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Formulation and Evaluation of Capecitabine-Loaded Microsponges for Colon Targeting.
Subhabrota Majumdar1, Sanjay Dey2, Beduin Mahanti3
1Department of Pharmaceutics, Calcutta Institute of Pharmaceutical Technology & AHS, Banitabla, Uluberia, Howrah- 711316, West Bengal, India.
Current Drug Delivery
|August 13, 2025
Summary
Colon-targeting capecitabine (CAP) microsponges were developed to improve oral bioavailability. The optimized formulation demonstrated sustained release and enhanced CAP delivery for effective colon cancer management.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Oncology
Background:
- Capecitabine (CAP) is an oral chemotherapeutic prodrug of 5-fluorouracil, utilized for metastatic breast and colon cancers.
- CAP inhibits DNA synthesis, thereby slowing tumor progression.
Purpose of the Study:
- To develop colon-targeting capecitabine (CAP)-loaded microsponges.
- To utilize the quasi-emulsion solvent diffusion technique with Hydroxypropyl Cellulose (HPC) and Ethyl Cellulose (EC) polymers.
Main Methods:
- Formulation of CAP-loaded microsponges via quasi-emulsion solvent diffusion.
- Statistical optimization using a 3^2 factorial design.
- In vivo pharmacokinetic evaluation in Albino Wistar Rats.
Main Results:
- The F1 formulation (1:1 HPC:EC, 1000 rpm) showed optimal drug release (69.57% at 12h) and high entrapment efficiency (73.09%).
- Optimized microsponges significantly improved CAP oral bioavailability (1.48-fold AUC0-∞ increase, p<0.05) compared to aqueous CAP solution.
Conclusions:
- Developed CAP-loaded microsponges show potential for sustained colon delivery of capecitabine.
- This formulation enhances oral bioavailability, offering a promising approach for colon cancer treatment.
- Further studies on comparative evaluation and stability are recommended.
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