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Abstract

SCREENING OF NATURAL PERMEATION ENHANCERS (ESSENTIAL OILS) IN FORMULATION AND DEVELOPMENT OF TRANSDERMAL PATCHES

Samyuktha Metta*, M. Venkata Swamy, Naveena R., Madasani Nikitha Reddy, Swarna Latha Nagadani and Kadagoni Pravalika

Abstract

The drug delivery by oral route is so far most convenient and accepted route of drug delivery but now a day‟s considerable interest has been increased in delivery of drugs through skin to the systemic circulation and for local effect. However, the outer most layer of the human skin, stratum corneum; possess the formidable barrier to drug penetration thereby reducing bio-availability. Most of the drugs do not have an ability to penetrate the stratum corneum. Owing to the side effects of chemical penetration enhancers interest has been aroused among researchers to find out natural sources as penetration enhancers to improve the bio-availability of drugs so that they can be delivered through skin. A popular approach for improving transdermal drug delivery involves the use of penetration enhancers (sorption promoters or accelerants) which penetrate into skin to reversibly reduce the barrier resistance. The potential mechanisms of action of penetration enhancers include disruption of intercellular lipid and/or keratin domains and tight junctions. This results in enhanced drug partitioning into tissue, altered thermodynamic activity/solubility of drug etc. Synthetic chemicals (solvents, azones, pyrrolidones, surfactants etc.) generally used for this purpose are rapidly losing their value in transdermal patches due to reports of their absorption into the systemic circulation and subsequent possible toxic effect upon long term application. Essential oils are included in the list of Generally Recognized As Safe (GRAS) substances and have low irritancy potential. The current work was aimed to screen percutaneous permeation enhancement of various natural permeation enhancers (Essential oils) for transdermal delivery of an antifungal drug (Itraconazole) as they have minimum chances of side effects and have improved efficacy compared to chemical enhancers. The patches were formulated using different natural permeation enhancers (Essential oils such as pepper oil, clove oil & Ginger oil) in 2 different ratios. The physicochemical evaluation of the patches was performed for suitability. In vitro permeation studies were performed using Goat skin as the permeating membrane in Franz diffusion cell. The result indicated that maximum release was obtained at 6% of clove oil and it was concluded that that the problems of Itraconazole on oral administration like dissolution rate limited absorption of drug, gastric side effects, ulcer and bleeding can be overcome by applying Itraconazole topically in the form of transdermal patch & natural permeation enhancers (Essential oils) are suitable for effective delivery of drug via transdermal route.

Keywords: Transdermal, HPMC, EC, Eudragit, Itraconazole, Permeation enhancers, Pepper oil, Clove oil, Ginger oil.


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