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载卡马西平及辅酶 Q10 的壳聚糖脂质体的设计、优化和评价。

Chitosan-coated liposome-containing carbamazepine and coenzyme Q10: design, optimization and evaluation.

机构信息

Faculty of Pharmacy, Pharmaceutical Technology Department, Bezmialem Vakif University, Istanbul, Turkey.

出版信息

J Liposome Res. 2021 Dec;31(4):389-398. doi: 10.1080/08982104.2020.1849280. Epub 2020 Nov 26.

DOI:10.1080/08982104.2020.1849280
PMID:33183104
Abstract

Conventional formulations cannot sufficiently control seizures and influence on cognitive corruption and oxidative stress with chronic usage in patients with epilepsy. To defeat this issue, it was planned to develop polymeric liposome formulations that are using for their bioavailability and enhancer impact in oral epilepsy treatment. In this study, chitosan-coated liposomal formulations that encapsulate carbamazepine (CBZ) and coenzyme Q10 (CoQ10) were prepared and optimized by utilizing response surface methodology (RSM). Encapsulation efficiencies of CBZ and CoQ10, which were chosen as dependent variables for optimized chitosan-coated liposomal formulations were determined as 76.13%±2.34% and 82.36%±3.15%, respectively. Narrow size distribution was provided with an average size of 187.1 ± 2.35 nm, while a spherical and uniform shape was approved with transmission electron microscopy analyses. Cumulative release of 78.23% for CBZ and 27.12% for CoQ10 was obtained after 24 hours of release study in sink conditions. Physical stability analyses demonstrated that optimum liposomes were convenient for storage at 5 ± 3 °C for at least 90 days. As a result, optimum chitosan-coated liposome containing CBZ and CoQ10 formulations could be suggested as a hopeful approach concerning their release, particle size, high encapsulation efficiency and stability for the treatment of epilepsy.

摘要

传统制剂在癫痫患者的慢性使用中不能充分控制癫痫发作,也不能影响认知损害和氧化应激。为了解决这个问题,计划开发聚合物脂质体制剂,用于提高其生物利用度,并增强口服癫痫治疗的效果。在这项研究中,采用响应面法(RSM)制备并优化了壳聚糖包覆的脂质体制剂,该制剂包封了卡马西平(CBZ)和辅酶 Q10(CoQ10)。作为优化壳聚糖包覆脂质体制剂的依赖变量,测定了 CBZ 和 CoQ10 的包封效率,分别为 76.13%±2.34%和 82.36%±3.15%。平均粒径为 187.1±2.35nm,提供了较窄的粒径分布,而透射电子显微镜分析则证实了球形和均匀的形态。在 24 小时的释放研究中,在溶出条件下,CBZ 的累积释放率为 78.23%,CoQ10 的累积释放率为 27.12%。物理稳定性分析表明,最佳脂质体在 5±3°C 下至少可方便储存 90 天。因此,含有 CBZ 和 CoQ10 的最佳壳聚糖包覆脂质体制剂可以作为一种有希望的方法,用于治疗癫痫,其具有释放、粒径、高包封效率和稳定性等特点。

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