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Abstract

Protransfersomes For Effective Transdermal Delivery Of Norgestrel Preparation And In Vitro Characterization

Author(s): S Jain, R Sapre, R.B Umamaheswari, N.K Jain

The present study was aimed at formulation, performance evaluation and stability studies of new vesicular drug carriers system called protransfersomes bearing norgestrel. Protranfersomes of norgestrel were prepared and extensively characterized for drug loading, vesicular shape, vesicular size and size distribution, entrapment efficiency, degree of deformability, transit time, rate of hydration, drug diffusion across rat skin and stability study at 4o and at room temperature. The effects of various parameters such as type of alcohol, type of surfactant and amount of drug of formulation on transdermal permeability profile were assessed. In vitro flux, permeability coefficient and release rate pattern of norgestrel was calculated for transdermal delivery of norgestrel. In the release rate study, no lag phase could be detected and the release of norgestrel from proposed formulation through rat skin was found to be constant but slow (sustained release). Entrapment efficiency was found to be nearly 95% and it depends on the type of surfactant and concentration of surfactant. After one month storage of formulation in liquid crystalline nature, drug content and other characteristic parameters were not changed. Proposed system also cornpared for in vitro performance with well-known vesicular system proliposomes, and shows better skin permeation. Results indicate that the protransfersomal formulation for transdermal drug delivery of norgestrel provides effective contraception, better stability, higher entrapment efficiency, ability as a self penetration enhancer, easy to scale up and better for transdermal delivery as compared to proliposomes.