Dept of Pharmaceutics, JSS College of Pharmacy, JSS University, SS Nagar, Mysore 15, Karnataka, India.
Saudi Pharm J. 2013 Apr;21(2):177-86. doi: 10.1016/j.jsps.2012.07.002. Epub 2012 Aug 11.
The present investigation was designed with the intention to formulate a versatile 5-fluorouracil(5-FU) matrix tablet surpassing issues associated with current conventional chemotherapeutic drug delivery systems. The novel 5-FU matrix tablet fulfills therapeutic needs by engineering matrix tablets utilizing chitosan-sodium alginate interpolyelectrolyte complex (IPEC). IPEC was characterized by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray diffraction (XRD). The matrix tablets were formulated utilizing IPEC alone and in combination with chitosan, sodium alginate and sodium deoxycholate as permeation enhancer. Pharmaceutical properties, swelling studies, in vitro dissolution and diffusion studies, mucoadhesive studies and in vivo studies were performed for formulated 5-FU. The selected chitosan-sodium alginate IPEC offers pH independent 5-FU release in comparison to alone or physical mixture of chitosan and sodium alginate. Furthermore, novel matrix tablets demonstrated significantly higher bioadhesive properties with controlled 5-FU release without the initial burst effect and also demonstrated a higher permeation of 5-FU. To conclude, the developed novel 5-FU matrix tablets pave way as an excellent alternative for cancer treatment which could potentially minimize the dose dependent side effects and provide better patient compliance.
本研究旨在设计一种通用的 5-氟尿嘧啶(5-FU)基质片剂,克服当前常规化疗药物传递系统存在的问题。新型 5-FU 基质片剂通过利用壳聚糖-海藻酸钠聚电解质复合物(IPEC)工程基质片剂来满足治疗需求。通过傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)和 X 射线衍射(XRD)对 IPEC 进行了表征。该基质片剂仅使用 IPEC 以及与壳聚糖、海藻酸钠和脱氧胆酸钠作为渗透增强剂组合进行了配方设计。对所制备的 5-FU 进行了药物特性、溶胀研究、体外溶解和扩散研究、黏膜黏附研究和体内研究。与壳聚糖和海藻酸钠的单独使用或物理混合物相比,所选的壳聚糖-海藻酸钠 IPEC 提供了 pH 依赖性的 5-FU 释放。此外,新型基质片剂表现出显著更高的生物黏附特性,可控制 5-FU 释放,无初始突释效应,并且 5-FU 的渗透也更高。总之,开发的新型 5-FU 基质片剂为癌症治疗提供了一种极好的替代方案,有可能最大限度地减少剂量依赖性副作用并提高患者的顺应性。