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作为鼻腔给药载体的热可逆木葡聚糖凝胶。

Thermally reversible xyloglucan gels as vehicles for nasal drug delivery.

机构信息

Department of Pharmaceutics and Quality Assurance, R. C. Patel Institute of Pharmaceutical Education and Research, Karvand Naka Shirpur, Dist Dhule, Shirpur, India.

出版信息

Drug Deliv. 2012 Jun-Jul;19(5):270-6. doi: 10.3109/10717544.2012.704095.

Abstract

The aim of this study was to investigate the potential application of thermosensitive gels formed by a xyloglucan polysaccharide derived from tamarind seed for nasal drug delivery. Xyloglucan that had been partially degraded by β-galactosidase to eliminate 45% of galactose residues formed gels at concentrations of 2.5% w/w at gelation temperatures decreasing over the range 27-28°C. The in vitro release of ondansetron hydrochloride from the enzyme-degraded xyloglucan gels followed higuchi kinetics over a period of 5 h at 34°C by anomalous transport mechanism. The ex vivo permeation of ondansetron hydrochloride from the gels was sustained. Histological examination of nasal mucosa following a single administration of the gels showed no evidence of mucosal damage. Finally, the bioavailability study in rabbits revealed that the absolute bioavailability of ondansetron hydrochloride was significantly increased from 28.64% in the case of the oral drug solution to 52.79% in the case of the nasal in situ gel. The results of this study suggest the potential of the enzyme-degraded xyloglucan gels as vehicles for nasal delivery of drugs.

摘要

本研究旨在探讨从罗望子种子中提取的木葡聚糖多糖形成的温敏凝胶在鼻用药物传递中的潜在应用。用β-半乳糖苷酶部分降解木葡聚糖,以去除 45%的半乳糖残基,在浓度为 2.5%w/w 的情况下,凝胶化温度在 27-28°C 的范围内降低。在 34°C 下,盐酸昂丹司琼通过异常传输机制,在 5 小时内按照 Higuchi 动力学规律从酶解木葡聚糖凝胶中释放。盐酸昂丹司琼从凝胶中的体外渗透是持续的。单次给予凝胶后,对鼻黏膜进行组织学检查,未见黏膜损伤的证据。最后,在兔体内生物利用度研究中发现,与口服药物溶液相比,盐酸昂丹司琼的绝对生物利用度从 28.64%显著提高至鼻内原位凝胶的 52.79%。本研究结果表明,酶解木葡聚糖凝胶作为药物鼻用传递载体具有潜力。

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