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红霉素制剂——迈向先进药物递送的历程

Erythromycin Formulations-A Journey to Advanced Drug Delivery.

作者信息

Platon Vera-Maria, Dragoi Brindusa, Marin Luminita

机构信息

"Petru Poni" Institute of Macromolecular Chemistry of Romanian Academy, 700487 Iasi, Romania.

TRANSCEND Research Center, Regional Institute of Oncology, 700483 Iasi, Romania.

出版信息

Pharmaceutics. 2022 Oct 13;14(10):2180. doi: 10.3390/pharmaceutics14102180.

Abstract

Erythromycin (ERY) is a macrolide compound with a broad antimicrobial spectrum which is currently being used to treat a large number of bacterial infections affecting the skin, respiratory tract, intestines, bones and other systems, proving great value from a clinical point of view. It became popular immediately after its discovery in 1952, due to its therapeutic effect against pathogens resistant to other drugs. Despite this major advantage, ERY exhibits several drawbacks, raising serious clinical challenges. Among them, the very low solubility in water and instability under acidic conditions cause a limited efficacy and bioavailability. Apart from this, higher doses promote drug resistance and undesirable effects. In order to overcome these disadvantages, during the past decades, a large variety of ERY formulations, including nanoparticles, have emerged. Despite the interest in ERY-(nano)formulations, a review on them is lacking. Therefore, this work was aimed at reviewing all efforts made to encapsulate ERY in formulations of various chemical compositions, sizes and morphologies. In addition, their preparation/synthesis, physico-chemical properties and performances were carefully analysed. Limitations of these studies, particularly the quantification of ERY, are discussed as well.

摘要

红霉素(ERY)是一种具有广泛抗菌谱的大环内酯类化合物,目前正用于治疗大量影响皮肤、呼吸道、肠道、骨骼和其他系统的细菌感染,从临床角度来看具有重要价值。它在1952年被发现后立即受到欢迎,因为它对耐其他药物的病原体具有治疗作用。尽管有这一主要优势,但ERY也存在一些缺点,带来了严重的临床挑战。其中,在水中的极低溶解度和在酸性条件下的不稳定性导致疗效和生物利用度有限。除此之外,高剂量会促进耐药性和产生不良影响。为了克服这些缺点,在过去几十年中,出现了各种各样的ERY制剂,包括纳米颗粒。尽管人们对ERY-(纳米)制剂感兴趣,但缺乏对它们的综述。因此,这项工作旨在综述将ERY封装在各种化学成分、尺寸和形态的制剂中的所有努力。此外,还仔细分析了它们的制备/合成、物理化学性质和性能。这些研究的局限性,特别是ERY的定量问题,也进行了讨论。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f20d/9608461/9739dc006b10/pharmaceutics-14-02180-sch002.jpg

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