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基于交联瓜尔胶和硼酸钠的微球作为5-氟尿嘧啶的结肠靶向抗癌药物递送系统。

Cross-linked guar gum and sodium borate based microspheres as colon-targeted anticancer drug delivery systems for 5-fluorouracil.

作者信息

Kamal Tehsin, Sarfraz Muhammad, Arafat Mosab, Mikov Momir, Rahman Nisarur

机构信息

Department of Pharmacy, COMSATS Institute of Information Technology, Abbottabad, Pakistan.

College of Pharmacy, Al Ain University of Science and Technology, Al Ain, Al Ain, Abu Dhabi, UAE.

出版信息

Pak J Pharm Sci. 2017 Nov;30(6(Supplementary)):2329-2336.

Abstract

The aim was to prepare cross linked polymer of 5-fluorouracil loaded microspheres containing guar gum and sodium borate for colon-targeted drug delivery systems. Micro spheres were prepared using emulsification cross linking method. The influence of drug polymer ratio, cross linker agent concentrations and cross linking timing on in vitro drug release and characteristics in terms of drug loading, entrapment efficiency and yielding percentage were investigated. The optimum drug loading, entrapment efficiency and percent yield were obtained from formulations with the lowest content of cross linker agent over 2 h of cross linking timing but with the highest drug to polymer ratio 1:11. The optimum in vitro drug release was obvious upon decreasing drug to polymer ratio up to 1:09, resulting in 81.5% drug release over 24 h. In conclusion, micro spheres composed of gaur gum and sodium borate can delay and control the release of 5-fluorouracil over 24 h. Thus, further in vivo studies are suggested for final assessment.

摘要

目的是制备用于结肠靶向给药系统的含瓜尔胶和硼酸钠的5-氟尿嘧啶负载微球交联聚合物。采用乳化交联法制备微球。研究了药物与聚合物比例、交联剂浓度和交联时间对体外药物释放以及载药量、包封率和产率等特性的影响。在交联时间为2小时、交联剂含量最低但药物与聚合物比例最高为1:11的配方中获得了最佳载药量、包封率和产率。当药物与聚合物比例降至1:09时,最佳体外药物释放明显,24小时内药物释放率达81.5%。总之,由瓜尔胶和硼酸钠组成的微球可在24小时内延迟并控制5-氟尿嘧啶的释放。因此,建议进一步进行体内研究以进行最终评估。

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