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目的:制备羟基喜树碱的长循环纳米粒并进行体外释药性质考察。方法:合成了聚乙二醇-聚己内酯嵌段共聚物,并以此为载体材料,采用溶剂扩散法制备羟基喜树碱长循环纳米粒,对其进行表征及体外释药研究。结果:以共聚物PEG4000-PCL2000、PEG4000-PCL1250、PEG2000-PCL2000、PEG2000-PCL1250为载体制备的4种HCPT-PEG-PCL-NPs的平均粒径依次为116.1、110.0、119.9、99.1nm,平均ξ电位依次为-22.4、-16.9、-33.5、-28.8 mV,平均包封率依次为88.29%、83.10%、80.67%、77.46%,平均载药量依次为2.96%、2.56%、2.31%、2.14%;所制备的HCPT-PEG-PCL-NPs均具有一定的缓释作用,体外释药均符合Weibull分布模型,其释药机理应是药物的被动扩散与载体基质的溶蚀协同作用。结论:所制备的HCPT-PEG-PCL-NPs包封率和载药量较高,粒径分布均匀,体外释药具有缓释特点,为羟基喜树碱的临床应用提供了更广阔的前景。
OBJECTIVE: To prepare hydroxycamptothecin long circulating nanoparticles and investigate the in vitro release properties. Methods: Polyethylene glycol-polycaprolactone block copolymer was synthesized and used as the carrier material. The hydroxycamptothecin long-circulating nanoparticles were prepared by solvent diffusion method, and characterized and characterized in vitro. Results: The average diameters of the four HCPT-PEG-PCL-NPs prepared with the copolymers PEG4000-PCL2000, PEG4000-PCL1250, PEG2000-PCL2000 and PEG2000-PCL1250 were 116.1, 110.0, 119.9 and 99.1 nm, The average entrapment efficiencies were -22.4, -16.9, -33.5 and -28.8 mV, with the average entrapment efficiencies of 88.29%, 83.10%, 80.67% and 77.46%, respectively. The average drug loading rates were 2.96%, 2.56%, 2.31% and 2.14 %. The prepared HCPT-PEG-PCL-NPs all had sustained-release effect. The drug release in vitro was in accordance with the Weibull distribution model. The mechanism of drug release should be the synergistic effect of passive diffusion of drugs and dissolution of carrier matrix. CONCLUSION: The prepared HCPT-PEG-PCL-NPs have high encapsulation efficiency and drug loading, uniform particle size distribution and sustained release characteristics in vitro, which provide a broader prospect for the clinical application of HCPT-PEG-PCL-NPs.