Chen Ru-da, Ren Fei, Li Guo-feng, Liu Si-jia
Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.
Nan Fang Yi Ke Da Xue Xue Bao. 2010 Apr;30(4):763-6.
To evaluate the effect of different preparation methods on the encapsulation efficiency (EE) and drug loading (DL) of paclitaxel-loaded polybutylcyanoacrylate nanoparticles (PTX-PBCA-NPs) and optimize the preparation of PTX-PBCA-NPs.
With DL and EE as the major indexes, the qualities of PTX-PBCA-NPs produced by the interfacial polymerization and emulsion polymerization method were compared. The optimized prescription was obtained by orthogonal design.
The ranges of EE of PTX-PBCA-NPs with the two methods were both 94.39%-99.23%. The highest DL with interfacial polymerization was (1.07-/+0.03)%, as compared to (0.86-/+0.01)% with emulsion polymerization. The optimized preparation conditions resulted in the mean size of PTX-PBCA-NPs of 235.6 nm, DL of 0.80%, and EE of 95.71%.
The EE of PTX-PBCA-NPs prepared by the above two methods is consistent with the requirement of the Pharmacopoeia of China, and PTX-PBCA-NPs containing higher DL can be obtained via interfacial polymerization.
评估不同制备方法对载紫杉醇聚氰基丙烯酸丁酯纳米粒（PTX-PBCA-NPs）包封率（EE）和载药量（DL）的影响，并优化PTX-PBCA-NPs的制备工艺。
以DL和EE为主要指标，比较界面聚合法和乳液聚合法制备PTX-PBCA-NPs的质量。通过正交设计获得优化处方。
两种方法制备的PTX-PBCA-NPs的EE范围均为94.39%-99.23%。界面聚合法的最高DL为（1.07±0.03）%，而乳液聚合法为（0.86±0.01）%。优化的制备条件使得PTX-PBCA-NPs的平均粒径为235.6nm，DL为0.80%，EE为95.71%。
上述两种方法制备的PTX-PBCA-NPs的EE符合《中国药典》要求，且通过界面聚合法可获得载药量较高的PTX-PBCA-NPs。
