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用于胃溃疡潜在治疗的水飞蓟素负载壳聚糖-蒙脱石微珠的制备与评价

Formulation and Evaluation of Silymarin-Loaded Chitosan-Montmorilloite Microbeads for the Potential Treatment of Gastric Ulcers.

作者信息

Sharma Ameya, Puri Vivek, Kakkar Vandita, Singh Inderbir

机构信息

Department of Pharmaceutics, Chitkara College of Pharmacy, Chitkara University, Patiala 140401, India.

University Institute of Pharmaceutical Sciences, Panjab University, Chandigarh 160101, India.

出版信息

J Funct Biomater. 2018 Sep 10;9(3):52. doi: 10.3390/jfb9030052.

DOI:10.3390/jfb9030052
PMID:30201932
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6164251/
Abstract

Silymarin-loaded mucoadhesive microbeads of Chitosan-MMT were developed using the ionotropic gelation technique. Characterization of the microbeads was performed by DSC, XRD, SEM, and FTIR techniques. In vitro mucoadhesion and drug release studies; gastroprotective studies including the measurement of ulcerative index; the determination of gastric wall mucus; and the determination of percentage protection, biochemical, and histopathological studies were also performed. Microbeads batches were evaluated for particle size (120⁻140 µm), actual drug content, (49.36⁻58.18%) and entrapment efficiency (72.52⁻92.39%).Biochemical estimation of myeloperoxidase was found to be 0.10⁻0.75 µmoles/g/tissue. Significant reduction in the ulcerative index showed the gastroprotective effect of the formulation. Silymarin-loaded beads of Chitosan-MMT were found to exhibit good mucoadhesion and efficient release of the drug, and were found to be a promising drug carrier system for the treatment of gastric ulcers.

摘要

采用离子凝胶化技术制备了负载水飞蓟素的壳聚糖-蒙脱土粘膜粘附微球。通过差示扫描量热法（DSC）、X射线衍射法（XRD）、扫描电子显微镜法（SEM）和傅里叶变换红外光谱法（FTIR）对微球进行了表征。还进行了体外粘膜粘附和药物释放研究；包括溃疡指数测量的胃保护研究；胃壁粘液的测定；以及保护百分比、生化和组织病理学研究的测定。对微球批次进行了粒径（120⁻140 µm）、实际药物含量（49.36⁻58.18%）和包封率（72.52⁻92.39%）的评估。发现髓过氧化物酶的生化估计值为0.10⁻0.75微摩尔/克/组织。溃疡指数的显著降低显示了该制剂的胃保护作用。发现负载水飞蓟素的壳聚糖-蒙脱土微球具有良好的粘膜粘附性和药物的有效释放，并且被发现是一种有前途的用于治疗胃溃疡的药物载体系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/324726f85363/jfb-09-00052-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/117edd76d1fa/jfb-09-00052-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/a6e2e5bd3d5e/jfb-09-00052-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/2b101940bf56/jfb-09-00052-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/7137b60a5859/jfb-09-00052-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/c6e9c4f52b59/jfb-09-00052-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/324726f85363/jfb-09-00052-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/117edd76d1fa/jfb-09-00052-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/a6e2e5bd3d5e/jfb-09-00052-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/2b101940bf56/jfb-09-00052-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/7137b60a5859/jfb-09-00052-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/c6e9c4f52b59/jfb-09-00052-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b27a/6164251/324726f85363/jfb-09-00052-g006.jpg

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