番茄红素脂质体生物利用率的比较研究

番茄红素的理化性质极大地限制了其生理活性功能的发挥，脂质体作为一种常见药物载体，考虑将其作为番茄红素的产品剂型，提高番茄红素的生物利用率。选取薄膜- 超声法制备番茄红素脂质体，经体外实验及体内实验研究可知：油溶番茄红素在人工胃液和无胆酸盐的人工肠液中无释放，但在添加胆酸盐的人工肠液中释放率达91%；番茄红素脂质体和番茄红素微胶囊在人工胃液中释放率低于22%，在添加胆酸盐和无胆酸盐的人工肠液中24h 释放率均达80%～90%。以油溶番茄红素为参照剂型，自制番茄红素脂质体与市售番茄红素微胶囊均具有较长的体内滞后时间和较低的清除率，延长了有效作用时间；自制番茄红素脂质体相对生物利用率为154.42%，大大优于油溶番茄红素，接近市售番茄红素微胶囊(205.03%)。

Comparative Study on Bioavailability of Lycopene Liposomes,Lycopene Microcapsules and Soybean Oil-based Preparation of Lycopene

The physical and chemical properties of lycopene have been shown to hamper its biological functions. In this study, the liposome technique, providing one kind of commonly used carriers for drugs, was considered for the production of lycopene liposome with high stability and bioavailability. An ultrasonic-assisted film-forming method was used to prepare lycopene liposomes. Results indicated that low release rate of soybean oil-based preparation of lycopene in mimic gastric or intestinal fluid without bile salt was observed; however, the release of soybean oil-based preparation of lycopene in mimic intestinal fluid with bile salt reached up to 91%. The release of lycopene from liposome and microcapsule preparations was less than 22% in mimic gastric fluid, while its release in two kinds of mimic intestinal fluid was between 80% and 90%. Compared with soybean oil-based preparation of lycopene, lycopene liposomes prepared in our laboratory and commercially-available lycopene microcapsules exhibited longer retention time in body and lower clearance, which provided a prolonged efficiency for lycopene. Moreover, the bioavailability of lycopene liposomes was 154.42%, which was close to lycopene microcapsules and much higher than soybean oil-based preparation of lycopene.