College of Pharmacy, Jinan University, Guangzhou 510632, China.
Guangzhou Hospital of Integrated Traditional Chinese and Western Medicine, Guangzhou 510800, China.
Int J Pharm. 2019 Apr 20;561:274-282. doi: 10.1016/j.ijpharm.2019.03.006. Epub 2019 Mar 6.
A polymer-lipid hybrid nanocarrier was developed to encapsulate psoralen (PSO) to improve its water solubility and bioavailability. The effects of PSO-loaded polymer-lipid hybrid nanoparticles (PSO-PLNs) on breast cancer MCF-7 cells were investigated. PSO-PLNs were prepared through a nanoprecipitation method and were optimized by a central composite design-response surface methodology using particle size and entrapment efficiency as indices. Dynamic light scattering and transmission electron microscopy analysis confirmed the physicochemical characterizations of PSO-PLNs, which had an average size of 93.44 ± 2.39 nm and a zeta potential of -27.63 ± 0.31 mV. In vitro drug release of PSO-PLNs was evaluated using dialysis and showed a delayed release compared with free PSO. The in vivo anticancer efficiency of PSO-PLNs was appreciated using a MCF-7 breast tumor model. Administration of PSO-PLNs showed similar antitumor efficacy but lower toxicity compared with doxorubicin. Our designed nanocarriers successfully optimized the pharmacokinetics of PSO via improved systemic delivery.
一种聚合物-脂质杂化纳米载体被开发出来，用于包裹补骨脂素（PSO），以提高其水溶性和生物利用度。研究了载补骨脂素的聚合物-脂质杂化纳米粒（PSO-PLNs）对乳腺癌 MCF-7 细胞的影响。PSO-PLNs 通过纳米沉淀法制备，并通过中心组合设计-响应面法优化，以粒径和包封效率为指标。动态光散射和透射电子显微镜分析证实了 PSO-PLNs 的理化特性，其平均粒径为 93.44±2.39nm，zeta 电位为-27.63±0.31mV。采用透析法评价了 PSO-PLNs 的体外药物释放，结果表明其释放速度较游离 PSO 延迟。PSO-PLNs 的体内抗癌效率在 MCF-7 乳腺癌模型中得到了评估。与多柔比星相比，PSO-PLNs 的给药表现出相似的抗肿瘤疗效，但毒性较低。我们设计的纳米载体通过改善系统递送来成功优化了 PSO 的药代动力学。
