AAPS: Transdermal Patch Shows Promise for HIV Therapy

IQP-0410 transdermal patch is non-toxic, doesn't degrade, and has potent in vitro activity

WEDNESDAY, Oct. 26 (HealthDay News) -- A transdermal patch has been developed which is capable of delivering the dual-acting HIV nonnucleoside reverse transcriptase inhibitor, IQP-0410, at therapeutic levels over an extended period, according to a study presented at the annual meeting and exposition of the American Association of Pharmaceutical Scientists, held from Oct. 23 to 27 in Washington D.C.

Anthony Ham, Ph.D., from ImQuest Biosciences in Frederick, Md., and colleagues investigated the feasibility of transdermal patches for delivery of IQP-0410. Solvent cast manufacturing was used to formulate IQP-0410 into ethyl cellulose/HPMC-based film patches. The bioactivity of IQP-0410 was evaluated by testing its in vitro antiviral activity, mechanism of action, and toxicity in primary and established cells. In vitro and ex vivo testing of patches was performed.

The investigators found that there was no toxic irritation to the epidermal tissue with flexible, strong transdermal patches. IQP-0410 was loaded into the patches at 249 ± 7.22 µg/cm² and showed potent in vitro anti-HIV activity. On exposure to 95 percent relative humidity, hygroscopicity of 17.49 ± 0.78 percent was observed. Under in vitro conditions, 96.4 percent of IQP-0410 was released in a controlled manner over seven days, and was linearly delivered through the skin when applied to ex vivo epidermal tissue. No significant degradation of the patches was observed over three months under standard and accelerated stability conditions.

"Transdermal patches applied to permeable substrate are capable of non-toxic delivery of IQP-0410 at therapeutic levels over extended periods following a single application," the authors write.

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