盐酸利多卡因多囊脂质体的制备和质量评价

目的:制备具有缓释特性的盐酸利多卡因多囊脂质体,考察其理化性质。方法:以卵磷脂和胆固醇为膜材,采用复乳法制备盐酸利多卡因多囊脂质体,用透射电镜观察其外观形态,用激光粒度分析仪测定粒径,检测包封率和体外释药特性。结果:盐酸利多卡因多囊脂质体的外观形态圆整、规则,粒径分布在300～700nm及1～6μm两区域,包封率为(27.10±0.66)%。多囊脂质体在pH 7.4的磷酸盐缓冲液中,24h的累积释药百分率为(92.7±3.6)%。结论:盐酸利多卡因多囊脂质体具有一定的缓释特性。

Preparation and quality evaluation of lidocaine hydrochloride multivesicular liposomes

Objective: To prepare lidocaine hydrochloride multivesicular liposomes which have sustained-releasing characteristics and investigate their physicochemical properties.Methods: Lidocaine hydrochloride multivesicular liposomes were prepared by multiple emulsion method with lecithin and cholesterol as film materials.Morphological characteristics of the liposomes were detected by transmission electron microscope and particle diameters were tested by laser partical size analyzer.Entrapment efficiency and in vitro drug releasing characteristics of the multivesicular liposomes were studied.Results: The lidocaine hydrochloride multivesicular liposomes had a spherical shape and a smooth surface,with two diameter ranges of 300-700 nm and 1-6 μm.The entrapment efficiency was(27.10±0.66)%,and the cumulative drug releasing percentage in 24 h was up to(92.7±3.6)% in phosphate buffer solution(pH 7.4).Conclusion: The lidocaine hydrochloride multivesicular liposomes have sustained-releasing properties.