In vitro controlled release of colon targeted mesalamine from compritol ATO 888 based matrix tablets using factorial...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Materials Science

Background:

• Mesalamine is used for inflammatory bowel disease, requiring targeted delivery to the colon.
• Conventional formulations may have suboptimal release profiles and targeting efficiency.
• Developing controlled-release systems enhances therapeutic efficacy and patient compliance.

Purpose of the Study:

• To design and develop a 24-hour controlled-release matrix formulation for mesalamine.
• To achieve colon targeting using pectin as a bacterial-dependent polymer.
• To optimize the formulation using a 3(2) full factorial design.

Main Methods:

• Formulation of mesalamine solid dispersions with glyceryl behenate (Compritol 888 ATO) as a matrix agent.
• Incorporation of pectin for colon targeting.
• Preparation of matrix tablets by direct compression.
• In vitro drug release studies.
• Optimization using a 3(2) full factorial design with glyceryl behenate and pectin as variables.
• Surface and cross-section analysis using scanning electron microscopy (SEM).

Main Results:

• Mesalamine release extended beyond 24 hours from the developed matrix tablets.
• SEM images revealed pores and channels in the matrix, facilitating drug release.
• Pectin incorporation effectively contributed to colon targeting.
• The drug release mechanism was primarily diffusion-controlled.
• Factorial design indicated that optimal glyceryl behenate and high pectin amounts favor colon targeting and controlled release.

Conclusions:

• A novel colon-targeted, 24-hour controlled-release mesalamine formulation was successfully developed.
• The combination of glyceryl behenate and pectin offers a promising approach for effective mesalamine delivery.
• The formulation's characteristics suggest improved therapeutic outcomes for colonic diseases.