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导电聚并苯和增塑剂在脱蛋白天然橡胶透皮贴片中的效果对电控制萘普生释放-渗透的影响。

Effects of conductive polyazulene and plasticizer embedded in deproteinized natural rubber transdermal patch on electrically controlled naproxen release-permeation.

机构信息

The Petroleum and Petrochemical College, Chulalongkorn University, Bangkok 10330, Thailand.

Department of Chemistry, Faculty of Science, King Mongkut's University of Technology Thonburi, Bangkok 10140, Thailand.

出版信息

Int J Pharm. 2019 Apr 20;561:296-304. doi: 10.1016/j.ijpharm.2019.02.046. Epub 2019 Mar 6.

Abstract

Naproxen (Npx) was utilized as an anionic drug and loaded in the deproteinized natural rubber (DPNR) films prepared by the UV irradiation. The in-vitro drug release-permeation from the DPNR films and through the pig skin was investigated under the effects of the plasticizer type and amount, silicone oil (Si) and dibutyl phthalate (DBP), applied electric potential, and used conductive polyazulene as the drug encapsulation host. The drug release-permeation consisted of 2 successive periods: the pore formation period and release-permeation period. In the first period, the scaling exponent n values were between 0.5 and 1 indicating the decreasing drug rate with time. In the second stage, the scaling exponent n values were higher than 1 indicating the increasing drug rate with time. The Npx release-permeation amount increased with increasing amount of hydrophilic plasticizers. The efficiency of plasticizers on the Npx release-permeation amount was ranked as follows: DBP > Si. The Npx release-permeation amount was drastically enhanced from the applied electrical potential due to the electro-repulsive force between the negatively charged drug and the negatively charged electrode, and the presence of the Npx-doped conductive polyazulene. Other characteristics were also investigated in details namely the matrix morphology, and the pore formation during the two periods.

摘要

萘普生(Npx)被用作阴离子药物,并负载在通过紫外光照射制备的脱蛋白天然橡胶(DPNR)膜中。在施加的电场、用作药物封装主体的导电聚蓝以及不同类型和用量的增塑剂的影响下,研究了 DPNR 膜中以及通过猪皮的体外药物释放-渗透。药物释放-渗透包括 2 个连续阶段:成孔阶段和释放-渗透阶段。在第一阶段,标度指数 n 值在 0.5 到 1 之间,表明药物随时间的释放速率降低。在第二阶段,标度指数 n 值大于 1,表明药物随时间的释放速率增加。随着亲水性增塑剂用量的增加,Npx 的释放渗透量增加。增塑剂对 Npx 释放渗透量的效率排序如下:DBP > Si。由于带负电荷的药物和带负电荷的电极之间的电排斥力以及掺杂 Npx 的导电聚蓝的存在,施加电场会大大增加 Npx 的释放渗透量。还详细研究了其他特性,即基质形态和两个阶段的成孔。

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