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蜂毒肽的口服结肠靶向给药:包衣海藻酸钙凝胶珠包载脂质体的研制

Oral colon-specific drug delivery for bee venom peptide: development of a coated calcium alginate gel beads-entrapped liposome.

作者信息

Xing Liu, Dawei Chen, Liping Xie, Rongqing Zhang

机构信息

Department of Pharmaceutical Science, School of Pharmacy, Shenyang Pharmaceutical University, Shenyang 100016, China.

出版信息

J Control Release. 2003 Dec 12;93(3):293-300. doi: 10.1016/j.jconrel.2003.08.019.

Abstract

Colon-specific drug delivery systems (CDDSs) can be used to improve the bioavailability of protein and peptide drugs through the oral route. A novel formulation for oral administration using coated calcium alginate gel beads-entrapped liposome and bee venom peptide as a model drug has been investigated for colon-specific drug delivery in vitro. Drug release studies under conditions mimicking stomach to colon transit have shown that the drug was protected from being released completely in the physiological environment of the stomach and small intestine. The release rate of bee venom from the coated calcium alginate gel beads-entrapped liposome was dependent on the concentration of calcium and sodium alginate, the amount of bee venom in the liposome, as well as the coating. Furthermore, a human gamma-scintigraphy technique was used in vivo to determine drug delivery more precisely. The colonic arrival time of the tablets was found to be 4-5 h. The results clearly demonstrated that the coated calcium alginate gel beads-entrapped liposome is a potential system for colon-specific drug delivery.

摘要

结肠特异性给药系统(CDDSs)可用于通过口服途径提高蛋白质和肽类药物的生物利用度。已对一种使用包衣海藻酸钙凝胶珠包裹脂质体并以蜂毒肽作为模型药物的新型口服制剂进行了体外结肠特异性给药研究。在模拟胃到结肠转运的条件下进行的药物释放研究表明,该药物在胃和小肠的生理环境中可避免完全释放。从包衣海藻酸钙凝胶珠包裹脂质体中释放蜂毒的速率取决于海藻酸钙和海藻酸钠的浓度、脂质体中蜂毒的含量以及包衣情况。此外,体内使用了人体γ闪烁扫描技术以更精确地确定药物递送情况。发现片剂到达结肠的时间为4 - 5小时。结果清楚地表明,包衣海藻酸钙凝胶珠包裹脂质体是一种潜在的结肠特异性给药系统。

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