Effect of Chemical Penetration Enhancer-Adhesive Interaction on Drug Release from Transdermal Patch: Mechanism Study Based on FT-IR Spectroscopy, 13.sup.C NMR Spectroscopy, and Molecular Simulation.

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Date: July 2021
From: AAPS PharmSciTech(Vol. 22, Issue 5)
Publisher: Springer
Document Type: Report; Brief article
Length: 255 words

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Abstract :

Keywords: KEY WORDS Chemical penetration enhancer; Drug release; Transdermal patch; Miscibility; Hydrogen bonding Abstract Chemical penetration enhancers (CPEs) are commonly added into transdermal patches to impart improved skin permeation of drug. However, significant unexplained variability in drug release kinetics in transdermal patches is possible as a result of the addition of CPEs investigations into the underlying mechanisms are still limited. In the present study, a diverse set of CPEs was employed to draw broad conclusions. Solubility parameters of CPEs and acrylate pressure-sensitive adhesive were calculated by molecular dynamics simulation and Fedors group contribution method to evaluate drug-adhesive miscibility. CPE-adhesive interaction was characterized by FT-IR study, 13.sup.C NMR spectroscopy, and molecular docking simulation. Results showed that release enhancement ratio (ER.sub.R) of CPEs for zolmitriptan was rank ordered as isopropyl myristate azone Plurol Oleique.sup.® CC497 Span.sup.® 80 N-methylpyrrolidone Transcutol.sup.® P. It was found that solubility parameter difference (Î[delta]) between CPE and adhesive was negatively related with ER.sub.R. It was proved that hydrogen bonding between CPE and adhesive would increase drug release rate, but only if the CPE showed good miscibility with adhesive. CPE like isopropyl myristate, which had good miscibility with adhesive, could decrease drug-adhesive interaction leading to the release of drug from adhesive. Author Affiliation: (1) Department of Pharmaceutical Sciences, Shenyang Pharmaceutical University, 103 Wenhua Road, 110016, Shenyang, Liaoning, China (2) College of Pharmacy, Beihua University, 3999 East Binjiang Road, 132013, Jilin, Jilin, China (e) fangliang2003@yahoo.com Article History: Registration Date: 05/17/2021 Received Date: 03/09/2021 Accepted Date: 05/15/2021 Online Date: 06/30/2021 Byline:

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Gale Document Number: GALE|A667039442