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用于抗真菌治疗的两性霉素B口服制剂的设计

Design of amphotericin B oral formulation for antifungal therapy.

作者信息

Liu Min, Chen Meiwan, Yang Zhiwen

机构信息

b Urology Department , First Affiliated Hospital of Gannan Medical University, Gannan Medical University , Ganzhou , China , and.

c State Key Laboratory of Quality Research in Chinese Medicine , Institute of Chinese Medical Sciences, University of Macau , Macau , China.

出版信息

Drug Deliv. 2017 Nov;24(1):1-9. doi: 10.1080/10717544.2016.1225852.

Abstract

Amphotericin B (AmB) remains the "gold standard" for systemic antifungal therapy, even though new drugs are emerging as the attractive antifungal agents. Since AmB has negligible oral absorption as a consequence of its unfavorable physicochemical characterizations, its use is restricted to parenteral administration which is accompanied by severe side effects. As greater understanding of the gastrointestinal tract has developed, the advanced drug delivery systems are emerging with the potential to overcome the barriers of AmB oral delivery. Much research has demonstrated that oral AmB formulations such as lipid formulations may have beneficial therapeutic efficacy with reduced adverse effects and suitable for clinical application. Here we reviewed the different formulation strategies to enhance oral drug efficacy, and discussed the current trends and future perspectives for AmB oral administration in the treatment of antifungal infections.

摘要

两性霉素B(AmB)仍然是全身抗真菌治疗的“金标准”,尽管新药物正成为有吸引力的抗真菌剂。由于AmB因其不利的物理化学特性而口服吸收可忽略不计,其使用仅限于肠胃外给药,而肠胃外给药会伴随严重的副作用。随着对胃肠道的了解日益深入,先进的药物递送系统正在出现,有可能克服AmB口服给药的障碍。大量研究表明,口服AmB制剂如脂质制剂可能具有有益的治疗效果,副作用减少且适合临床应用。在此,我们综述了提高口服药物疗效的不同制剂策略,并讨论了AmB口服给药治疗真菌感染的当前趋势和未来前景。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fbfd/8241147/a1d414ef623f/IDRD_A_1225852_F0001_B.jpg

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