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包载儿茶素脂质体的果胶酸钙凝胶珠的制备与表征

Preparation and characterization of calcium pectinate gel beads entrapping catechin-loaded liposomes.

作者信息

Lee Ji-Soo, Chung Donghwa, Lee Hyeon Gyu

机构信息

Department of Food and Nutrition, Hanyang University, 17 Haengdang-dong, Seongdong-gu, Seoul 133-791, Republic of Korea.

出版信息

Int J Biol Macromol. 2008 Mar 1;42(2):178-84. doi: 10.1016/j.ijbiomac.2007.10.008. Epub 2007 Oct 18.

Abstract

Calcium pectinate gel (CPG) beads entrapping catechin-loaded liposomes were prepared with or without hydroxypropylmethylcellulose (HPMC) (denoted as CPG-LH and CPG-L beads, respectively) and characterized in comparison with the CPG beads prepared without liposome and HPMC (denoted as CPG-C beads). For all types of beads, the catechin entrapment efficiency decreased by about 40-50% as the concentration of CaCl2 in gelling media increased from 2 to 6%. At a constant CaCl2 level, the entrapment efficiency was higher in the order of CPG-LH, CPG-L, and CPG-C beads. The in vitro release test showed that in simulated intestinal fluid the rate of catechin release was higher in the order of CPG-C, CPG-L, and CPG-LH beads, indicating that the catechin release was slowed by liposome and further retarded when HPMC was used simultaneously, whereas not in simulated gastric fluid. The addition of cholesterol in liposome could not retard but accelerated the catechin release. The results suggest that the CPG beads reinforced with liposome and HPMC could be employed for a sustained oral delivery of catechins, although further improvements are necessary.

摘要

制备了包载儿茶素脂质体的果胶酸钙凝胶(CPG)珠,分别添加或不添加羟丙基甲基纤维素(HPMC)(分别记为CPG-LH珠和CPG-L珠),并与未添加脂质体和HPMC制备的CPG珠(记为CPG-C珠)进行比较表征。对于所有类型的珠子,随着凝胶介质中CaCl2浓度从2%增加到6%,儿茶素包封率下降约40-50%。在CaCl2浓度恒定的情况下,包封率按CPG-LH珠、CPG-L珠和CPG-C珠的顺序依次升高。体外释放试验表明,在模拟肠液中,儿茶素释放速率按CPG-C珠、CPG-L珠和CPG-LH珠的顺序依次升高,这表明脂质体减缓了儿茶素的释放,同时使用HPMC时进一步延缓了释放,而在模拟胃液中则不然。脂质体中添加胆固醇不能延缓反而加速了儿茶素的释放。结果表明,尽管还需要进一步改进,但用脂质体和HPMC增强的CPG珠可用于儿茶素的口服缓释给药。

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