Glycyrrhizic acid-loaded pH-sensitive poly-(lactic-co-glycolic acid) nanoparticles for the amelioration of inflammatory bowel disease

• Published in: Nanomedicine (London, England) England), 2019-08, Vol.14 (15), p.1945-1969
• Main Authors: Zeeshan, Mahira, Ali, Hussain, Khan, Salman, Mukhtar, Mahwash, Khan, Muhammad Ijaz, Arshad, Muhammad
• Format: Article
• Language: English
• Subjects: Animals; Anti-Inflammatory Agents - administration & dosage; Anti-Inflammatory Agents - pharmacokinetics; Anti-Inflammatory Agents - therapeutic use; antioxidant assay; Colon; Colon - drug effects; colon targeting; Delayed-Action Preparations - chemistry; Drug delivery systems; Drug dosages; DSS-induced colitis; gastroenterology; glycyrrhizic acid; Glycyrrhizic Acid - administration & dosage; Glycyrrhizic Acid - pharmacokinetics; Glycyrrhizic Acid - therapeutic use; Hydrogen-Ion Concentration; Inflammation; Inflammatory bowel disease; Inflammatory Bowel Diseases - drug therapy; kinetic models; Lipids; Male; Metabolism; Metabolites; Mice, Inbred BALB C; Molecular weight; Nanoparticles; Nanoparticles - chemistry; pH-sensitive nanoparticles; PLGA nanoparticles; Polylactic Acid-Polyglycolic Acid Copolymer - chemistry; Polymers; Polymethacrylic Acids - chemistry; Polyvinyl alcohol; Sodium; sustained release nanoparticles; Ulcers; x-ray photoelectron spectroscopy
• ISSN: 1743-5889; 1748-6963
• DOI: 10.2217/nnm-2018-0415

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.