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用于包封环丙沙星和依托泊苷的壳聚糖包被脂质体制剂

Chitosan-Coated Liposome Formulations for Encapsulation of Ciprofloxacin and Etoposide.

作者信息

Gil-Gonzalo Rubén, Durante-Salmerón D Alonzo, Pouri Saeedeh, Doncel-Pérez Ernesto, Alcántara Andrés R, Aranaz Inmaculada, Acosta Niuris

机构信息

Pluridisciplinar Institute, Complutense University of Madrid, Paseo Juan XXIII, 1, E-28040 Madrid, Spain.

Department of Chemistry in Pharmaceutical Science, Pharmacy Faculty, Complutense University of Madrid, Plaza de Ramón y Cajal s/n, E-28040 Madrid, Spain.

出版信息

Pharmaceutics. 2024 Aug 2;16(8):1036. doi: 10.3390/pharmaceutics16081036.

Abstract

Cancer and bacterial infections rank among the most significant global health threats. accounting for roughly 25 million fatalities each year. This statistic underscores the urgent necessity for developing novel drugs, enhancing current treatments, and implementing systems that boost their bioavailability to achieve superior therapeutic outcomes. Liposomes have been recognised as effective carriers; nonetheless, they encounter issues with long-term stability and structural integrity, which limit their pharmaceutical applicability. Chitosomes (chitosan-coated liposomes) are generally a good alternative to solve these issues. This research aims to demonstrate the effective individual encapsulation of ciprofloxacin (antibacterial, hydrophilic) and etoposide (anticancer, hydrophobic), within chitosomes to create more effective drug delivery systems (oral administration for ciprofloxacin, parenteral administration for etoposide). Thus, liposomes and chitosomes were prepared using the thin-film hydration technique and were characterised through ATR-FTIR, Dynamic Light Scattering (DLS), zeta potential, and release profiling. In both cases, the application of chitosomes enhanced long-term stability in size and surface charge. Chitosome-encapsulated ciprofloxacin formulations exhibited a slower and sustained release profile, while the combined effect of etoposide and chitosan showed heightened efficacy against the glioblastoma cell line U373. Therefore, coating liposomes with chitosan improved the encapsulation system's properties, resulting in a promising method for drug delivery.

摘要

癌症和细菌感染是全球最重大的健康威胁之一,每年造成约2500万人死亡。这一统计数据凸显了开发新型药物、改进现有治疗方法以及实施提高药物生物利用度以实现更好治疗效果的系统的迫切必要性。脂质体已被认为是有效的载体;然而,它们存在长期稳定性和结构完整性方面的问题,这限制了它们在制药领域的应用。壳聚糖脂质体(壳聚糖包被的脂质体)通常是解决这些问题的一个不错选择。本研究旨在证明将环丙沙星(抗菌、亲水性)和依托泊苷(抗癌、疏水性)有效单独包封在壳聚糖脂质体内,以创建更有效的药物递送系统(环丙沙星口服给药,依托泊苷肠胃外给药)。因此,采用薄膜水化技术制备了脂质体和壳聚糖脂质体,并通过衰减全反射傅里叶变换红外光谱(ATR-FTIR)、动态光散射(DLS)、zeta电位和释放曲线进行了表征。在这两种情况下,壳聚糖脂质体的应用提高了粒径和表面电荷的长期稳定性。壳聚糖脂质体包封的环丙沙星制剂表现出较慢且持续的释放曲线,而依托泊苷和壳聚糖的联合作用对胶质母细胞瘤细胞系U373显示出更高的疗效。因此,用壳聚糖包被脂质体改善了包封系统的性能,为药物递送提供了一种有前景的方法。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6ae9/11359655/4124fa25c037/pharmaceutics-16-01036-g001.jpg

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