Preparation of Pectin/Chitosan-based Paclitaxel Colon-targeted Microcapsules and Study on Their Tolerance in an in vitro Artificial Gastrointestinal Tract
WEN Wei-tian
ZHANG Cai-ling
Abstract：Objective: To develop a pectin and chitosan-based colon-targeted microcapsule for paclitaxel (PTX) and evaluate its stability and drug release characteristics in an artificial simulated gastrointestinal environment. Methods: Pectin/chitosan double-polymer microcapsules (PCPM) were prepared using an ionic gelation method combined with spray-drying technology, with PTX as the model drug. The morphology and mechanical strength of the microcapsules were observed using a stereomicroscope, and the encapsulation efficiency and drug loading were determined. The drug release behavior and tolerance of the microcapsules were analyzed by simulating artificial gastric juice (pH 1.2) and intestinal fluid (pH 6.8) environments. Results: The average particle sizes of PPS (Note: Likely a typo in the original text; presumably a control sample such as pure pectin microcapsules) and PCPM microcapsules were (38±4) μm and (50±5) μm, respectively. The encapsulation efficiencies were 95.7%±1.0% and 86.2%±7.6%, and the drug loadings were 47.8%±0.5% and 43.1%±3.8%, respectively. The protection rate of PTX in PCPM microcapsules was significantly higher than that of the PTX standard in artificial gastrointestinal fluid, reaching 67.0%±0.8% at 2 h. The total release rate in colonic fluid reached 91.0%±0.8% within 8 h, indicating that PCPM microcapsules achieve colon-specific drug release through enzymatic hydrolysis in the gastrointestinal tract. Conclusion: PCPM has good gastrointestinal tolerance and colon-targeted drug release performance, which is a new strategy for colon-targeted delivery of oral formulations of PTX.
Keywords：pectinchitosanpaclitaxelmicrocapsulecolon targetingartificial gastrointestinal tolerance
Publication Date：2025-03-31
Online Publishing Date：2025-08-15(First online date of this platform, not the publication date of the document)
Pages：7( 27-33 )