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Presented by , Ms. Kiran Wanare M- Pharm ( Pharmacognosy & Phytochemistry ) HERBAL NOVEL DRUG DELIVERY SYSTEM


INTRODUCTION Novel drug delivery system is advantageous in delivering the herbal drug at predetermined rate and delivery of drug at the site of action which minimizes the toxic effects with the increase in bioavailability of the drugs . In novel drug delivery technology , control of the distribution of drug is achieved by incorporating the drug in carrier system or in changing the structure of the drug at molecular level . Herbal drugs are becoming more popular in the modern world for their application to cure variety of diseases with less toxic effects and better therapeutic effects 1/5/2013 2

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The novel carriers should ideally fulfill two prerequisites . Firstly, it should deliver the drug at a rate directed by the needs of the body, over the period of treatment . Secondly , it should channel the active entity of herbal drug to the site of action 1/5/2013 3

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In phyto -formulation research, developing nano dosage forms (polymeric nanoparticles and nanocapsules , liposomes , solid lipid nanoparticles , phytosomes and nanoemulsion etc .) have a number of advantages for herbal drugs, including enhancement of solubility and bioavailability, protection from toxicity, enhancement of pharmacological activity, enhancement of stability, improving tissue macrophages distribution , sustained delivery, protection from physical and chemical degradation etc . Thus the nano sized novel drug delivery systems of herbal drugs have a potential future for enhancing the activity and overcoming problems associated with plant medicines 1/5/2013 4

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The method by which a drug is derived can have a significant effect on its efficacy. An optimum amount of the concerned drug is administered to the patient in such a way that it reaches exactly the ‘site of action’ and produce therapeutic effects. Some drugs have an optimum concentration range within which maximum benefit is derived, and conc above or below this range can be toxic or produce no therapeutic benefit at all. To minimize drug degradation and loss, to prevent harmful side-effects and to increase drug bioavailability and the fraction of drug accumulated in the required zone, Various drug delivery and drug targeting system are currently under development. 1/5/2013 5

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Novel drug delivery system is a new approach to drug delivery. It helps the drug to act longer and more effectively. This overcomes limitations of old methods of drug administration, In novel drug delivery technology, control of the distribution of drug is achieved by incorporating the drug in carrier system or in changing the structure of the drug at molecular level 1/5/2013 6

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Drawbacks of conventional dosage forms Poor patient compliance, increased chances of missing the dose of a drug with short half life for which frequent administration is necessary. The unavoidable fluctuation of drug conc may lead to under medication or over medication. A typical peak valley plasma conc time profile is obtained which make attainment of steady state condition difficult. The fluctuations in drug levels may lead to precipitation of adverse effects especially of a drug with small therapeutic index whenever over medication occur 1/5/2013 7

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Advantages of novel drug delivery system Enhancement of solubility. Increased bioavailability. Protection from toxicity. Enhancement of pharmacological activity Enhancement of stability. Improved tissue macrophages distribution. Sustained delivery. Protection from physical and chemical degradation. 1/5/2013 8

Herbal drugs : 

Herbal drugs Herbal formulation means a dosage form consisting of one or more herbs or processed herb in specified quantities to provide specific nutritional, cosmetic benefits, and other benefits meant for use to diagnose treat, or to alter the structure or physiology of human beings or animals. Herbal preparations are obtained by subjecting whole plants, fragmented or cut plants, plants part to treatment such as extraction, distillation, expression fractionation, purification, concentration or fermentation. This include comminuted or powdered herbal substances,extract . essential oils, expressed juices etc 1/5/2013 9

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Advantages of herbal drugs 1 Low risk of side effect 2 More effectiveness. 3 Lower cost 4 Widespread availability Limitation of Herbal drug 1 Not suitable for many disease 2 Lack of dosage instruction 3 Poison risk associated with wild herbs 4 Lack of regulation 5 Longer duration of treatmen t 1/5/2013 10

Different novel drug delivery system for herbal drugs: 

Different novel drug delivery system for herbal drugs 1/5/2013 11

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LIPOSOME Liposomes are biodegradeable , colloidal and spherical vesicles (0.05-5.0 μm in diameter) composed of a bilayer membrane entrapping an aqueous core. Aqueous core enclosed in one or more phospholipids layer used to convey vaccine, drug, enzyme or other subs to target cell or organ. Li et al. prepared liposomes containing extract of T.wilfordii thin-film dispersion method . 1/5/2013 12

Advantages of liposome formulation : 

Advantages of liposome formulation Hydrophobic and hydrophilic drug can be delivered. Liposome herbal therapy acts as a carrier for small cytotoxic molecules and as vehicle for macromolecules as gene. Sustained and controlled release of formulation can be possible. 1/5/2013 13

Liposomal herbal formulation & their applications: 

Liposomal herbal formulation & their applications Name of Bioactive Component/Plant Application Reference Essential oil of Atractylodes macrocephala Koidz Increase in solubility & bioavailability 5 Essential oil of O. dictamnus Increase in activity 5 Extracts of Tripterygium wilfordi Reduction in side effect 6 Quercetin Increase in bioavailability and reduction in side effect 7 Silymarin extract Increase in hepatoprotective activity 8 Essential oil of Artemisia arborescens L. Increase in stability 9 Capsaicin Increase in permeation as prolongation of action 10 Taxanes Decrease in toxicity 11 1/5/2013 14


ETHOSOMES Ethosomes are vesicles composed of phospholipids and high concentration of ethanol. High concentration of ethanol in the vesicles led to enhancement in their permeability through the skin by fluidising the lipid domain of the skin. Zhou et al. developed a novel transmembrane pH gradient active loading method to prepare alkaloids binary ethosomes of sophora alopecuroides below the phase trasition temperature of the phosphatidyl choline . 1/5/2013 15

Advantages of ethanol drug delivery: 

Advantages of ethanol drug delivery Transermal permeationn of drug through skin can be enhanced. Large amount of diverse groups of drugs can be delivered. The ethosomal drug is administered in semisolid form, resulting in improved patient compliance. 1/5/2013 16


TRANSFEROSOMAL Transferosomal are phospholipid vesicles which act as potential carriers for the transdermal delivery of the drug as they overcome the difficulty of penetration through the intracellular pores of the skin due to their flexibility. Patel et al. prepared transferosomes containing the curcumin gel and an increase in the permeation was observed when compared with the simple gel through the skin 1/5/2013 17

Herbal Transferosomal and ethosomal formulation: 

Herbal Transferosomal and ethosomal formulation Name of Bioactive component/Plant Application Reference Capsaicin Transferosomes Increased skin penetration 12 Curcumin Transferosomes Increased skin penetration 13 Vincristine Transferosomes Increase in Permeability 14 Colchicine Transferosomes Reduction in GIT side effects 15 Ammonium Glycyrrhizinate Increase drug permeation through dermis 16 TRiptolide Increase in Bioavailability 17 Sophpra alopencerides Increase in Permeability 18 1/5/2013 18


PHYTOSOME Phytosome process the phosphotidylcholine and the plant components actually form a 1:1 or a 2:1 molecular complex depending on the substance(s) complexes, involving chemical bonds. The flavonoid and terpenoid constituents of plant extracts lend themselves quite well for the direct binding to phosphatidylcholine . Phytosomes results from the reaction of a stoichiometric amount of the phospholipid ( phosphatidylcholine ) with the standardized extract or polyphenolic constituents (like simple flavonoids ) in a non polar solvent. 1/5/2013 19

Advantages of phytosomes : 

Advantages of phytosomes It enhances the absorption of lipid insoluble polar phytoconstituents through oral as well as topical route showing better bioavailability, hence significantly greater therapeutic benefit. As the absorption of active constituent(s) is improved, its dose requirement is also reduced. Phosphatidylcholine used in preparation of phytosomes , besides acting as a carrier also acts as a hepatoprotective , hence giving the synergistic effect when hepatoprotective substances are employed. Chemical bonds are formed between phosphatidylcholine molecule and phytoconstituent , so the phytosomes show better stability profile . Added nutritional benefit of phospholipids. 1/5/2013 20

Phytosomal Herbal Products: 

Phytosomal Herbal Products Phytosomes Source Use Silybin Phytosomes Silybin flavonoids from Silybium marianum Hepatoprotective , antioxidant for liver Ginkgo Phytosomes Ginkgo flavonoids from Ginkgo biloba Protect brain and vascular linings Ginseng Phytosomes Ginsenosides from Panax ginseng Nutraceuticals and immuno modulator Green tea Phytosomes Epigallocatechin from Tea sinesis Anticancer, Nutraceuticals Grape seedPhytosomes Procyanidins from Vitis vinifera Nutraceuticals , cardio protective Olive oil Phytosomes Polyphenol from Olea europaea oil Antioxidant 1/5/2013 21


IMPLANT These are the polymeric devices which are used for the controlled and sustained delivery of the drugs. These are directly placed in the body fluids/cavities and are fabricated by using biodegradable polymers. A microsurgery is always required for the insertion of these devices . Implants of the extract of danshen ( Radix Salviae Miltiorrhizae ) were developed using the chitosan and gelatin 1/5/2013 22


MICRO-EMULSIONS Nanoemulsions and Microemulsions are the emulsions of O/W type having the size range of several microns. They are prepared by using the surfactants which are considered safe for the human use and approved by the FDA. These types of emulsions have higher surface area and hence can easilypenetrate through the skin. They are also non toxic and non irritant in nature and can be used in the animals and veterinarypurpos . Nanoemulsions can be prepared by the high pressure homogenization and microfluidisation technique . 1/5/2013 23

Marketed novel drug delivery formulations of plant active and extracts.: 

Marketed novel drug delivery formulations of plant active and extracts. Brand name Plant active/extracts Type of NDDS Company name Reference White tea liposome Herbasec Camellia sinesis extract Liposome Cosmetochem 19 Green tea liposome Herbasec Camellia sinesis extract Liposome Cosmetochem 20 White hibiscus liposome Herbasec White hibiscus extract Liposome Cosmetochem 21 Aloe vera liposome Herbasec Aloe vera extract Liposome Cosmetochem 22 Guarana liposome Herbasec Guarana extract Phytosome Cosmetochem 23 1/5/2013 24

Recent Patents on Novel Herbal Formulations: 

Recent Patents on Novel Herbal Formulations US patent No. Active ingredient Novel System incorporate Reference US 5948414 Opioid analgesic and aloe Nasal spray 24 US 6340478 B1 Ginsenosides Microencapsulated and controlled release formulation 25 US 6890561 B1 Isoflavones Microencapsulated formulation 26 US 6896898 B1 Alkaloids of Aconitum Sp. Transdermal delivery system 27 US patent 2007,0042062 A1 Glycine max containing 7s globulin protein extract, curcumin , Ginger officinalis Herbal Tablet dosage form 28 1/5/2013 25


References Medina OP, Zhu Y, Kairemo K. Curr Pharm Des 2004;10:2981–9. Sharma G, Anabousi S, Ehrhardt C, Kumar MNVR. J Drug Target2006;14:301–10. Terreno E, Castelli DD, Cabellab C, DastruW, Saninoa A, Stancanellob J, et al. Chem Biodivers 2008;5:1901–2. Chanchal D, Swarnlata S. J Cosmet Dermatol 2008;7:89–95. Wen Z, Liu B, Zheng Z, You X, Pu Y, Li Q. Preparation of Liposomes entrapping essential oil from Atractylodes macrocephala Koidz by modified RESS technique. Chem Eng Res Design 2010; 88 (8A):1102-1107. 1/5/2013 26

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Li HR, Li SF, Duan HQ. Preparation of liposomes containing extracts of Tripterygium wilfordii and evaluation of its stability. Zhongguo Zhong Yao Za Zhi 2007; 32(20):2128-31. Priprem A, Watanatorn J, Sutthiparinyanont S, Phachonpai W and Muchimapura S. Anxiety and cognitive effects of Quercetin liposomes in rats. Nanomedicine 2008; 4:70-78. Mohamed S, El- Samaligy , Nagia NA, Mahmoud EA. Evaluation of hybrid liposomes -encapsulated silymarin regarding physical stability and in vivo performance. Int J Pharm 2006; 319:121-129. Sinico C, Logu AD, Lai F et al. Liposomal incorporation of Artemisia arborescens L. essential oil and in vitro antiviral activity. Eur J Pharm Biopharm , 2005; 59:161-168. Mahajan A, Mangat P, Bhatia A, Katare OP. A novel herbal capsaicin loaded liposomal formulation: design, development and evaluation. Pharmaceutical sciences, section11. July 2010. Available from: URL: http:// www.puchd.ac.in/csc2007/abstract/section_11- PHARM.pdf Straubinger RM, Balasubramanian SV. Preparation and characterization of Taxane containing liposomes . Methods Enzymol 2005; 391: 97-117. 1/5/2013 27

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Xiao-Ying L, Luo JB, Yan ZH, Rong HS, Huang WM. Preparation and in vitro-in vivo evaluations of topically applied capsaicin transferosomes . Yao Xue Xue Bao 2006 ; 41(5):461-466. Patel R, Singh SK, Singh S, Sheth NR, Gendle R. Development and characterization of curcumin loaded transferosomes for transdermal delivery. J Pharm Sci 2009 ; 1(4):71-80. Lu Y, Hou SX, Chen T, Sun YY, Yang BX and Yuan ZY. Preparation of transferosomes of vicristine sulfate and study on its precutaneous penetration. Zhongguo Zhong Yao Za Zhi 2005, 30(12): 900-903. Singh Pal Harvinder , Utreja Puneet , Tiwari Kumar Ashok , Jain Subheet . Elastic Liposomal formulation for sustained Del ivery of colchicine : In vi t ro Characterization and in vivo evaluation of Anti-Gout Activity . American Association of Pharmaceutical Scientists 2009,11(1):54-64 Patel S. Ethosomes : A promising tool for Transdermal delivery of drug. August 2010. Available from: URL: http ://www. Pharmainfo . Net Gangwar S, Singh S, Garg G. Ethosomes : A novel tool for drug delivery through skin. J Pharm Res 2010; 3(4 ):688-691. 1/5/2013 28

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Paolino D, Lucania G, Mardente D, Alhaique F, Fresta M. Ethosomes : for skin delivery of ammonium glycyrrhizinate : in vitro percutaneous permeation through human skin and in vivo anti inflammatory activity on human volunteers. J Control Release 2005; 106: 99-110. Ind J Pharm Edu Res, Jul-Sept, 2011/ Vol 45/ Issue 3 233 Ashwani Goyal et al Potential of Novel Drug Delivery Systems for Herbal Drugs Chen Jin- Guang , Liu Feng Yu, Gao Tian Wen . Preparation and anti inflammatory activity of triptolideethosomes in an erythema model. Journal of Liposomal Research 2 0 1 0 ; 2 0 ( 4 ) : 2 9 7 - 3 0 3 ( 7 ) . Bombardelli E, Curri SB, Gariboldi PG. Fitoterapia 1989;60:55–70. Bombardelli E. Boll Chim Farma 1991;130:431–8. Bombardelli E ( Indena S.P.A.). Pharmaceutical and cosmetic compositionscontaining complexes of flavanolignans with phospholipids. Bombardelli E, Patri G, Pozzi R ( Indena S.p.A .). Complexes of saponins and their aglycons with phospholipids and pharmaceutical and cosmetic compositions containing them Patent US5166139, 1992. 1/5/2013 29

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Wiersma JG, inventors ; Nouvean Technologies, Inc., Tequesta, Fla , Assignee. Herbal Based Nasal Spray. US patent 5,948,414, 1999 Sep 7. Blatt Y , Kimmelman E, Cohen D, Rotman A, inventors; Bio Dar Ltd., yavne (IL), Assignee . Microencapsulated and Controlled-Release Herbal Formulations. US patent 6,340,478 B1, 2002 Jan 22. Blatt Y, Arad O, Kimmelman E, Cohen D, Pinto R, Rotman A, inventors; Bio Dar Ltd., Yavne (IL), Assignee. Microencapsulated and Controlled- ReleaseFormulations of Isoflavones from enriched fractions of Soy and other Plants. US Patent 6,890,561 B1, 2005May 10. Xiong W, Patel DC, inventors; XEL Herbaceuticals,Inc ., Salt Lake city, UT (US), Assignee. TransdermalDelivery System for Alkaloids of Aconitum Species. USpatent 6,896,898 B1, 2005 May 24. Pushpangadan P, Rao CV, Kartik R, Mehrotra S, GoelRK , Acharya S, Somanathan M, inventors; Council ofscientific and industrial research, New Delhi, Assignee. Novel herbal formulation as brain tonic. US patent 2005/0142232 A1, 2005 June 30. 1/5/2013 30