Implementation of the Box-Behnken Design in the Development and Optimization of Methotrexate-Loaded Microsponges for...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Methotrexate (MTX) is a vital anticancer drug with poor oral absorption due to low water solubility.
• Developing advanced drug delivery systems is crucial to enhance MTX bioavailability and therapeutic efficacy.

Purpose of the Study:

• To formulate and optimize sustained-release methotrexate-loaded microsponges using a quasi-emulsion solvent diffusion method.
• To enhance intestinal absorption and bioavailability of MTX for improved colon cancer therapy.

Main Methods:

• Utilized Box-Behnken design (BBD) for formulation optimization.
• Characterized microsponges for particle size, encapsulation efficiency (EE), and drug release kinetics.
• Employed FTIR and DSC for compatibility studies and cytotoxicity assays on HT-29 colon cancer cells.

Main Results:

• Optimized microsponges achieved 87.19% EE and 2.176 µm particle size.
• Demonstrated sustained drug release (85.71%) and good stability across various pH conditions.
• MTX-loaded microsponges significantly reduced HT-29 colon cancer cell viability in a dose-dependent manner.

Conclusions:

• The developed MTX-loaded microsponges, optimized via BBD and encapsulated in Eudragit S-100 coated capsules, show potential for targeted colon drug delivery.
• This formulation represents a promising carrier system for colon cancer treatment, enhancing MTX's therapeutic index.