Le-Deygen Irina M, Mamaeva Polina V, Skuredina Anna A, Safronova Anastasia S, Belogurova Natalia G, Kudryashova Elena V
Chemical Enzymology Department, Lomonosov Moscow State University, 119991 Moscow, Russia.
J Funct Biomater. 2023 Jul 20;14(7):381. doi: 10.3390/jfb14070381.
The therapy of resistant forms of tuberculosis requires the simultaneous use of several drugs, in particular, a combination of rifampicin and levofloxacin. In this paper, we aimed to design a combined system for the simultaneous delivery of these drugs for potential inhalation administration. A feature of this system is the incorporation of rifampicin into optimized liposomal vesicles capable of forming a multipoint non-covalent complex with chitosan-β-cyclodextrin conjugates. Levofloxacin is incorporated into cyclodextrin tori by forming a host-guest complex. Here, a comprehensive study of the physicochemical properties of the obtained systems was carried out and special attention was paid to the kinetics of cargo release for individual drugs and in the combined system. The release of levofloxacin in combined system is slow and is described by the Higuchi model in all cases. The release of rifampicin from liposomes during the formation of complexes with polymeric conjugates is characterized by the change of the Higuchi model to the Korsmeyer-Peppas model with the main type of diffusion against Fick's law. Microbiological studies in solid and liquid growth media a consistently high antibacterial activity of the obtained systems was shown against and .
耐药型结核病的治疗需要同时使用多种药物，特别是利福平与左氧氟沙星的联合使用。在本文中，我们旨在设计一种联合给药系统，用于同时递送这些药物以便进行潜在的吸入给药。该系统的一个特点是将利福平包封于优化的脂质体囊泡中，这些脂质体能够与壳聚糖-β-环糊精缀合物形成多点非共价复合物。左氧氟沙星通过形成主客体复合物被包封于环糊精环中。在此，我们对所得系统的理化性质进行了全面研究，并特别关注了单一药物及联合系统中药物释放的动力学。联合系统中左氧氟沙星的释放缓慢，在所有情况下均符合 Higuchi 模型。在与聚合物缀合物形成复合物的过程中，利福平从脂质体中的释放表现为从 Higuchi 模型转变为 Korsmeyer-Peppas 模型，主要扩散类型违反菲克定律。在固体和液体生长培养基中进行的微生物学研究表明，所得系统对……和……始终具有高抗菌活性。
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