Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: Development,characterization, and performance evaluation |
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Authors: | Subheet Jain Rachna Sapre Ashok K Tiwary Narendra K Jain |
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Institution: | (1) The First Affiliated Hospital, College of Medicine, Zhejiang University, #79 QingChun Road, Hangzhou, Zhejiang Province, China;(2) Institution of Pharmaceutics, Zhejiang University, Hangzhou, China |
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Abstract: | The present investigation aimed at formulation, performance evaluation, and stability studies of new vesicular drug carrier
system protransfersomes for transdermal delivery of the contraceptive agent, levonorgestrel. Protransfersome gel (PTG) formulations
of levonorgestrel were prepared and characterized for vesicle shape, size, entrapment efficiency, turbidity, and drug permeation
across rat skin and were evaluated for their stability. The system was evaluated in vivo for biological assay of progestational
activity including endometrial assay, inhibition of the formation of corpora lutea, and weight gain of uterus. The effects
of different formulation variables (type of alcohol, type and concentration of surfactant) on transdermal permeability profile
were assessed. The optimized PTG formulation showed enhanced in vitro skin permeation flux of 15.82±0.37 μg/cm2/hr as compared to 0.032±0.01 μg/cm2/hr for plain drug solution. PTG also showed good stability and after 2 months of storage there was no change in liquid crystalline
nature, drug content, and other characteristic parameters. The peak plasma concentration of levonorgestrel (0.139±0.05 μg/mL)
was achieved within 4 hours and maintained until 48 hours by a single topical application of optimized PTG formulation. In
vivo performance of the PTG formulation showed increase in the therapeutic efficacy of drug. Results indicated that the optimized
protransfersomal formulation of levonorgestrel had better skin permeation potential, sustained release characteristic, and
better stability than proliposomal formulation. |
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Keywords: | contraception transdermal delivery protransfersomes levonorgestrel stability |
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