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具有黏附性的瓜尔胶基水凝胶互穿壳聚糖-g-聚己内酯胶束用于利福平递送。

Mucoadhesive guargum hydrogel inter-connected chitosan-g-polycaprolactone micelles for rifampicin delivery.

机构信息

Henan Key Laboratory of Cancer Epigenetics, Cancer Institute, The First affiliated Hospital, and College of Clinical Medicine of Henan University of Science and Technology, Luoyang, 471003, China.

Biomaterials in Medicinal Chemistry Laboratory, Department of Natural Products Chemistry, School of Chemistry, Madurai Kamaraj University, Madurai, 625021, India.

出版信息

Carbohydr Polym. 2019 Feb 15;206:1-10. doi: 10.1016/j.carbpol.2018.10.098. Epub 2018 Oct 29.

DOI:10.1016/j.carbpol.2018.10.098
PMID:30553301
Abstract

Natural polymer guar gum has one of the highest viscosities in water solution and hence, these are significantly used in pharmaceutical applications. Guar gum inter-connected micelles as a new carrier has been developed for poor water soluble rifampicin drug. The hydrogel inter-connected micelle core was formulated as a hydrophilic inner and hydrophobic outer core by using guar gum/chitosan/polycaprolactone and the carrier interaction with rifampicin was confirmed by FT-IR. The morphological observations were carried out through TEM, SEM and AFM analysis. The encapsulation efficiency and in-vitro drug release behavior of prepared hydrogel based micelle system was analyzed by UV-vis spectrometry. The anti-bacterial activity against K. pneumoniae and S. aureus was studied by observing their ruptured surface by SEM. The cytotoxicity study reveals that the pure polymeric system has no toxic effect whereas drug loaded ones showed superior activity against THP-1 cells. From the cell apoptosis analyses, the apoptosis was carried out in a time dependent manner. The cell uptake behavior was also observed in THP-1 cells which indicate that the hydrogel based micelle system is an excellent material for the mucoadhesive on intracellular alveolar macrophage treatment.

摘要

天然高分子瓜尔胶在水溶液中的粘度最高,因此在药物应用中得到了广泛的应用。为了提高疏水性利福平药物的水溶性,开发了以瓜尔胶/壳聚糖/聚己内酯为载体的互穿胶束作为新的载体。通过 FT-IR 证实了水凝胶互穿胶束核与利福平的载体相互作用。通过 TEM、SEM 和 AFM 分析进行了形态观察。通过紫外可见分光光度法分析了制备的水凝胶基胶束系统的包封效率和体外药物释放行为。通过观察 SEM 破裂表面研究了对 K. pneumoniae 和 S. aureus 的抗菌活性。细胞毒性研究表明,纯聚合物体系没有毒性,而载药体系对 THP-1 细胞表现出更好的活性。从细胞凋亡分析来看,细胞凋亡是时间依赖性的。在 THP-1 细胞中也观察到了细胞摄取行为,这表明基于水凝胶的胶束系统是一种用于细胞内肺泡巨噬细胞治疗的黏附性的优秀材料。

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