Design, optimization, and evaluation of a pH-sensitive hydrogel system for colon-targeted mesalamine delivery
摘要
This study investigates a pH-responsive hydrogel for the targeted delivery of mesalamine to treat colitis. The hydrogel exhibited excellent pH-dependent swelling and drug release behaviour, releasing approximately 80% of cumulative mesalamine in colonic (pH 7.4) conditions over 48 h. In vitro, drug release from the pH-responsive hydrogel in response to extracellular acidity was demonstrated. In preclinical in vivo studies, rats treated with the pH-responsive hydrogel had significantly lower Disease Activity Index (DAI) scores (1.5 ± 0.3) than disease controls (6.2 ± 0.5). Histopathological analysis of colon tissue showed reduced epithelial erosion and inflammation. Biochemical assessments indicated decreased oxidative stress markers (MDA: 5.3 ± 0.8 nmol/g tissue). We also had restored antioxidant levels (GSH: 0.75 ± 0.05 µmol/g tissue). Proinflammatory cytokine levels in treated animals were reduced to less than 8 nmol/g tissue compared to elevated levels in the disease control group. These findings suggest that the developed pH-responsive hydrogel is a promising carrier for targeted mesalamine delivery in ulcerative colitis management.
Graphical Abstract