Biomaterial Group, Faculty of Biomedical Engineering (Center of Excellence), Amirkabir University of Technology, P. O. Box 15875-4413, Tehran, Iran.
Appl Biochem Biotechnol. 2012 Nov;168(6):1434-47. doi: 10.1007/s12010-012-9868-4. Epub 2012 Sep 14.
The objective of the present study was to prepare a polymeric drug delivery system with no burst effect. To attain this goal, doxorubicin (Dox) as an effective anticancer drug was loaded into poly(lactide-co-glycolide) (PLGA) nanoparticles (NPs) to improve the drug performance and also maximize the release period. After the synthesis process, the freshly made PLGA NPs with two different lactide-to-glycolide ratios (75:25 and 50:50) were evaluated physically and chemically. To determine the encapsulation efficiency, a centrifugation method was applied. Also, the drug loading effect on particle size, polydispersity index, and zeta potential was examined. The results indicated that the NPs had nearly the same diameters around 360 nm, and the entrapment efficiencies for 75:25 PLGA and 50:50 PLGA were reported around 39 and 48 %, respectively. A slight increase in all parameters was observed due to the increase of the drug loading content. The primary release was 7.91 % (w/w) and 14.70 % (w/w) for 75:25 and 50:50 drug-loaded NPs, respectively; no burst effect was observed. After 20 days, the drug release was around 70.98 and 62.22 % of the total entrapped drug for 75:25 and 50:50 drug-loaded NPs, respectively. Finally, it was found that Dox was an appropriate anticancer agent with good capability to be encapsulated in polymeric NPs and could be released from the carriers with no burst effect and favor rate.
本研究的目的是制备无突释效应的聚合物药物传递系统。为了实现这一目标，将阿霉素（Dox）作为一种有效的抗癌药物载入聚（乳酸-共-乙醇酸）（PLGA）纳米粒（NPs）中，以提高药物性能并最大限度地延长释放周期。合成后，对两种不同乳酸-乙醇酸比例（75:25 和 50:50）的新鲜 PLGA NPs 进行物理和化学评估。为了确定包封效率，采用了离心法。还考察了药物载量对粒径、多分散指数和 Zeta 电位的影响。结果表明， NPs 的直径约为 360nm，75:25PLGA 和 50:50PLGA 的包封效率分别约为 39%和 48%。由于药物载量的增加，所有参数都略有增加。75:25 载药 NPs 和 50:50 载药 NPs 的初始释放率分别为 7.91%（w/w）和 14.70%（w/w）；没有突释效应。20 天后，75:25 和 50:50 载药 NPs 的总包封药物的药物释放率分别约为 70.98%和 62.22%。最后，发现 Dox 是一种合适的抗癌药物，具有良好的能力被封装在聚合物 NPs 中，可以从载体中无突释效应和有利的速度释放。
