磷脂纳米囊泡的制备工艺及透黏膜能力  

Preparation and Permeation Studies of Soybean Lecithin-based Vesicles

作　　者：朱丹丹[1] 陈华兵[1] 郑静南[1] 杜丹荣[1] 牟东升[1] 杨祥良[1] 

机构地区：[1]华中科技大学生命科学与技术学院药物研究所,武汉430074

出　　处：《中国医学科学院学报》2006年第4期492-496,共5页Acta Academiae Medicinae Sinicae

摘　　要：目的对比研究磷脂纳米囊泡的制备工艺,并以胰岛素为模型药物,研究了胰岛素磷脂纳米囊泡透口腔黏膜的能力。方法分别采用超声波法、高剪切法、高压匀质法制备磷脂纳米囊泡,用激光散射法研究了不同工艺条件对磷脂纳米囊泡粒径和多分散指数的影响;采用离体透黏膜实验评价胰岛素磷脂纳米囊泡的透口腔黏膜能力。结果超声波法制备的3个处方磷脂纳米囊泡平均粒径分别为97·39、85·60、100·60nm,高压匀质法制备的3个处方磷脂纳米囊泡平均粒径分别为58·7、88·7、91·9nm,多分散指数均小于0·4,体系稳定。而采用高剪切法制备的磷脂纳米囊泡粒径与多分散指数较大,且体系不稳定。电镜照片显示高压匀质法制备的磷脂纳米囊泡呈球形,其粒径小于100nm。透黏膜实验显示,胰岛素磷脂纳米囊泡和对照组的透黏膜速率分别为0·0024和0·0008IU·ml-1·min-1,在180min磷脂纳米囊泡组胰岛素的累积透黏膜量达到(0·436±0·010)IU·ml-1,是对照组胰岛素透黏膜量的2·46倍。结论高压匀质法制备的磷脂纳米囊泡具有粒径小、粒径分布狭窄、稳定性好、透黏膜能力强等特点,有望成为一种新型的胰岛素透黏膜纳米载体。Objective To investigate various methods for constructing soybean lecithin （SL）-based vesicles and evaluate the permeation-enhancing effect of SL-based vesicles on the penetration of insulin through buccal mucosa. Methods The ultrasonic method, high speed shear method and high pressure homogenization method were respectively used to prepare the SL-based vesicles, and the particle size of the vesicles was measured with photon correlation spectrometry （PCS）. The penetration rate of insulin through porcine buccal muco- sa was investigated with the Valia-Chien diffusion cells. Results The average particle sizes of 3 formulations of SL-based vesicles were 97.39, 85.60, and 100.60 nm when prepared by ultrasonic method, and were 58.7, 88.7, and 91.9 nm when prepared by high pressure homogenization method. Both vesicles presented good stability. However, the SL-based vesicles prepared by high speed shear method had larger average diameters and were found to be unstable. Transmission electron microscopy showed that SL-based vesicles had a spherical shape and the result accorded with PCS. The permeation flux of insulin of formulation 1 and control solution were 0. 0024 and 0. 0008 IU·ml^-l·min^-l, respectively. The accumulative amount of formulation 1 at 180 min was （0. 436 ± 0. 010 ） IU ·ml^-l, which was 1.46 times higher than the control solution. Conclusions The SL-based vesicles obtained using high pressure homogenization method are characterized by small particle size, narrow distribution, good stability, and powerful permeation-enhancing effect, which enables them to be good carriers for the buccal delivery of insulin.

关 键 词：高压匀质法 磷脂 囊泡 胰岛素 透黏膜 

分 类 号：R944.1[医药卫生—药剂学]