IMPRACTICALITY EXAMINATION FOR TRANSDERMAL TRANSFER OF ELVITEGRAVIR INTERPRETATIONS

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Dr. Hina Umbreen, Dr. Iqra Sadaf, Dr. Sidra Tahir

Abstract-The aim of this study was to test the feasibility of transdermal delivery of elvitegravir (EVG), a potent HIV-1 integrase inhibitor for development of a transdermal patch of the same for HIV prophylaxis. The targeted skin permeation flux was about 25 μg/cm2/h. In vitro drug permeation studies were performed using vertical Franz diffusion cells. Passive permeation of EVG through dermatomed human skin and human epidermis was investigated. Effect of 5% w/w oleic acid, 25% v/v ethanol, 40% w/w dimethyl sulfoxide, 10% w/w lauric acid, and combination of 20% w/w dimethyl sulfoxide, 10% w/w oleic acid, and 5% w/w lauric acid in propylene glycol on the permeation of EVG through human epidermis was evaluated. Phosphate buffered saline (pH 7.4) containing 10% v/v propylene carbonate and/or polyethylene glycol 400 was used as the receptor. Sampling of the receptor was performed at pre-determined time points for 168 h and analysis was done using HPLC. Permeation of EVG through dermatomed human skin and human epidermis from its free solution in propylene glycol was found to be 5.51 ± 3.48 μg/cm2 and 21.14 ± 3.23 μg/cm2 (control), respectively after 168 h. Oleic acid and dimethyl sulfoxide significantly enhanced the permeation of EVG to 235.97 ± 49.06 μg/cm2 and 700.01 ± 107.03 μg/cm2, respectively, through human epidermis in comparison to the control group (p<0.05). Overall, even with the use of different enhancers or their combination, the targeted permeation flux was not achieved. EVG was thus, not considered further for patch development.

Elvitegravir (EVG), Potent HIV-1, HIV prophylaxis