Rani Deepika, Ahuja Munish
Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar 125001 (Haryana), India.
Drug Delivery Research Laboratory, Department of Pharmaceutical Sciences, Guru Jambheshwar University of Science & Technology, Hisar 125001 (Haryana), India.
Int J Biol Macromol. 2017 Jun;99:233-240. doi: 10.1016/j.ijbiomac.2017.02.036. Epub 2017 Feb 24.
Carboxymethylation of Lepidium sativum polyuronide was carried out to improve its functionality. Carboxymethyl modification was accomplished by reacting it with monochloroacetic acid under alkaline conditions, which yielded a product with degree of carboxymethyl substitution of 1.75. The results of characterization studies revealed that carboxymethylation of L. sativum polyuronide improves its flow property, changes compression behavior from elastic to plastic, diminishes its viscosity and swelling, and increases its crystallinity. The interaction between the anionic carboxymethyl lepidium polyuronide and Mg ions was utilized to prepare ionically gelled nanoparticles employing ofloxacin as a model drug. A selected nanoparticulate formulation prepared by interaction between solutions of ofloxacin (0.1%, w/v) containing carboxymethyl lepidium polyuronide (0.15%, w/v) and magnesium chloride (0.05%, w/v) had particle size of 405nm and drug entrapment of 90.41%. On comparative evaluation, no significant difference was observed between the antibacterial activity of selected nanoformulation and conventional aqueous solution of ofloxacin. Further, the nanoparticulate formulation was observed to sustain the release of ofloxacin with 97% of the drug getting released over 12h. The release of ofloxacin from nanoformulation was found to follow first order kinetics with the mechanism of release being erosion of polymer matrix.
对独行菜聚糖醛酸进行羧甲基化以改善其功能。羧甲基化修饰是通过在碱性条件下使其与一氯乙酸反应来完成的,得到了羧甲基取代度为1.75的产物。表征研究结果表明,独行菜聚糖醛酸的羧甲基化改善了其流动性,将压缩行为从弹性变为塑性,降低了其粘度和溶胀度,并提高了其结晶度。利用阴离子羧甲基化独行菜聚糖醛酸与镁离子之间的相互作用,以氧氟沙星为模型药物制备离子凝胶化纳米颗粒。通过含有羧甲基化独行菜聚糖醛酸(0.15%,w/v)的氧氟沙星溶液(0.1%,w/v)与氯化镁(0.05%,w/v)之间的相互作用制备的一种选定纳米颗粒制剂,其粒径为405nm,药物包封率为90.41%。经比较评估,选定的纳米制剂与氧氟沙星传统水溶液的抗菌活性之间未观察到显著差异。此外,观察到纳米颗粒制剂可维持氧氟沙星的释放,12小时内97%的药物被释放。发现氧氟沙星从纳米制剂中的释放遵循一级动力学,释放机制为聚合物基质的侵蚀。