阿奇霉素脂质体水凝胶:在加强治疗 MRSA 相关皮肤感染方面向前迈进了一步。

IF 2.1 4区 医学 Q3 PHARMACOLOGY & PHARMACY Acta Pharmaceutica Pub Date : 2023-12-26 Print Date: 2023-12-01 DOI:10.2478/acph-2023-0042
Zora Rukavina, May Wenche Jøraholmen, Dunja Božić, Ivana Frankol, Petra Golja Gašparović, Nataša Škalko-Basnet, Maja Šegvić Klarić, Željka Vanić
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引用次数: 0

摘要

封装在各种脂质体(AZT-脂质体)中的阿奇霉素(AZT)对耐甲氧西林金黄色葡萄球菌(MRSA)具有明显的体外活性(1)。本研究是这项工作的后续,试图进一步探索 AZT 脂质体加入壳聚糖水凝胶(CHG)后的抗 MRSA 潜力。将 AZT 脂质体掺入 CHG(脂质体 CHG)的目的是确保制剂具有适当的粘度和质地特性、改变抗生素释放和增强抗菌活性,从而提高 AZT 脂质体在局部治疗 MRSA 相关皮肤感染中的治疗潜力。我们对四种不同的脂质体 CHG 进行了评估,并根据其对 MRSA 的抗菌活性、AZT 释放情况、细胞毒性以及质地和流变特性进行了比较。据我们所知,这项研究首次探讨了脂质体 CHGs 局部治疗 MRSA 相关皮肤感染的潜力。CHG 确保了适当的粘弹性和质地特性,从而延长了 AZT 在施用部位的保留时间和释放时间,增强了夹带 AZT 脂质体的抗 MRSA 效果。就抗 MRSA 活性和生物相容性而言,CATL-CHG(CHG 中的阳离子脂质体)制剂被认为是治疗 MRSA 相关皮肤感染最有前景的制剂。
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Azithromycin-loaded liposomal hydrogel: a step forward for enhanced treatment of MRSA-related skin infections.

Azithromycin (AZT) encapsulated into various types of liposomes (AZT-liposomes) displayed pronounced in vitro activity against methicillin-resistant Staphylococcus aureus (MRSA) (1). The present study represents a follow-up to this previous work, attempting to further explore the anti-MRSA potential of AZT-liposomes when incorporated into chitosan hydrogel (CHG). Incorporation of AZT-liposomes into CHG (liposomal CHGs) was intended to ensure proper viscosity and texture properties of the formulation, modification of antibiotic release, and enhanced antibacterial activity, aiming to upgrade the therapeutical potential of AZT-liposomes in localized treatment of MRSA-related skin infections. Four different liposomal CHGs were evaluated and compared on the grounds of antibacterial activity against MRSA, AZT release profiles, cytotoxicity, as well as texture, and rheological properties. To our knowledge, this study is the first to investigate the potential of liposomal CHGs for the topical localized treatment of MRSA-related skin infections. CHG ensured proper viscoelastic and texture properties to achieve prolonged retention and prolonged release of AZT at the application site, which resulted in a boosted anti-MRSA effect of the entrapped AZT-liposomes. With respect to anti-MRSA activity and biocompatibility, formulation CATL-CHG (cationic liposomes in CHG) is considered to be the most promising formulation for the treatment of MRSA-related skin infections.

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来源期刊
Acta Pharmaceutica
Acta Pharmaceutica PHARMACOLOGY & PHARMACY-
CiteScore
5.20
自引率
3.60%
发文量
20
审稿时长
>12 weeks
期刊介绍: AP is an international, multidisciplinary journal devoted to pharmaceutical and allied sciences and contains articles predominantly on core biomedical and health subjects. The aim of AP is to increase the impact of pharmaceutical research in academia, industry and laboratories. With strong emphasis on quality and originality, AP publishes reports from the discovery of a drug up to clinical practice. Topics covered are: analytics, biochemistry, biopharmaceutics, biotechnology, cell biology, cell cultures, clinical pharmacy, drug design, drug delivery, drug disposition, drug stability, gene technology, medicine (including diagnostics and therapy), medicinal chemistry, metabolism, molecular modeling, pharmacology (clinical and animal), peptide and protein chemistry, pharmacognosy, pharmacoepidemiology, pharmacoeconomics, pharmacodynamics and pharmacokinetics, protein design, radiopharmaceuticals, and toxicology.
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