Xi Na, Hou Lian-Bing
Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.
Zhong Yao Cai. 2010 Apr;33(4):610-3.
To prepare long-circulating hydroxycamptothecin nanoparticles and study its in vitro drug release characteristics.
The HCPT-PEG-PCL-NPs were prepared by solvent-diffusion method using PEG-PCL block copolymer synthesized as a matrix and HCPT as an antitumor agent. Then the obtained NPs were evaluated and its in vitro drug release characteristics were investigated.
When using PEG4000-PCL2000, PEG4000-PCL1250, PEG2000-PCL2000, PEG2000-PCL1250 as the carrier material to prepare NPs, the average particle size of NPs in turn were 116.1, 110.0, 119.9, 99.1 nm; the zeta potential were -22.4, - 16. 9, -33.5, - 28.8 mV; the entrapment efficiency were 88.29%, 83.10%, 80.67%, 77.46%; and the drug loading were 2.96%, 2.56%, 2.31%, 2.14%, respectively. HCPT-PEG-PCL-NPs all showed a certain degree of sustained-release characteristics and their release mechanisms were fitted to Weibull modle, which showed that the drug release process included passive diffusion and matrix-eroded procedure.
The HCPT-PEG-PCL-NPs has high entrapment efficiency, drug loading, uniform particle size, and can retard drug release in vitro, so it provides an extensive prospect for clinical application of HCPT.
制备长循环羟基喜树碱纳米粒并研究其体外释药特性。
以合成的聚乙二醇-聚己内酯嵌段共聚物为基质、羟基喜树碱为抗肿瘤药物，采用溶剂扩散法制备羟基喜树碱-聚乙二醇-聚己内酯纳米粒（HCPT-PEG-PCL-NPs）。然后对所得纳米粒进行评价并研究其体外释药特性。
以聚乙二醇4000-聚己内酯2000、聚乙二醇4000-聚己内酯1250、聚乙二醇2000-聚己内酯2000、聚乙二醇2000-聚己内酯1250为载体材料制备纳米粒时，纳米粒的平均粒径依次为116.1、110.0、119.9、99.1nm；ζ电位依次为-22.4、-16.9、-33.5、-28.8mV；包封率依次为88.29%、83.10%、80.67%、77.46%；载药量依次为2.96%、2.56%、2.31%、2.14%。HCPT-PEG-PCL-NPs均表现出一定程度的缓释特性，其释药机制符合威布尔模型，表明药物释放过程包括被动扩散和基质溶蚀过程。
HCPT-PEG-PCL-NPs具有较高的包封率、载药量，粒径均匀，且能在体外延缓药物释放，为羟基喜树碱的临床应用提供了广阔前景。
