Zhang Fang, Chang Minglu, Yu Yanna, Zhang Yongchun, Liu Guangpu, Wei Ting, Zuo Tiantian, Guan Yuanyuan, Lin Guimei, Zhao Zhongxi
School of Pharmaceutical Sciences, Shandong University, Jinan, China.
J Pharm Pharmacol. 2015 Nov;67(11):1546-55. doi: 10.1111/jphp.12472. Epub 2015 Aug 10.
Lipid emulsified nanoparticles (LPNPs) have been developed to load anticancer drug docetaxel (DTX) in this work.
We evaluated DTX-loaded lipid emulsified nanoparticles (DTX-LPNPs) in vitro compared with the conventional nanoparticles (DTX-NPs). The newly developed formulation was compared with DTX-NPs in terms of physicochemical properties and in-vitro efficacy.
These two formulations had similar physicochemical properties in our results. And it has been proven that phosphatidylethanolamine had higher emulsification efficiency (20-fold of polyvinyl alcohol) in the same preparation procedure. The in-vitro release of DTX from DTX-LPNPs showed burst release initially and then followed by a sustained release, which prolonged the half time. The cytotoxicity test indicated that the DTX-LPNPs were more effective against tumour growth, and the IC50 of Duopafei, DTX-NPs and DTX-LPNPs for the inhibition of human lung cancer A549 cells at 48 h (n = 3) were found to be 3.53 ± 0.43, 1.15 ± 0.06 and 0.55 ± 0.08 μm, respectively. The evaluation of the cellular uptake showed that DTX-LPNPs improved the drug delivery into cytoplasm compared with the commercial product Duopafei and DTX-NPs.
DTX-LPNPs may be a promising formulation for cancer therapy.
在本研究中已研发出脂质乳化纳米颗粒（LPNPs）来负载抗癌药物多西他赛（DTX）。
我们将负载DTX的脂质乳化纳米颗粒（DTX-LPNPs）与传统纳米颗粒（DTX-NPs）进行了体外评估。将新研发的制剂在物理化学性质和体外疗效方面与DTX-NPs进行了比较。
在我们的研究结果中，这两种制剂具有相似的物理化学性质。并且已证实在相同的制备过程中，磷脂酰乙醇胺具有更高的乳化效率（是聚乙烯醇的20倍）。DTX从DTX-LPNPs的体外释放最初呈现突释，随后是缓释，这延长了半衰期。细胞毒性试验表明DTX-LPNPs对肿瘤生长更有效，在48小时（n = 3）时，多帕菲、DTX-NPs和DTX-LPNPs对人肺癌A549细胞抑制的IC50分别为3.53±0.43、1.15±0.06和0.55±0.08μm。细胞摄取评估表明，与市售产品多帕菲和DTX-NPs相比，DTX-LPNPs提高了药物向细胞质的递送。
DTX-LPNPs可能是一种有前景的癌症治疗制剂。
