-processes-based-on-hierarchical-titanium-silicate-zeolite",totalDownloads:2342,totalCrossrefCites:1,totalDimensionsCites:8,hasAltmetrics:0,abstract:"Since it was claimed by EniChem in 1983 for the first time, titanium silicate‐1 (TS‐1) zeolite presented the most delightful catalytic performance in the area of selective organic oxidation reactions. To enhance the mass diffusion property, hierarchical titanium silicate with hollow cavities within crystal was prepared by using a post‐synthesis treatment in the presence of organic template, and then, it was commercially produced and employed in many industrial catalytic oxidation processes, such as propylene epoxidation, phenol hydroxylation, and cyclohexanone ammoximation. Moreover, we also developed several totally novel oxidation reactions on hollow titanium silicate (HTS) zeolite, i.e., Baeyer‐Villiger oxidation of cyclohexanone and chlorohydrination of allyl chloride with HCl and H2O2. In all cases, HTS shows much better catalytic performance than TS‐1, attributing to the mass diffusion intensification by introducing hollow cavities. On the other hand, enormous works on synthesizing hierarchical TS‐1 zeolites with open intracrystalline mesopores have been done via silanization treatment and recrystallization. Based on them, several bulk molecule oxidation processes with tert‐butyl hydroperoxide, such as epoxidation of fatty acid methyl ester (FAME) and large olefins, have been carried out. As a consequence, hierarchical TS‐1 zeolites supply a platform for developing environmental‐friendly catalytic oxidation processes to remarkably overcome the drawbacks of traditional routes.",signatures:"Changjiu Xia, Xinxin Peng, Yao Zhang, Baorong Wang, Min Lin, Bin\nZhu, Yibin Luo and Xingtian Shu",downloadPdfUrl:"/chapter/pdf-download/55675",previewPdfUrl:"/chapter/pdf-preview/55675",authors:[{id:"182654",title:"Dr.",name:"Changjiu",surname:"Xia",slug:"changjiu-xia",fullName:"Changjiu Xia"},{id:"182925",title:"Prof.",name:"Min",surname:"Lin",slug:"min-lin",fullName:"Min Lin"},{id:"182927",title:"Prof.",name:"Bin",surname:"Zhu",slug:"bin-zhu",fullName:"Bin Zhu"},{id:"182928",title:"Prof.",name:"Xingtian",surname:"Shu",slug:"xingtian-shu",fullName:"Xingtian Shu"},{id:"187312",title:"Prof.",name:"YiBin",surname:"Luo",slug:"yibin-luo",fullName:"YiBin Luo"},{id:"200872",title:"Mr.",name:"Xinxin",surname:"Peng",slug:"xinxin-peng",fullName:"Xinxin Peng"},{id:"204876",title:"Dr.",name:"Baorong",surname:"Wang",slug:"baorong-wang",fullName:"Baorong Wang"},{id:"204877",title:"Mr.",name:"Yao",surname:"Zhang",slug:"yao-zhang",fullName:"Yao Zhang"}],corrections:null}],productType:{id:"1",title:"Edited Volume",chapterContentType:"chapter",authoredCaption:"Edited by"},subseries:null,tags:null},relatedBooks:[{type:"book",id:"2874",title:"Hydrogenation",subtitle:null,isOpenForSubmission:!1,hash:"737b7439c2b3372d6c4b34ce28a37fe4",slug:"hydrogenation",bookSignature:"Iyad Karamé",coverURL:"https://cdn.intechopen.com/books/images_new/2874.jpg",editedByType:"Edited by",editors:[{id:"145512",title:"Prof.",name:"Iyad",surname:"Karamé",slug:"iyad-karame",fullName:"Iyad Karamé"}],equalEditorOne:null,equalEditorTwo:null,equalEditorThree:null,productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"5206",title:"Recent Advances in Organocatalysis",subtitle:null,isOpenForSubmission:!1,hash:"d06787ec7084c188686d860994f03abe",slug:"recent-advances-in-organocatalysis",bookSignature:"Iyad Karame and Hassan Srour",coverURL:"https://cdn.intechopen.com/books/images_new/5206.jpg",editedByType:"Edited by",editors:[{id:"145512",title:"Prof.",name:"Iyad",surname:"Karamé",slug:"iyad-karame",fullName:"Iyad Karamé"}],equalEditorOne:null,equalEditorTwo:null,equalEditorThree:null,productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"6186",title:"Carbon Dioxide Chemistry, Capture and Oil Recovery",subtitle:null,isOpenForSubmission:!1,hash:"720a601cd2b5476cbeb817906a4ab2dd",slug:"carbon-dioxide-chemistry-capture-and-oil-recovery",bookSignature:"Iyad Karamé, Janah Shaya and Hassan Srour",coverURL:"https://cdn.intechopen.com/books/images_new/6186.jpg",editedByType:"Edited by",editors:[{id:"145512",title:"Prof.",name:"Iyad",surname:"Karamé",slug:"iyad-karame",fullName:"Iyad Karamé"}],equalEditorOne:null,equalEditorTwo:null,equalEditorThree:null,productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"5768",title:"Desalination",subtitle:null,isOpenForSubmission:!1,hash:"939ab36830b6159adf8da8f9413277f3",slug:"desalination",bookSignature:"Taner Yonar",coverURL:"https://cdn.intechopen.com/books/images_new/5768.jpg",editedByType:"Edited by",editors:[{id:"32956",title:"Dr.",name:"Taner",surname:"Yonar",slug:"taner-yonar",fullName:"Taner Yonar"}],equalEditorOne:null,equalEditorTwo:null,equalEditorThree:null,productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}},{type:"book",id:"7512",title:"Lanthanides",subtitle:null,isOpenForSubmission:!1,hash:"f7bcbda594eacb5a3bd7149e94628753",slug:"lanthanides",bookSignature:"Nasser S. 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Spiess"}],equalEditorOne:null,equalEditorTwo:null,equalEditorThree:null,productType:{id:"1",chapterContentType:"chapter",authoredCaption:"Edited by"}}]},onlineFirst:{chapter:{type:"chapter",id:"76831",title:"Current Updates on Global Phytoceuticals and Novel Phyto Drug Delivery System in Herbal Medicine",doi:"10.5772/intechopen.97671",slug:"current-updates-on-global-phytoceuticals-and-novel-phyto-drug-delivery-system-in-herbal-medicine",body:'The contribution of natural products to human kind is tremendous in modern drug discovery and its usage is well known before the era of Christ. Lead molecules from plants and microbial origin are significant [1]. In the global pharmaceutical industry, about 34% of the medicines originated from natural molecules. Among the 34%, 6% were natural products, 27.5% were natural products derivatives, thus played important source of lead molecules in manufacturing therapeutic agents in pharmaceutical industries globally [2, 3].
Based on the survey in the dispensing area of union territory of Puducherry, India, the potent phyto molecules as Active Pharmaceutical Ingredient (API) is being prescribed by modern physicians, are
Atropine, a tropane alkaloid (
Pilocarpine, an imidazole alkaloid (
Morphine, a phenanthrene alkaloid (
Codeine, a phenanthrene alkaloid (
Digoxin, a cardiac glycoside (
Vincristine sulphate, an indole alkaloid, (
Taxol, a diterpene alkaloid (
Caffeine, a purine alkaloid (
Ergometrine, an indole alkaloid (
Capsaicin, a pungent principle (
β – Carotene, a tetraterpene (
Antibiotics - Penicillin from
The important milestone of natural molecules in the time travel of drug discovery and also in global pharmaceutical market is, they act as precursors for some of the semisynthetic molecules [4, 5, 6].
Chloroquine, semisynthetic derivative of quinine (
Diosgenin, a steroidal saponin (
Table 1 gives the remarkable contribution of pharmaceutical phyto API, is being prescribed in modern medicine along with formulation.
Pharmaceutical phyto API in modern medicine.
Excipients in formulating different dosage forms are pharmacologically inert thereby promotes the therapeutic activity of API. Bioavailability, safety, efficacy and stability of the dosage forms is depend on the nature of excipients. Excipients are classified as diluents, binders, surfactants, preservatives, sweeteners etc. [7]. The usage of herbal excipients as phytomolecules is veiled due to the popularity of synthetic molecules in the domain of pharmacy.
Natural excipients are biodegradable in nature
As ecofriendly in the aspect of pharmaceutical effluents
Most of the herbal excipients are carbohydrate in nature and hence they are non-toxic in nature
Cost of the excipients are cheaper when compared to synthetic molecules
Natural excipients are easily available from different natural sources.
Though natural excipients are advantageous, in some aspects they do possess some limitations, in the source of raw materials as herbal excipients. Possibility of attack of microbial contamination in contact with external environment, availability as raw material is varied depending upon climatic conditions and geographical origin, more importantly heavy metal contaminations. These are the challenges faced in herbal excipients as a source of raw materials in pharmaceutical industries.
The requirement of human community is the source of the drug should always from natural resources instead of synthetic origin not only the API but also the excipients.
Because of the low viscosity of acacia emulsions, creaming occurs rather quickly and thickening agents tragacanth, sodium alginate and agar are used as stabilizers. Acacia emulsions are palatable and thereby are stable over a wide pH range (2–10), but they are too sticky for external use.
Compound tragacanth powder contains acacia (20%), tragacanth (15%), starch (20%) and sucrose. It is generally used in the form of compound powder (about 2 g per 100 ml of mixture) or as the mucilage (10 to 20 ml per 150 ml of product). The compound powder is always used as a vehicle other than water or chloroform water to avoid displacement of part of a medicinally active vehicle by the mucilage.
Tragacanth is the dried gummy exudation obtained by incision from stems and branches of
Tragacanth jellies sometimes called bassorin pastes since the hydrophilic component of tragacanth that forms gels in water is been named bassorin. As a lubricant 2–3% is adequate, 5% is necessary for dermatological vehicle. Bassorin paste consist of tragacanth 5%, alcohol 10%, glycerol 2% and water made upto 100 ml, is been used as a vehicle for Ichthammol, resorcinol, salicylic acid and other medicaments. Tragacanth based catheter lubricants and electrode and contraceptives jellies have been developed.
The disadvantage of tragacanth jelly is\t\t
They vary in viscosity, due to geographical origin of the gum and variations in milling and storage.
It tends to flake when the film left on the skin.
When the pH range alters from 4 to 5 to 7, the viscosity is lost.
They are susceptible to microbial degradation.
Agar is the dried gelatinous substance obtained from
Agar used as a gelling agent, thickening agent and stabilizer in liquid dosage forms. It is used as emulsifying agent and bulk laxatives. It is used in the manufacturing of jellies and confectionary items. In microbiology, it is used in the preparation of bacteriological culture medium.
(Rutaceae) (Rosaceae) (Apiaceae) (Asteraceae)
The source of pectin is from plants of different families. The important sources of pectin are
Pectin is obtained from the inner rind of citrus fruits or from apple pulp remaining after cider making. It is extracted with dilute acid and purified. Pectin dissolves in about 20 parts of water, producing a viscous opalescent acid solution. It is good emulgent in acid media but degraded at alkaline pH.
Lecithin is obtained from soybean oil
Gelatin is a protein, extracted by partial hydrolysis of animal collagenous tissue such as skins, tendons, ligaments and bones with in boiling water. Chemically gelatin contains different amino acids in which lysine is major essential amino acid. It does not contain tryptophan, gelatin composed of gluten protein.
In bacteriological culture media, gelatin is used in the form of absorbable gelatin sponge and gelatin film.
Lactose is a natural disaccharide contains galactose and glucose obtained from milk of mammals. Chemically lactose monohydrate is monohydrate of O-β-D galactopyranosyl – (1–4)-α-D glucopyranose.
Mannitol is a hexahydric alcohol obtained by isolation from stem of
Starch is a polysaccharide granules obtained from grains of maize (
Sometimes starch is used with other suspending agents because of the high viscosity of the mucilage. It is an ingredient of compound tragacanth powder. Starch is a poor emulsifying agent. Its emulsions are suspensions of large globules prevented from coalescing by the high viscosity of mucilage. It is occasionally used for preparing enemas containing oils.
Yellow bees wax is purified wax obtained from the honey comb of bees
Chemically bees wax is the esters of straight chain monohydric alcohols with straight chain acids. The chief constituent of the bees wax is myricyl palmitate (about 80%). In addition cerotic acid (15%), small quantity of melissic acid and aromatic substance cerolein present along with chief constituent.
Beeswax contains sterol containing substances. Higher alcohols (eg., cetyl and steary) form w/o emulsion. The chief constituent of beeswax is myricyl palmitate, is a ester of higher alcohol and responsible for emulsifying properties partly. In addition, beeswax contains small amounts of esters of cholesterol (a sterol producing w/o emulsions) and free cerotic acid (C25H51COOH) reacts with borax producing soap used as an emulgent in cold creams.
Lanolin is a waxy substance secreted by sebaceous glands of wool bearing animals. Hydrous wool fat is the purified fat like substance obtained from the wool of the sheep
It is too sticky in nature to use alone and generally mixed with hydrocarbons as in the official eye ointment base and simple ointment B.P. The above products absorb appreciable amount of aqueous liquids. Example is the B.P alkaloidal eye ointments are prepared by incorporating aqueous solution of the alkaloidal salt into base thus forming a stable semi-solid emulsion.
It does not rancidify readily. It is used in creams and ointments and as an emulsion stabilizer and in lotions. Retaining its properties and to improve the physical characteristics and stability of wool fat, the following process can be done
Hydrogenation: Hydrogenated wool fat is a white, odorless and non-sticky in nature and spreads easily on skin and absorbs 50% of water.
Fractionation
Treatment with ethylene oxide
Pharmaceutically in semi-solid dosage form, lanolin is used as water absorbable ointment base. It is a common ingredient and base for many water soluble creams and cosmetic preparations. It is used in topical liniments, as a lubricant and employed in rust preventive coatings.
Wool alcohols are obtained by crude fractionation of wool fat. Small amounts upto 2.5% used as a stabilizer in o/w emulsions. High concentrations cause phase inversion.
Sodium carboxy methyl cellulose is the sodium salt of poly carboxy methyl ether of cellulose from wood and cotton fiber
Sodium alginate is the sodium salt of alginic acid, a polyuronic acid obtained from the algal growth of the species of family Phaeophyceae. The common algae are
Alginic acid present in cell wall. The algae are harvested, dried, milled and extracted with dilute sodium carbonate solution results in a pasty mass. It is diluted to separate insoluble matter. Only soft water is used for extraction process. Further it is treated with calcium chloride or sulfuric acid for converting into calcium alginate. Purification can be done through washing. The next step is treating with hydrochloric acid. Alginic acid collected is treated with sodium carbonate for neutralization and conversion into sodium salt.
Sodium alginate is used as a stabilizing agent for emulsion, in the formulation of buccal tablets, as a cross linking polymer in enzyme immobilization. It is employed as a binding and disintegrating agent in tablet and lozenges, thickening and suspending agent in liquid dosage forms.
Irish moss is dried seaweed, red algae
Peppermint oil is obtained by steam distillation of fresh flowering tops of
Liquorice liquid extract is obtained from the dried, unpeeled, roots and stolons of
Lemon spirit is obtained by maceration of lemon peel which is the outer part of the pericarp of ripen fruits of
Orange syrup and compound orange spirit is prepared from fresh or dried outer peel of the ripen or nearly ripen fruits of
Earth is gifted by creator with rich heritage of botanicals in terms of natural products. Some of the natural products are potential in its therapeutic action for the betterment of mankind. Exploring the unexplored potential phytomolecules and converting it into novel formulation is the need of the hour to combat the challenging diseases and disorders.
Novel drug delivery in modern phytoceutical research can pave a way to determine its pharmacokinetic property, mechanism and site of action, accurate dose required to exert the desired therapeutic action. Phytomolecules can be incorporated into novel drug carriers as nanoparticles, nano and micro emulsions, matrix systems, solid dispersions, liposomes, solid lipid nanoparticles and the like. Improving phytodrug delivery to the receptor target improves the efficacy thereby minimize the toxicity due to delivery of precise dose at the site of action.
Exploring the novel phytomolecules as pharmacophores to combat various diseases and disorders is been realized due to resentment on synthetic molecules. The limited clinical usage of herbal medicine is due to hydrophobic nature of phytomolecules results in poor absorbable nature thereby leads to low bioavailability [9] and lower lipid solubility results in increased systemic clearance. In other fringe at the site of administration, the phytomolecules are not stable at acidic pH in stomach, results in degradation leads to loss of desired therapeutic action [10].
In order to overcome these challenges, developing novel phyto dosage forms will pave a way to deliver the potent phytomolecules at receptor target with improvement in bioavailability, specificity, efficacy and stability and to control the rate of release of phytodrug thereby reduction in dosage frequency, enhances solubility as well as absorption of phytomolecules.
Novel drug delivery strategies include modified drug in terms of sustained and controlled release (polymers, miscelles, liposomes, ethosomes, and nanotechnology), prodrugs, transdermal drug delivery systems, ocusert, insulin jet and micropump, patient controlled analgesia, drug eluting stents, gene therapy and personalized medicine.
Phytometabolites also act as carriers to deliver the drug into different sites (Brain, stomach, colon, lungs, etc.). The aim of thischapter is to articulate the current updates in the area of drug carriers in specific to colon target and the data mining on the nano engineered phytomolecules in pharmaceutical research in the area of phytopharmaceuticals.
The delivery of drugs into gastrointestinal tract is difficult due to physiological challenges like motility, hepatic clearance, acidic degradation, efflux mechanism, mucous turnover etc. Localizing orally administering drugs into the colon is complicated due to prediction of exact residence time of solid dosage forms in the stomach and small intestine. Also the residence time of the drugs depends on fed/fasted patterns, meal compositions and intensity of peristalsis. Solid dosage form may stay few minutes to 8 hour in stomach and 3 to 5 hour in bowel. Hence the colonic route of drug delivery can be used for systemic administration of drugs. Various approaches can be exploited to target the release of drug to colon by coating the drug with pH sensitive polymers, biodegradable polymers, embedding in biodegradable matrices and hydrogels, timed release systems, osmotic systems and bio adhesive systems [11].
Drug delivery systems targeted to colon by using natural polysaccharides finds superior over other systems. Moreover the uniqueness of polysaccharides are, retains their integrity and prevent the release of drug during its travel through GI tract and finally when it come in contact with colonic fluid it is digested by microorganism thereby the entrapped drug will be liberated. The polysaccharides been explored in colon specific drug release from plant origin are amylose, pectin, guar gum, alginates from algal origin, inulin, locust bean gum and pectin.
Amylose is a component of starch, a polysaccharide obtained from plant source. Chemically amylose is glycopyranose residues linked by α-(1–4) bonds. It is a poly (1–4-α-D-glucopyranose).
Chemical structure of amylose.
Natural polysaccharide | Reference |
---|---|
[12] | |
Amylose & Ethecol (1:4) coated pellets containing 300 mg (13C) glucose is developed for colonic drug delivery | [12] |
Epichlorhydrin treated crosslinked amylase investigated for colon target drug delivery | [13] |
Guar gum is the powdered endosperm of the seeds of
Alginates are natural hydrophilic polysaccharide derived from seaweeds. Chemically aliganates are 1➔4 linked D-mannuronic acid and L-glucuronic acid residues.
Alginates
Natural polysaccharide | Reference |
---|---|
Calcium alginate beads prepared as cores and 5-amino salicylic acid coated on them, act as controlled drug release. | [16] |
Calcium alginate coated with Aquacoat®, a pH independent polymer followed by 2% w/w coating of Eudragit® resisted the release of drug in acidic media and drug release triggered at alkaline pH, act as sustain release in colon. | [17] |
When drug coated with calcium alginate beads swells due to osmotic gradient and the film bursts and release the drug. The delivery of the drug will be to the distal intestine with minimum initial leak and thus provides sustained release in the colon.
Inulin is a polysaccharide which is a chemotaxonomic marker of the plants belongs to compositae family. Chemically inulin is β 2–1 linked D-fructose having glucosyl unit at the reducing end. Mostly fructose chains have glucose unit as the initial moiety.
Structure of Inulin.
Natural polysaccharide | Reference |
---|---|
Inulin incorporated into Eudragit® RS films resist degradation in the upper GI tract and digested in human fecal medium | [18] |
Inulin reacted with glycidyl methacrylated in N,N-dimethyl formamide in presence of dimethylaminopyridine as catalyst results in formation of hydrogel, degraded by inulinase enzymes causes bulk degradation. | [19] |
Carob gum is the synonym of Locust bean gum obtained from seeds of
β-o-Manp-β-o-mannopyranosyl unit.
α-o-Galp-α-o-galactopyranosyl unit.
Polysaccharide units of locust bean gum.
Locust bean gum and chitosan (2:3, 3:2 & 4:1) in combination used as a polymer for colon specific drug delivery. Invitro drug release and invivo studies revealed the core tablet is capable of protecting the drug release in stomach, small intestine. Further susceptible to colonic bacterial enzyme results in drug release [20].
Pectin is obtained from
Structure of Pectin.
Natural polysaccharide | Reference |
---|---|
Coating with pectin in presence of additives and hydrophobic polymers remains unaffected in gastric and small intestinal enzymes and digested in presence of colonic bacterial enzymes | [21] |
Insoluble salt of calcium pectinate by deesterification is utilized for the preparation of matrix tablets and incorporating indomethacin as water insoluble drug marker in the invitro release experiments. The release of indomethacin is significantly increased in rat caccal contents. | [22] |
Natural molecules other than plant source also plays important role in pharmaceutical sector. Chitosan high molecular weight polycationic polysaccharide obtained from chitin (Cuticles of various crustaceans, principally crabs and shrimps), chondroitin sulphate, a mucopolysaccharide consist of D-glucuronic acid linked to acetyl D – galactosamide obtained from extracts of cartilaginous cow and pig tissues and other sources such as shark, fish, and bird cartilages, cyclodextrins, an enzymatic conversion of starch, dextrans, a colloidal, hydrophilic and water soluble linear chains of α-D- glucose molecules obtained from microorganisms of the lactobacillus
Colon based drug delivery strategies are exploited to target the drug release to the colon. Several approaches is been and being investigated to achieve site specificity to colon. In this context, the presence of polysaccharides in the colon provides platform for the delivery of drugs to the colon. Specifically the natural polysaccharides remains intact in the pH condition of stomach and small intestine and when reaches the colon, the drug loaded natural polysaccharides are cleaved by polysaccharidases enzymes, due to presence of large number of derivatizable groups, wide range of molecular weights, varying chemical compositions, low toxicity and high stability. Challenges faced in use of polysaccharides as drug carriers ishydrophilicity that results in drug release slowly in upper GI tract. This can be overcome by crosslinking of the polysaccharides with epichlorhydrin, glutaraldehyde and STMP. In this aspect the crosslinking agents should not alter the biodegradability of the polysaccharide matrix in colon.
Phytomolecules are complex in structure contributes to its polarity. Non polar phytoconstituents are steroids, terpenoids, volatile oils, alkaloids and fixed oil, flavonoids are moderate polar constituent, alkaloidal salt, tannins, glycosides, phenols, gums, resins, mucilage are highly polar constituents. Employing novel drug delivered strategy for varied polar Phytoconstituents illuminate the focus of phytodrug in the global pharmaceutical sector. The advantage of converting phytomolecules into nano size results in increase in solubility in the systemic circulation thereby increase in bioavailability, physical stability, improving tissue macrophage distribution, protection from physical and chemical degradation, dose proportionality, smaller dosage form, smaller particle size with greater surface area provides higher absorption rate including lipophilic non polar phytomolecules, as a substitute for liposomes and vehicles. More importantly the nano sized phytomolecules potentially enhances the therapeutic action that ends in innovative therapeutic strategies for herbal medicines.
Nanotechnology is the engineered technology applied for the drug molecules at the nano size of 1-100 nm.Designing of drugs especially phytodrugs in nano dosage forms offers greater efficacy and cell specificity. Nanodosage forms are one of the significant novel drug delivery systems.
Plants containing volatile oils can be easily formulated into nanoemulsion. Nanoemulsions constitute vehicles for volatile oil with sizes ranging from 20 to 200 nm. Nanoemulsions are colloidal dispersion system mixed with emulsifying agents, surfactants and co-surfactants to form single phase. Nanoemulsions are classified into o/w type (oil dispersed in aqueous phase), w/o type (water dispersed in oil phase) and bicontinuous (microdomains of water and oil are interdispersed within the system). Multiple emulsion is also included in the types of nanoemulsion wherein both o/w and w/o emulsion present in one system. Hydrophobic and lipophilic surfactants are used for stability.
Following is the perception of phytonanoemulsion, formulation methods (Table 2), characterization techniques (Table 3).
S.No. | Method | Type | Principle |
---|---|---|---|
1 | Low energy emulsification | Phase inversion method | Using low temperature and high temperature |
Phase inversion composition method | Magnetic stirring and evaporation of the water miscible solvents under vacuum | ||
Solvent displacement method | Membrane contractor liquid phase forced through membrane pores leads to formation of droplets | ||
2 | High pressure emulsification | Ultrasonication | Sonicator probe contacts the liquid and it generates mechanical vibration leads to Cavitation |
High Pressure homogenization | 500-5000 psi | ||
Microfluidiser | 500–20,000 psi |
S.No | Parameters | Characterization method |
---|---|---|
1. | Droplet size analysis | Diffusion method using light scattering particle size analyzer |
2. | Viscosity | Brookfield viscometer |
3. | Dilution | The Nanoemulsion is diluted with water and observed for phase inversion |
4. | Drug content | HPLC method |
5. | Poly dispersity | Photon correlation spectroscopy |
6. | Refractive index | Refractometer |
7. | Dye test | The water soluble dye is added in an o/w type nanoemulsion and it takes up the color uniformly. Similarly, the emulsion is w/o type and the water soluble dye being added and the emulsion is not uniformly colored. |
8. | pH | pH meter |
9. | Zeta potential | Zeta sizer / zeta analyzer |
10. | Fluorescence test | Many oils exhibit fluorescence when exposed to UV light |
11. | Percentage transmittance | UV visible spectrophotometer |
12. | Conductance measurement | Conductometer |
13. | Filter paper test | Nanoemulsion dropped onto filter paper and observed for migration |
14. | Morphology and structure | TEM (Transmission Electron Microscopy) |
15. | Invitro skin permeation studies | Kesharychien-diffusion cell |
16. | Stability studies | Heating cooling cycle (the formulation were subjected to refrigerator (six cycles) at the temperature 4 °C and 45°C) stable formulation subjected to centrifugation test& Centrifugation (stable formulation were centrifuged at 3500 rpm) |
17. | Interaction study | Fourier transform infrared spectroscopy spectral analysis |
18. | Surface morphology | Atomic force microscope |
19. | Invitro drug release study | Dissolution test apparatus |
Phytomolecules is been formulated as novel dosage forms and over two decades it is been concentrated in scientific research. The plant actives and extracts are formulated into polymeric nanoparticles, nanocapsules, liposomes, phytosomes, nanoemulsions, microspheres, transferosomes, and ethosomes. Secondary metabolites formulated as novel phyto drug nano dosage forms (Table 4) and Table 5 gives the insight view of plant actives and extracts formulated into various novel dosage forms [48].
Secondary metabolites formulated as novel phyto drug nano dosage form.
S.No | Formulation | Method | Pharmacological action | Reference |
---|---|---|---|---|
1 | Liposome encapsulated Silymarin | Reverse evaporation technique | Hepatoprotective | [40] |
2 | Breviscapine liposome | Sustained delivery of breviscapine | To treat ischemic cerebrovascular and cardiovascular diseases | [41] |
3 | Paclitaxel liposome | Thin film hydration method | Anticancer | [42] |
4 | Berberine-loaded nanoparticles | Ionic gelation method | Anticancer | [43] |
5 | Glycyrrhizic acid-loaded nanoparticles | Rotary-evaporated film ultrasonication method | Anti-inflammatory & antihypertensive | [44] |
6 | Taxal loaded nanoparticles | Emulsion solvent evaporation method | Anticancer | [45] |
7 | Silybin phytosome | Silybin-phospholipid complexation | Hepatoprotective, antioxidant for liver and skin | [46] |
8 | Berberine nanoemulsion | Drawing ternary phase diagram | Hypolipidemic agent | [47] |
Phytomolecules in novel dosage forms.
Natural products either as a drug or pharmaceutical substance played vital role in the treatment and prevention of diseases in humans. Pharmacognosy is the established pharmaceutical science and is a mother of pharmacy wherein, phytochemistry and molecular pharmacology, is the heart of the drug discovery process. Investigation of plant products will give a way to enter as a lead molecule as pharmacophores in drug discovery process or as a drug carrier to receptor target rather than placing the herbs in traditional pharmacognosy.
Today pharmacognosy discipline is the carrier of potent traditional herbs that acts as a bridge and as a vehicle that transports to the site of modern drug discovery. Focusing pharmacognosy research not only identifies new chemical entities (NCE’s), but also exploring the biomolecules from natural sources as drug carriers, in formulating novel phyto drug dosage forms equivalent to the synthetic drug dosage forms in the area of pharmaceutical sciences.
My sincere thanks to my colleagues Mrs. S. Padma Priya and Dr. G. Poovi, Assistant professors, College of Pharmacy, MTPG & RIHS, Puducherry, India for their valuable comments during compilation of chapter write up.
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