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载吲哚美辛纳米粒的设计：聚合物基质和表面活性剂的影响。

Design of indomethacin-loaded nanoparticles: effect of polymer matrix and surfactant.

机构信息

Laboratório de Pesquisa em Fármacos, Centro de Ciências Biológicas e da Saúde, Colegiado de Farmácia, Universidade Federal do Amapá, Brazil ; Programa de Pós-Graduação em Biodiversidade Tropical, Universidade Federal do Amapá, Brazil.

出版信息

Int J Nanomedicine. 2013;8:3467-77. doi: 10.2147/IJN.S47621. Epub 2013 Sep 13.

DOI:10.2147/IJN.S47621
PMID:24092971
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3787932/
Abstract

Despite recent advances in nonsteroidal anti-inflammatory drug (NSAID) formulations, the design of targeted delivery systems to improve the efficacy and reduce side effects of NSAIDs continues to be a focus of much research. Enteric nanoparticles have been recognized as a potential system to reduce gastrointestinal irritations caused by NSAIDs. The aim of this study was to evaluate the effect of EUDRAGIT® L100, polyethylene glycol, and polysorbate 80 on encapsulation efficiency of indomethacin within enteric nanoparticles. Formulations were developed based on a multilevel factorial design (three factors, two levels). The amount of polyethylene glycol was shown to be the factor that had the greatest influence on the encapsulation efficiency (evaluated response) at 95% confidence level. Some properties of nanoparticles like process yield, drug-polymer interaction, particle morphology, and in vitro dissolution profile, which could affect biological performance, have also been evaluated.

摘要

尽管非甾体抗炎药 (NSAID) 制剂在最近取得了进展，但设计靶向递送系统以提高 NSAIDs 的疗效并降低其副作用仍然是许多研究的重点。肠溶性纳米粒已被认为是一种降低 NSAIDs 引起的胃肠道刺激的潜在系统。本研究旨在评估 EUDRAGIT® L100、聚乙二醇和聚山梨酯 80 对吲哚美辛在肠溶性纳米粒中包封效率的影响。根据多级析因设计（三个因素，两个水平）开发了配方。在 95%置信水平下，聚乙二醇的量被证明是对包封效率（评估响应）影响最大的因素。还评估了一些纳米粒的性质，如工艺收率、药物-聚合物相互作用、颗粒形态和体外溶解曲线，这些性质可能会影响生物性能。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9915/3787932/bd2d0186a111/ijn-8-3467Fig12.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9915/3787932/60455422cab5/ijn-8-3467Fig7.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9915/3787932/fa7f97899343/ijn-8-3467Fig8.jpg
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https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9915/3787932/bd2d0186a111/ijn-8-3467Fig12.jpg

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