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载紫杉醇的甘油棕榈酸酯纳米粒:体外释放和细胞毒性活性。

Paclitaxel-loaded glyceryl palmitostearate nanoparticles: in vitro release and cytotoxic activity.

机构信息

Centre for Post Graduate Studies and Research, New Drug Delivery Systems laboratory, Pharmacy Department, M S University of Baroda, Vadodara, Gujarat, India. vikram.

出版信息

J Drug Target. 2009 May;17(4):304-10. doi: 10.1080/10611860902737938.

Abstract

Solid lipid nanoparticles (SLNs) of paclitaxel using glyceryl palmitostearate (GPS) as matrix were prepared by modified hot homogenization method. The SLNs were characterized for mean particle size, percent entrapment efficiency, and zeta potential, which were found to be 207 nm, 96.26%, and -28.26 mV, respectively. Transmission electron microscopic studies revealed that the prepared SLNs were of spherical shape. Drug retarding efficiency of the lipid (GPS) was better in pH 7.4 compared with pH 3.5. The release profile showed tendency to follow Higuchi diffusion pattern in both the media. Chemosensitivity assay carried out using B16F10 cell lines showed that antiproliferative activity of paclitaxel was not hindered because of encapsulation.

摘要

采用改良的热熔匀化法制备以甘油棕榈酸硬脂酸酯(GPS)为基质的紫杉醇固体脂质纳米粒(SLNs)。对 SLNs 的平均粒径、包封率和 Zeta 电位进行了表征,分别为 207nm、96.26%和-28.26mV。透射电子显微镜研究表明,所制备的 SLNs 呈球形。脂质(GPS)在 pH7.4 时的药物延缓效率优于 pH3.5。在两种介质中,释放曲线均呈现出符合 Higuchi 扩散模式的趋势。使用 B16F10 细胞系进行的化疗敏感性试验表明,紫杉醇的抗增殖活性并未因包封而受到阻碍。

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