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基于双层脂质体的双药物递送系统作为有效治疗消化性溃疡的载体。

Double-liposome-based dual-drug delivery system as vectors for effective management of peptic ulcer.

机构信息

Pharmaceutics Research Laboratory, Department of Pharmaceutical Sciences, Dr. H.S. Gour University, Sagar, India.

出版信息

J Liposome Res. 2012 Sep;22(3):205-14. doi: 10.3109/08982104.2012.655284.

DOI:10.3109/08982104.2012.655284
PMID:22889385
Abstract

The aim of the present investigation was to prepare and evaluate a vesicular dual-drug delivery system for effective management of the mucosal ulcer. Inner encapsulating and double liposomes were prepared by the glass-bead and reverse-phase evaporation methods, respectively. The formulation consisted of inner liposomes bearing ranitidine bismuth citrate (RBC) and outer liposomes encapsulating amoxicillin trihydrate (AMOX). The optimized inner liposomes and double liposomes were extensively characterized for vesicle size, morphology, zeta potential, vesicles count, entrapment efficiency, and in vitro drug release. In vitro, the double liposomes demonstrated a sustained release of AMOX and RBC of 93.6 ± 1.9 and 84.1 ± 0.9%, respectively, at the end of 144 hours. Ex vivo studies were conducted on Helicobacter pylori (ATCC26695) bacterial cell lines. Double liposomes showed a more enhanced percent H. pylori growth inhibition than the plain drug combination. Further, in vivo studies illustrated enhanced antisecretory and ulcer-protective activity of double liposomes, as compared to the plain drug combination. Microscopic studies also supported the ulcer-protective action of the formulation. Thus, it may be concluded that double liposomes are instrumental in reducing gastric secretions and targeting ulcer sites with the interception of minimal side effects, thus suggesting their potential in ulcer therapy.

摘要

本研究旨在制备并评价一种用于有效治疗黏膜溃疡的囊泡型双药递药系统。采用玻璃珠法和反相蒸发法分别制备内包封和双层脂质体。该制剂由载有雷尼替丁枸橼酸铋(RBC)的内脂质体和包载阿莫西林三水合物(AMOX)的外脂质体组成。对优化的内脂质体和双层脂质体进行了广泛的表征,包括囊泡大小、形态、Zeta 电位、囊泡计数、包封效率和体外药物释放。体外研究结果表明,双层脂质体在 144 小时后可分别持续释放 93.6±1.9%和 84.1±0.9%的 AMOX 和 RBC。在幽门螺杆菌(ATCC26695)细菌细胞系上进行了离体研究。双层脂质体显示出比普通药物组合更显著的抑制幽门螺杆菌生长的百分比。此外,体内研究表明,与普通药物组合相比,双层脂质体具有增强的抗分泌和溃疡保护活性。显微镜研究也支持该制剂的溃疡保护作用。因此,可以得出结论,双层脂质体通过减少胃酸分泌并靶向溃疡部位,同时最小化副作用,在溃疡治疗中具有潜在的应用价值。

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