College of Pharmacy, University of Kentucky, Lexington, KY, United States.
Adv Drug Deliv Rev. 2022 May;184:114252. doi: 10.1016/j.addr.2022.114252. Epub 2022 Mar 30.
Drug carriers to deliver macrolide antibiotics, such as azithromycin, show promise as antibacterial agents. Macrolide drug carriers have largely focused on improving the drug stability and pharmacokinetics, while reducing adverse reactions and improving antibacterial activity. Recently, macrolides have shown promise in treating inflammatory conditions by promoting a reparative effect and limiting detrimental pro-inflammatory responses, which shifts the immunologic setpoint from suppression to balance. While macrolide drug carriers have only recently been investigated for their ability to modulate immune responses, the previous strategies that deliver macrolides for antibacterial therapy provide a roadmap for repurposing the macrolide drug carriers for therapeutic interventions targeting inflammatory conditions. This review describes the antibacterial and immunomodulatory activity of macrolides, while assessing the past in vivo evaluation of drug carriers used to deliver macrolides with the intention of presenting a case for increased effort to translate macrolide drug carriers into the clinic.
载药系统递送大环内酯类抗生素(如阿奇霉素)有望成为抗菌药物。大环内酯类药物载体主要集中在提高药物稳定性和药代动力学,减少不良反应和提高抗菌活性。最近,大环内酯类药物通过促进修复作用和限制有害的促炎反应显示出在治疗炎症疾病方面的潜力,从而将免疫设定点从抑制转向平衡。虽然大环内酯类药物载体最近才被研究其调节免疫反应的能力,但以前用于抗菌治疗的递送大环内酯类药物的策略为重新利用大环内酯类药物载体提供了一个针对炎症疾病的治疗干预的路线图。本综述描述了大环内酯类的抗菌和免疫调节活性,同时评估了过去用于递送大环内酯类药物的载药系统的体内评估,旨在提出增加将大环内酯类药物载体转化为临床应用的努力。