Singh Neha, Seedat Fehmeeda, Pillay Viness, Sweet Joe L, Danckwerts Michael P
Department of Pharmacy and Pharmacology, University of the Witwatersrand, Parktown, South Africa.
J Microencapsul. 2006 Mar;23(2):153-67. doi: 10.1080/02652040500435139.
The application of nicotine in the research phase of Alzheimer's disease (AD) treatment has shown promise. The present study was aimed at understanding the incorporation of nicotine into poly-lactic acid (PLA) and poly(D,L-lactic-co-glycolic) acid (PLGA) microparticles which were then re-incorporated into a cross-linked zinc-alginate-pectinate polyspheric multi-particulate system to be employed as a possible brain implant for the treatment of AD. The Box-Behnken design was employed to prepare 15 PLA-PLGA formulations, which were tested for their drug incorporation efficiency and release potential and subsequently optimized using multiple regression and an artificial neural network generalized feed-forward model. Based on the rapid burst effect from the microparticles, further incorporation was conducted in a zinc-alginate-pectinate system using ionotropic gelation. Although double incorporation continued to provide a burst effect, this was followed by a lag period for 7 days and a second phase of drug release.
尼古丁在阿尔茨海默病（AD）治疗研究阶段的应用已显示出前景。本研究旨在了解尼古丁掺入聚乳酸（PLA）和聚（D，L-乳酸-共-乙醇酸）（PLGA）微粒中的情况，然后将这些微粒重新掺入交联的锌-藻酸盐-果胶酸盐多球形多微粒系统中，用作治疗AD的一种可能的脑植入物。采用Box-Behnken设计制备了15种PLA-PLGA制剂，测试了它们的药物掺入效率和释放潜力，随后使用多元回归和人工神经网络广义前馈模型进行优化。基于微粒的快速突释效应，利用离子凝胶法在锌-藻酸盐-果胶酸盐系统中进行了进一步掺入。虽然双重掺入继续产生突释效应，但随后有7天的延迟期和第二阶段的药物释放。
