氟尿嘧啶隐形泡囊的制备及其体外性质的研究

目的制备氟尿嘧啶隐形泡囊并考察其理化性质和体外细胞毒性。方法用自制Plu-Chol,以改良注入法制备氟尿嘧啶隐形泡囊,考察泡囊的形态、粒径、电位、包封率和体外释放特性,通过MTT比色法比较泡囊与原药对Hela细胞的作用效应。结果氟尿嘧啶隐形泡囊在电镜下的外观为球形,平均粒径为904.87±0.45 nm,Zeta电位为-66.75 mV,包封率为30.93%±1.71%;体外释放符合Weibull distribution模型,且具有明显的缓释性(氟尿嘧啶隐形泡囊释药t1/2为游离氟尿嘧啶的3.75倍);细胞毒性试验表明泡囊对Hela细胞的杀伤作用明显优于原药(IC50降低了83.95%,P<0.01)。结论所制氟尿嘧啶隐形泡囊的操作简单,对肿瘤细胞的杀伤力显著强于原药。

Study on the preparation and properties of Fluorouracil stealth niosomes in vitro

OBJECTIVE To prepare Fluorouracil stealth niosomes and evaluate their physicochemical properties and cytotoxicity in vitro.METHODS Fluorouracil-loaded stealth niosomes were prepared by modified injection-extrude method with Plu-Chol made in our lab as the excipient.The appearance,particle size,Zeta potential,efficiency of entrapment and release behavior were evaluated.Cytotoxicity on Hela cells in vitro was evaluated by MTT method.RESULTS The particle diameter of the spherically-looking Fluorouracil stealth niosomes was 904.87±0.45 nm with the Zeta potential of-66.75 mV and the entrapment rate of 30.93%±1.71%.The release profile in vitro could be characterized by the Weibull distribution equation,and showed an obvious sustained release feature（the release t₁/2 of fluorouracil stealth niosomes was 3.75 times as large as that of the free drug）.The results showed that cytotoxicity of niosomes on Hela cells was significantly stronger than that of the free drug（IC₅0 was decreased 83.95%,P<0.01）.CONCLUSION Fluorouracil stealth niosomes were easy to prepare and showed a significantly higher antitumor efficiency than the free drug.