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image of Formulation and Evaluation of Capecitabine-Loaded Microsponges for Colon Targeting

Abstract

Introduction

Capecitabine (CAP) is a chemotherapeutic drug used oral administration for the management of metastatic cancers of the breast and colon. CAP is a prodrug of 5-fluorouracil, which inhibits DNA synthesis and slows tumor growth. The objective of the current research was to develop colon-targeting CAP-loaded microsponges by quasi-emulsion solvent diffusion technique employing Hydroxypropyl Cellulose (HPC) and Ethyl Cellulose (EC) as constituent polymers at different ratios with varying stirring speeds (rpm).

Methods

In the present study, CAP-loaded microsponges were formulated by quasi-emulsion solvent diffusion method using HPC and EC as polymers at different ratios with varying stirring speeds. The 32-factorial design was used to perform the statistical optimization of CAP-loaded microsponges. The pharmacokinetic study of the optimized formulation of CAP-loaded microsponges was performed using Albino Wistar Rats.

Results

Based on the statistical optimization, the F1 formulation prepared using a 7:1 ratio of HPC and EC with 1000 rpm stirring speed was selected for its effective drug release (31.13 ± 1.73% after 8 hours and 69.57 ± 2.53% after 12 hours) and the highest drug entrapment efficiency (73.09 ± 3.54%). The 1.28-fold increase in indicated that the optimized CAP-loaded microsponge formulation significantly (< 0.05) improved the oral bioavailability of CAP compared to its aqueous solution, when administered orally.

Discussion

These findings indicated the potential delivery of CAP by these CAP-loaded microsponges to the colon, enabling sustained delivery and improving the bioavailability of CAP. However, comparative evaluation with existing marketed formulation and stability studies is essential to validate its therapeutic implications.

Conclusion

The developed CAP-loaded microsponges could serve as an effective carrier for the sustained release of CAP, thereby improving the oral bioavailability of CAP for the management of colon cancer.

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2025-08-11
2025-09-25

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Formulation and Evaluation of Capecitabine-Loaded Microsponges for Colon Targeting
Bentham Science Publishers ; https://doi.org/10.2174/0115672018389882250704071618
/content/journals/cdd/10.2174/0115672018389882250704071618
/content/journals/cdd/10.2174/0115672018389882250704071618
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  • Article Type:     Research Article
Keywords: microsponges ; drug delivery ; optimization ; colon cancer ; colon targeting ; Capecitabine

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