Colonic Delivery of Celastrol-Loaded Layer-by-Layer Liposomes with Pectin/Trimethylated Chitosan Coating to Enhance Its Anti-Ulcerative Colitis Effects.

ABSTRACT: Herein, a flexible oral colon-targeting delivery system, mediated by electrostatic layer-by-layer alternate deposition with pectin-trimethyl chitosan (TMC) onto liposomes-loading celastrol (Cel/PT-LbL Lipo), was fabricated to enhance anti-UC efficacy. Along with layer-by-layer coating, Cel/Lipo exhibited surface charge reversal, a slight increase in particle size, and a sustained drug release profile in a simulative gastrointestinal tract medium. Based on its bilayer coating of polysaccharides, Cel/PT-LbL Lipo alleviated cytotoxicity of celastrol in colon epithelial NCM460 cells. Due to the strong mucoadhesion of TMC with mucin, PT-LbL Lipo benefited colon localization and prolonged retention ability of its payloads. Ultimately, Cel/PT-LbL Lipo significantly mitigated colitis symptoms and

SUBMITTER: Xian J 

PROVIDER: S-EPMC8703354 | biostudies-literature | 2021 Nov

REPOSITORIES: biostudies-literature