载利伐斯的明 PLGA 和 PBCA 纳米粒的制备、优化、表征、体外及药效学研究。
Rivastigmine-loaded PLGA and PBCA nanoparticles: preparation, optimization, characterization, in vitro and pharmacodynamic studies.
机构信息
TIFAC Centre of Relevance and Excellence, Centre of PG studies and Research, Pharmacy Department, The Maharaja Sayajirao University of Baroda, Donors Plaza, Fatehgunj, Vadodara 390002, Gujarat, India.
出版信息
Eur J Pharm Biopharm. 2010 Oct;76(2):189-99. doi: 10.1016/j.ejpb.2010.07.007. Epub 2010 Jul 15.
Sustained release nanoparticulate formulations of Rivastigmine tartrate (RT) were prepared, optimized (using factorial design) and characterized using the biodegradable polymers, PLGA and PBCA as carriers. The pharmacodynamic performances of the nanoparticles (NPs) were evaluated for brain targeting and memory improvement in scopolamine-induced amnesic mice using Morris Water Maze Test. PLGA NPs were prepared by nanoprecipitation technique, while PBCA NPs were prepared by emulsion polymerization technique. Effect of key formulation variables on particle size (PS) and percentage drug entrapment (PDE) of NPs was studied by using factorial design. PLGA NPs showed PS of 135.6±4.2nm and PDE of 74.46±0.76 %, whereas PBCA NPS showed PS of 146.8±2.6nm and PDE of 57.32±0.91%. FTIR and GPC characterization confirmed complete polymerization of n-butyl cyanoacrylate (nBCA) monomer into PBCA. DSC thermograms indicated that RT was dispersed as amorphous state in both PLGA and PBCA NPs. TEM studies indicated that the NPs were spherical. In vitro studies showed 30.86±2.07% and 43.59±3.80% release from PLGA and PBCA NPs in 72h, respectively. Pharmacodynamic study demonstrated faster regain of memory loss in amnesic mice with both PLGA and PBCA NPs when compared to RT solution. This indicates rapid and higher extent of transport of RT into the mice brain and thus shows the suitability of both NPs as potential carriers for providing sustained brain delivery of RT.
制备并优化了（使用析因设计）酒石酸瑞伐他汀（RT）的缓释纳米颗粒制剂，使用可生物降解的聚合物 PLGA 和 PBCA 作为载体进行了表征。通过 Morris 水迷宫测试评估了纳米颗粒（NPs）的药效学性能，用于治疗东莨菪碱诱导的健忘症小鼠的脑靶向和记忆改善。PLGA NPs 通过纳米沉淀技术制备，而 PBCA NPs 通过乳液聚合技术制备。通过析因设计研究了关键制剂变量对 NPs 粒径（PS）和药物包封率（PDE）的影响。PLGA NPs 的 PS 为 135.6±4.2nm，PDE 为 74.46±0.76%，而 PBCA NPS 的 PS 为 146.8±2.6nm，PDE 为 57.32±0.91%。FTIR 和 GPC 表征证实了正丁基氰基丙烯酸酯（nBCA）单体完全聚合为 PBCA。DSC 热图谱表明 RT 在 PLGA 和 PBCA NPs 中均呈无定形态分散。TEM 研究表明 NPs 为球形。体外研究表明，在 72 小时内，PLGA 和 PBCA NPs 分别释放了 30.86±2.07%和 43.59±3.80%的 RT。药效学研究表明，与 RT 溶液相比，PLGA 和 PBCA NPs 可使健忘症小鼠更快地恢复记忆丧失。这表明 RT 更快且更大程度地进入小鼠大脑，因此表明两种 NPs 均适合作为提供 RT 持续脑递送的潜在载体。
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