两性霉素 B 的眼部给药:当前挑战与未来展望。

Velmurugan Kailasam, Samhita Sai Veda Koduganti, Oindrilla Dasgupta, Prashant Garg, Jayabalan Nirmal
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摘要

简介两性霉素 B 是一种多烯类抗生素,被用作治疗真菌性角膜炎的非处方眼药水。两性霉素 B 溶解性、渗透性差,极易水解降解,因此配制给药系统具有挑战性。尽管存在这些缺点,但它仍是一种有效的抗真菌药物,可用于治疗念珠菌和其他真菌。然而,在眼部给药方面,对它的研究还不多。因此,本综述聚焦两性霉素 B 在眼部给药方面的潜力和日益重要的意义:在这篇综述中,我们系统地总结了两性霉素 B 在眼部疾病中的应用、两性霉素 B 的各种制剂挑战、标示外眼部用药以及稳定性问题。本文还讨论了两性霉素 B 在不同条件下的降解机制:在过去的几十年里,人们探索了多种纳米载体,以改善两性霉素 B 的制剂难题。此外,由于临床研究不足和毒性情况不明,美国食品和药物管理局(FDA)尚未批准用于眼部给药的两性霉素 B 制剂。本综述旨在提供有关两性霉素 B 用于眼部给药的全面信息。
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Ocular delivery of Amphotericin B: current challenges and future perspectives.

Introduction: Amphotericin B is a polyene antibiotic that is used as an off-label eye drop to treat fungal keratitis. Poor solubility, permeability and high susceptibility to hydrolytic degradation make it challenging to formulate a drug delivery system. Despite its drawbacks, it is a potent antifungal drug against Candida and other fungal species. However, it has not been explored much in ocular drug delivery. Hence, this review brings into focus the potential and increasing significance of Amphotericin B in ocular drug delivery.

Areas covered: In this review, we have systematically summarized the use of Amphotericin B in ocular diseases, the various formulation challenges for Amphotericin B, along with its off-label ocular usage, and stability concerns. The degradation mechanism of Amphotericin B in different conditions was discussed in this article as well.

Expert opinion: In the last few decades, several nanocarriers have been explored to improve the formulation challenges associated with Amphotericin B. Also, due to insufficient clinical studies and unknown toxicity profile, there is no US Food and Drug Administration (FDA) approved Amphotericin B formulation for ocular drug delivery. This review aims to offer thorough information about Amphotericin B in ocular drug delivery.

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