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载异烟肼和利福平的 archaeosomes 的制备、表征和体外评价。

Preparation, characterization, and in vitro evaluation of isoniazid and rifampicin-loaded archaeosomes.

机构信息

Department of Bioengineering, Faculty of Chemical and Metallurgical Engineering, Yildiz Technical University, Istanbul, Turkey.

Department of Chemistry, Faculty of Arts and Sciences, Marmara University, Istanbul, Turkey.

出版信息

Chem Biol Drug Des. 2018 Jan;91(1):153-161. doi: 10.1111/cbdd.13066. Epub 2017 Aug 8.

DOI:10.1111/cbdd.13066
PMID:28667670
Abstract

The ability of Archaea to adapt their membrane lipid compositions to extreme environments has brought in archaeosomes into consideration for the development of drug delivery systems overcoming the physical, biological blockades that the body exhibits against drug therapies. In this study, we prepared unilamellar archaeosomes, from the polar lipid fraction extracted from Haloarcula 2TK2 strain, and explored its potential as a drug delivery vehicle. Rifampicin and isoniazid which are conventional drugs in tuberculosis medication were loaded separately and together in the same archaeosome formulation for the benefits of the combined therapy. Particle size and zeta potential of archaeosomes were measured by photon correlation spectroscopy, and the morphology was assessed by with an atomic force microscope. Encapsulation efficiency and loading capacities of the drugs were determined, and in vitro drug releases were monitored spectrophotometrically. Our study demonstrates that rifampicin and isoniazid could be successfully loaded separately and together in archaeosomes with reasonable drug-loading and desired vesicle-specific characters. Both of the drugs had greater affinity for archaeosomes than a conventional liposome formulation. The results imply that archaeosomes prepared from extremely halophilic archaeon were compatible with the liposomes for the development of stable and sustained release of antituberculosis drugs.

摘要

古菌能够适应其膜脂组成以适应极端环境,这使得 archaeosomes 成为克服机体对药物治疗产生的物理和生物障碍的药物传递系统的候选物。在这项研究中,我们从极端嗜盐古菌 Haloarcula 2TK2 菌株中提取的极性脂质部分制备了单层 archaeosomes,并探索了其作为药物传递载体的潜力。利福平(一种抗结核药物)和异烟肼(另一种抗结核药物)分别单独和一起载入到相同的 archaeosome 配方中,以实现联合治疗的益处。通过光子相关光谱法测量了 archaeosomes 的粒径和 zeta 电位,并通过原子力显微镜评估了其形态。测定了药物的包封效率和载药量,并通过分光光度法监测了体外药物释放。我们的研究表明,利福平(一种抗结核药物)和异烟肼(另一种抗结核药物)可以分别和一起成功载入 archaeosomes 中,具有合理的药物负载和所需的囊泡特异性特征。与传统的脂质体配方相比,两种药物对 archaeosomes 的亲和力都更强。结果表明,由极端嗜盐古菌制备的 archaeosomes 与脂质体兼容,可用于开发稳定和持续释放抗结核药物。

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