亚麻籽胶的巯基功能化：制备、表征及作为黏附聚合物的评价。
Thiol functionalization of flaxseed mucilage: Preparation, characterization and evaluation as mucoadhesive polymer.
机构信息
Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar 125001, India.
Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science and Technology, Hisar 125001, India.
出版信息
Int J Biol Macromol. 2019 Apr 1;126:101-106. doi: 10.1016/j.ijbiomac.2018.12.116. Epub 2018 Dec 14.
The aim of present study is to browse mucoadhesive potential of flaxseed mucilage after thiol functionalization. Thiol-derivatization of flaxseed mucilage (FSM) polysaccharide was obtained by esterification with thioglycolic acid. Thiolation of FSM was confirmed by -SH stretch in FTIR spectra at 2549.01 cm. Thiolated flaxseed mucilage (TFSM) was distinguished by XRD, DSC, NMR & SEM analysis. TFSM was found to contain 325.6 mM of thiol groups/g as determined by Ellman's method. The mucoadhesive property of drug loaded TFSM pellets, carried out by using chicken buccal pouch membrane, displayed greater ex-vivo bioadhesion time as compared to FSM. This improvement in mucoadhesion property of TFSM over FSM can be attributed to the formation of disulphide bond between mucus and thiolated mucilage. Further, the in-vitro dissolution study conducted in phosphate buffer (pH 6.8) provided release of diclofenac sodium for a prolonged period of 12 h for TFSM pellets by anomalous transport mechanism of drug release following zero order model of release kinetics.
本研究旨在探讨巯基化修饰对亚麻籽胶黏附性能的影响。采用巯基乙酸酯化法对亚麻籽胶（FSM）多糖进行巯基化修饰。FTIR 光谱中 2549.01 cm-1 处的 -SH 伸缩振动峰证实了 FSM 的巯基化。通过 XRD、DSC、NMR 和 SEM 分析对 TFSM 进行了区分。通过 Ellman 法测定，TFSM 中的巯基含量为 325.6 mM/g。通过鸡口腔囊膜进行载药 TFSM 丸剂的体外黏附实验，结果表明其体外黏附时间明显长于 FSM。TFSM 相较于 FSM 具有更好的黏附性能，这归因于巯基化亚麻籽胶与黏液之间形成了二硫键。此外，在 pH 6.8 的磷酸盐缓冲液中进行的体外溶出实验表明，TFSM 丸剂通过零级动力学模型的药物释放遵循异常转运机制，可在 12 小时内持续释放较长时间的双氯芬酸钠。
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