肺靶向顺铂泡囊的研制与体外性质的评价

Preparation of lung-targeting cis-diamminedichloroplatinum niosomes and evaluation of their characteristics in vitro

目的研制肺靶向顺铂泡囊并对其进行体外评价。方法以包封率为指标,均匀设计法优化泡囊处方。考察泡囊的包封率、载药量、电位、表面形态、粒径、稳定性和体外释放等体外特性。结果泡囊呈圆球形、壁厚。PEG-泡囊表面粗糙,可看到表面栅状亲水性结构;而泡囊表面光滑。混悬状液态泡囊包封率均大于80%,15 d内稳定,冻干后4月内稳定性良好,粒径7~10μm,体外t1/2为5~8 h。结论所制泡囊的体外性质适合肺靶向研究,所用工艺简单,操作方便。

OBJECTIVE To prepare lung-targeting Cis-diam minedichloyoplatinum(CDDP) niosomes and evaluate their characteristics in vitro.METHODSThe entrapment efficiency was used as the index,and uniform design was adopted to optimize the formulations.The efficiency of entrapment,drug loading,Zeta potential,surface morphology,particle size,stability and release behavior of the niosomes were evaluated.RESULTSMicroscopic examination showed that the niosomes were spherical with a thick wall,and a grating hydrophilic struc...