Abstract

Aim

The present study was conducted to formulate and investigate liposomes for the dual drug delivery based on anti-tubercular drug(s) combination i.e. Isoniazid (INH) and Rifampicin (RIF).

Materials and methods

Mannosylated and non mannosylated liposomes were prepared by lipid thin film hydration method, using DSPC: Chol at a molar ratio 6:4 while in case of mannosylated liposomes DSPC: Chol: Man-C4-Chol at a molar ratio 6.0:3.5:0.5 were used and extensively characterised. The particle size and zeta potential were recorded to be 1.29 ± 0.24 µm and −9.1 ± 0.11 mV. The drug entrapment (%) was recorded to be 84.7 ± 1.25% for Rifampicin and 31.8 ± 0.12% for Isoniazid.

Results

The antitubercular activity studied in Balb/C mice was maximum in the case of mannosylated liposomes. The biodistribution studies also revealed higher drug(s) concentration (accumulation) maintained over a protracted period.

Conclusions

The liposomal preparations are passively as well as actively uptaken by the alveolar macrophages which are the cellular tropics of infection. The mannosylated liposomes appear to be a potential carrier for dual drug delivery and targeted antitubercular therapy.

中文翻译：

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用于巨噬细胞靶向的双抗结核药物脂质体：开发、表征、离体和体内评估

 抽象的

 目的

本研究旨在配制和研究基于抗结核药物组合（即异烟肼（INH）和利福平（RIF））的双重药物递送的脂质体。

 材料和方法

通过脂质薄膜水合法制备甘露糖化和非甘露糖化脂质体，使用摩尔比为6:4的DSPC:Chol，而在甘露糖化脂质体的情况下，摩尔比为6.0:3.5:0.5的DSPC:Chol:Man-C4-Chol使用并广泛表征。粒径和 zeta 电位记录为 1.29 ± 0.24 µm 和 -9.1 ± 0.11 mV。利福平的药物包封率 (%) 为 84.7 ± 1.25%，异烟肼为 31.8 ± 0.12%。

 结果

在 Balb/C 小鼠中研究的抗结核活性在甘露糖化脂质体的情况下是最大的。生物分布研究还表明，在较长一段时间内维持较高的药物浓度（蓄积）。

 结论

脂质体制剂被肺泡巨噬细胞被动和主动吸收，肺泡巨噬细胞是感染的细胞趋向性。甘露糖化脂质体似乎是双重药物递送和靶向抗结核治疗的潜在载体。