Abruzzo Angela, Parolin Carola, Rossi Martina, Vitali Beatrice, Cappadone Concettina, Bigucci Federica
Department of Pharmacy and Biotechnology, University of Bologna, Via San Donato 19/2, 40127 Bologna, Italy.
Antibiotics (Basel). 2022 Aug 2;11(8):1040. doi: 10.3390/antibiotics11081040.
In recent years, the treatment of bacterial skin infections has been considered a major healthcare issue due to the growing emergence of antibiotic-resistant strains of . The incorporation of antibiotics in appropriate nanosystems could represent a promising strategy, able to overcome several drawbacks of the topical treatment of infections, including poor drug retention within the skin. The present work aims to develop microemulsions containing azithromycin (AZT), a broad-spectrum macrolide antibiotic. Firstly, AZT solubility in various oils, surfactants and co-surfactants was assessed to select the main components. Subsequently, microemulsions composed of vitamin E acetate, Labrasol and Transcutol P were prepared and characterized for their pH, viscosity, droplet size, zeta potential and ability to release the drug and to promote its retention inside porcine skin. Antimicrobial activity against methicillin-resistant strains (MRSA) and the biocompatibility of microemulsions were evaluated. Microemulsions showed an acceptable pH and were characterized by different droplet sizes and viscosities depending on their composition. Interestingly, they provided a prolonged release of AZT and promoted its accumulation inside the skin. Finally, microemulsions retained AZT efficacy on MRSA and were not cytotoxic. Hence, the developed AZT-loaded microemulsions could be considered as useful nanocarriers for the treatment of antibiotic-resistant infections of the skin.
近年来,由于抗生素耐药菌株的不断出现,细菌性皮肤感染的治疗已被视为一个重大的医疗保健问题。将抗生素纳入合适的纳米系统可能是一种有前景的策略,能够克服局部感染治疗的几个缺点,包括药物在皮肤内保留不佳。本研究旨在开发含有阿奇霉素(AZT)的微乳液,阿奇霉素是一种广谱大环内酯类抗生素。首先,评估了阿奇霉素在各种油、表面活性剂和助表面活性剂中的溶解度,以选择主要成分。随后,制备了由维生素E醋酸酯、Labrasol和Transcutol P组成的微乳液,并对其pH值、粘度、液滴大小、zeta电位以及释放药物和促进其在猪皮肤内保留的能力进行了表征。评估了微乳液对耐甲氧西林菌株(MRSA)的抗菌活性和生物相容性。微乳液显示出可接受的pH值,并且根据其组成具有不同的液滴大小和粘度。有趣的是,它们提供了阿奇霉素的缓释,并促进了其在皮肤内的积累。最后,微乳液保留了对MRSA的疗效且无细胞毒性。因此,所开发的载阿奇霉素微乳液可被视为治疗皮肤抗生素耐药感染的有用纳米载体。