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A novel pH-enzyme-dependent mesalamine colon-specific delivery system
Lei Jin1, Yi-Cun Ding1, Yu Zhang1
1Department of Gastroenterology, Putuo Hospital, Shanghai University of Traditional Chinese Medicine, Shanghai, People's Republic of China.
Drug Design, Development and Therapy
|July 7, 2016
Summary
This study developed a novel pH-enzyme double-dependent mesalamine colon-specific delivery system. The new microparticle system enhances mesalamine absorption in the colon, maintaining therapeutic drug concentrations longer.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Colonic Drug Targeting
Background:
- Inflammatory bowel disease (IBD) management often requires targeted delivery of mesalamine to the colon.
- Conventional mesalamine formulations may exhibit suboptimal colonic drug concentrations and systemic side effects.
- Developing advanced drug delivery systems is crucial for improving therapeutic efficacy and patient outcomes.
Purpose of the Study:
- To design and evaluate a novel pH-enzyme double-dependent mesalamine colon-specific delivery system.
- To assess the in vitro drug release characteristics of the mesalamine-coated microparticles.
- To investigate the in vivo pharmacokinetic and biodistribution profiles of the developed delivery system.
Main Methods:
- Mesalamine-coated microparticles were designed and characterized for particle size (mean diameter 312.2 µm).
- In vitro drug release studies were conducted in simulated gastric (HCl, pH 1.2) and intestinal (PBS, pH 7.4) conditions, followed by extended incubation.
- In vivo pharmacokinetic and biodistribution studies were performed in rats, comparing coated microparticles to suspensions.
Main Results:
- In vitro studies showed minimal mesalamine release at pH 1.2 and 7.4, with 71% release over 20 hours during incubation, indicating colon-specific release.
- In vivo, coated microparticles resulted in a 1.9-fold greater area under the plasma concentration-time curve (AUC0-t) compared to suspensions over 12 hours.
- Colonic AUC0-t was significantly higher (2.63-fold, P<0.05) for coated microparticles, demonstrating enhanced colonic drug exposure.
Conclusions:
- The developed pH-enzyme double-dependent mesalamine-coated microparticles effectively achieve colon-specific drug delivery.
- This system demonstrates sustained drug release and significantly improved colonic drug concentration compared to conventional suspensions.
- The findings suggest potential for enhanced therapeutic efficacy in treating colonic diseases like IBD.
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