Department of Pharmacy, Quaid-i-Azam University, Islamabad 45320, Pakistan.
Department of Pharmaceutical Technology, University of Szeged, Eötvös u. 6, 6720, Hungary.
Nanomedicine (Lond). 2019 Aug;14(15):1945-1969. doi: 10.2217/nnm-2018-0415. Epub 2019 Jul 29.
To fabricate and evaluate the therapeutic efficacy of glycyrrhizic acid (GA)-loaded pH-sensitive nanoformulations that specifically target and combat mucosal inflammation of the colon. GA-loaded Eudragit S100/poly-(lactic-co-glycolic acid) nanoparticles were developed through modified double-emulsion evaporation coupled with solvent evaporation coating techniques and analyzed for physicochemical characteristics, surface chemistry, release kinetics, site-retention and therapeutic effectiveness. Nanoparticles have a particle size of approximately 200 nm, high encapsulation efficiency, desired surface chemistry with pH-dependent and sustained drug release behavior following the Gompertz kinetic model. retention and therapeutic effectiveness in the inflamed colon tissues were confirmed by macroscopic and microscopic indices, cytokine analysis and antioxidant assays. GA-loaded Eudragit S100/poly-(lactic-co-glycolic acid) nanoparticles could efficiently deliver GA to the colon and ameliorate the mucosal inflammation for a prolonged duration.
制备并评价甘草酸（GA）载药 pH 敏感纳米制剂，该纳米制剂特异性靶向并治疗结肠黏膜炎症。 通过改良的双重乳液蒸发法结合溶剂蒸发包衣技术，制备了载 GA 的 Eudragit S100/聚（乳酸-共-羟基乙酸）纳米粒，并对其理化特性、表面化学、释放动力学、部位保留和治疗效果进行了分析。 纳米粒的粒径约为 200nm，具有较高的包封效率，所需的表面化学性质，具有 pH 依赖性和符合 Gompertz 动力学模型的持续药物释放行为。 通过宏观和微观指标、细胞因子分析和抗氧化测定，证实了载 GA 的 Eudragit S100/聚（乳酸-共-羟基乙酸）纳米粒在炎症结肠组织中的保留和治疗效果。 载 GA 的 Eudragit S100/聚（乳酸-共-羟基乙酸）纳米粒可以有效地将 GA 递送到结肠，并在较长时间内改善黏膜炎症。
