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使用生物相容性天然树胶卡蒂拉制备用于结肠靶向递送5-氟尿嘧啶的聚合物微球制剂

Polymeric Microsphere Formulation for Colon Targeted Delivery of 5-Fluorouracil Using Biocompatible Natural Gum Katira.

作者信息

Karan Saumen, Choudhury Hira, Chakra Biplab Kumar, Chatterjee Tapan Kumar

机构信息

Department of Pharmaceutical Technology, Jadavpur University, Kolkata, India. Email:

Department of Pharmaceutical Technology, School of Pharmacy, International Medical University, Jalan Jalil Perkasa, Bukit Jalil, Kuala Lumpur, Malaysia.

出版信息

Asian Pac J Cancer Prev. 2019 Jul 1;20(7):2181-2194. doi: 10.31557/APJCP.2019.20.7.2181.

Abstract

Controlled release delivery system of chemotherapeutic agents at the site of colon endorses modern drug-entrapped delivery tools, which release the entrappedagents at a controlled rate for anextended period providing patient compliance and additional protection from the degradinggastric environment. Thus, the present study was aimed to develop and optimize a novel polymeric microsphere of 5-fluorouracil (5-FU) using natural gum katira to obtain an optimal therapeutic response at the colon. Due course of experimentation, in-vivo safety profile of the gum katira in an animal model was established. Modified solvent extraction/evaporation technique wasemployed to encapsulate 5-FU in the natural polymeric microsphere and was characterized using in-vitro studies to investigate particle size, morphology, encapsulation efficiency and release of the drug from developed formulation. Formulated and optimized polymeric microsphere of 5-FU using gum katira polymer own optimal physicochemical characteristics with a fine spherical particle with size ranged from 210.37±7.50 to 314.45±7.80 μm.Targeted microsphere exhibited good cytotoxicity and also has high drug entrapment efficiency, and satisfactory release pattern of the drug within a time frame of 12 h. Finally, we foresee that the optimized polymeric gum katiramicrosphere of 5-FU could be a promising micro-carrier for efficient colon drug targeting delivery tool with improved chemotherapeutic efficacy against colon cancer.

摘要

结肠部位化疗药物的控释给药系统采用了现代载药递送工具,这些工具能以可控速率长时间释放所载药物,提高患者依从性,并额外保护药物免受胃部降解环境的影响。因此,本研究旨在开发并优化一种以天然树胶卡蒂拉为载体的新型5-氟尿嘧啶(5-FU)聚合物微球,以在结肠部位获得最佳治疗效果。在实验过程中,确定了卡蒂拉树胶在动物模型中的体内安全性。采用改良溶剂萃取/蒸发技术将5-FU包裹在天然聚合物微球中,并通过体外研究对其进行表征,以研究粒径、形态、包封效率以及药物从所开发制剂中的释放情况。使用卡蒂拉树胶聚合物制备并优化的5-FU聚合物微球具有最佳的理化特性,呈精细球形颗粒,粒径范围为210.37±7.50至314.45±7.80μm。靶向微球表现出良好的细胞毒性,并且具有较高的药物包封率,以及在12小时内令人满意的药物释放模式。最后,我们预计,优化后的5-FU卡蒂拉树胶聚合物微球可能是一种有前景的微载体,可作为高效的结肠药物靶向递送工具,提高对结肠癌的化疗疗效。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/55bd/6745213/5760c304e40a/APJCP-20-2181-g001.jpg

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