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包裹在壳聚糖包被脂质体中的头孢他啶和松萝酸用于口服抗结直肠癌诱导

Ceftazidime and Usnic Acid Encapsulated in Chitosan-Coated Liposomes for Oral Administration against Colorectal Cancer-Inducing .

作者信息

de Souza Jaqueline Barbosa, de Lacerda Coriolano Davi, Dos Santos Silva Rayza Camila, da Costa Júnior Sérgio Dias, de Almeida Campos Luís André, Cavalcanti Iago Dillion Lima, Lira Nogueira Mariane Cajubá de Britto, Pereira Valéria Rêgo Alves, Brelaz-de-Castro Maria Carolina Accioly, Cavalcanti Isabella Macário Ferro

机构信息

Institute Keizo Asami (iLIKA), Federal University of Pernambuco (UFPE), Recife 50670-901, PE, Brazil.

Laboratory of Nanotechnology, Biotechnology and Cell Culture (NanoBioCel), Academic Center of Vitória (CAV), Federal University of Pernambuco (UFPE), Vitória de Santo Antão 55608-680, PE, Brazil.

出版信息

Pharmaceuticals (Basel). 2024 Jun 19;17(6):802. doi: 10.3390/ph17060802.

Abstract

has been associated with the induction of colorectal cancer (CRC). Thus, combined therapy incorporating usnic acid (UA) and antibiotics such as ceftazidime (CAZ), co-encapsulated in liposomes, could be an alternative. Coating the liposomes with chitosan (Chi) could facilitate the oral administration of this nanocarrier. Liposomes were prepared using the lipid film hydration method, followed by sonication and chitosan coating via the drip technique. Characterization included particle size, polydispersity index, zeta potential, pH, encapsulation efficiency, and physicochemical analyses. The minimum inhibitory concentration and minimum bactericidal concentration were determined against ATCC 25922, NCTC 13846, and H10407 using the microdilution method. Antibiofilm assays were conducted using the crystal violet method. The liposomes exhibited sizes ranging from 116.5 ± 5.3 to 240.3 ± 3.5 nm and zeta potentials between +16.4 ± 0.6 and +28 ± 0.8 mV. The encapsulation efficiencies were 51.5 ± 0.2% for CAZ and 99.94 ± 0.1% for UA. Lipo-CAZ-Chi and Lipo-UA-Chi exhibited antibacterial activity, inhibited biofilm formation, and preformed biofilms of . The Lipo-CAZ-UA-Chi and Lipo-CAZ-Chi + Lipo-UA-Chi formulations showed enhanced activities, potentially due to co-encapsulation or combination effects. These findings suggest potential for in vivo oral administration in future antibacterial and antibiofilm therapies against CRC-inducing bacteria.

摘要

已与结直肠癌(CRC)的诱导相关联。因此,将松萝酸(UA)和抗生素如头孢他啶(CAZ)共包封在脂质体中的联合疗法可能是一种替代方案。用壳聚糖(Chi)包被脂质体可促进这种纳米载体的口服给药。脂质体采用脂质膜水化法制备,随后进行超声处理,并通过滴注技术进行壳聚糖包被。表征包括粒径、多分散指数、zeta电位、pH值、包封效率和物理化学分析。使用微量稀释法测定对ATCC 25922、NCTC 13846和H10407的最低抑菌浓度和最低杀菌浓度。使用结晶紫法进行抗生物膜测定。脂质体的粒径范围为116.5±5.3至240.3±3.5nm,zeta电位在+16.4±0.6和+28±0.8mV之间。CAZ的包封效率为51.5±0.2%,UA的包封效率为99.94±0.1%。Lipo-CAZ-Chi和Lipo-UA-Chi表现出抗菌活性,抑制生物膜形成,并对……的预形成生物膜有作用。Lipo-CAZ-UA-Chi和Lipo-CAZ-Chi + Lipo-UA-Chi制剂显示出增强的活性,可能是由于共包封或联合效应。这些发现表明在未来针对诱导CRC的细菌的抗菌和抗生物膜治疗中进行体内口服给药具有潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/9cfd/11206294/6037e817270b/pharmaceuticals-17-00802-g001.jpg

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