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萘普生和吲哚美辛从多孔顺式-1,4-聚异戊二烯基质的电控透皮给药

Electrically controlled transdermal delivery of naproxen and indomethacin from porous cis-1,4-polyisoprene matrix.

作者信息

Ruangmak Kamonpan, Paradee Nophawan, Niamlang Sumonman, Sakunpongpitiporn Phimchanok, Sirivat Anuvat

机构信息

The Petroleum and Petrochemical College, Chulalongkorn University, Bangkok, Thailand.

Sustainable Polymer & Innovative Composite Materials Research Group, Faculty of Science, Department of Chemistry, King Mongkut's University of Technology Thonburi, Bangkok, Thailand.

出版信息

J Biomed Mater Res B Appl Biomater. 2022 Feb;110(2):478-488. doi: 10.1002/jbm.b.34926. Epub 2021 Aug 16.

DOI:10.1002/jbm.b.34926
PMID:34399032
Abstract

This study is focused on the inquiry of using a porous polymeric structure to absorb and release transdermally two drugs through a skin from deproteinized natural rubber latex (DPNR). The porous DPNR films were fabricated from the internal formation of surfactant micelles and their subsequent leaching out to generate porous structures. The pore size of DPNR films increased with increasing surfactant amount. The model drugs were naproxen and indomethacin; their releases and release-permeations were investigated under the effects of surfactant amount, electrical potential, and drug size. Without electric field, the drug release mechanism was mainly driven by concentration gradient. The higher amount of drug released was obtained from the matrix with a larger pore size. Under electric field, the higher amounts of drug release were obtained in the shorter drug release durations, via the electrorepulsive force between the negatively charged drugs and the cathode electrode. The molecular drug size was a factor for the drug absorption, release rate and amount. For the drug release-permeation experiment through the pig skin, there were two release-permeation periods as governed by the combination of concentration gradient and swelling in the first period, and the matrix erosion in the second period. The fabricated porous DPNR films have been shown here to be potential to be used as a transdermal patch with electrically controllable drug release rate, amount and duration along with the facile drug-matrix loading and absorption.

摘要

本研究聚焦于探究使用多孔聚合物结构通过皮肤从脱蛋白天然橡胶胶乳(DPNR)中经皮吸收和释放两种药物。多孔DPNR膜是由表面活性剂胶束的内部形成及其随后的浸出以产生多孔结构而制成的。DPNR膜的孔径随表面活性剂用量的增加而增大。模型药物为萘普生和吲哚美辛;研究了在表面活性剂用量、电势和药物大小的影响下它们的释放及释放-渗透情况。在没有电场的情况下,药物释放机制主要由浓度梯度驱动。从具有较大孔径的基质中获得的药物释放量更高。在电场作用下,通过带负电荷的药物与阴极之间的电排斥力,在较短的药物释放持续时间内获得了更高的药物释放量。分子药物大小是药物吸收、释放速率和释放量的一个影响因素。对于通过猪皮的药物释放-渗透实验,存在两个释放-渗透阶段,第一阶段由浓度梯度和溶胀共同作用控制,第二阶段由基质侵蚀控制。此处展示的所制备的多孔DPNR膜具有用作经皮贴剂的潜力,其药物释放速率、释放量和持续时间可通过电控制,同时药物-基质加载和吸收简便易行。

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