What question did this study set out to answer?

To formulate and evaluate enteric-coated dextran microspheres designed for site-specific delivery of 5-fluorouracil to the colon.

May 20, 2014Drug DeliveryOpen Access

Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon

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Authors

GRG. RaiIndian Institute of Information Technology Design and Manufacturing Jabalpur AYAwesh K. YadavNational Institute of Pharmaceutical Education and Research NJNilesh JainIpca Laboratories (India)

Discussion

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Implication

Preclinical formulation study demonstrates targeted release of 5-fluorouracil in colonic conditions using enteric-coated dextran microspheres, suggesting a viable site-specific drug delivery system.

Key Points

To formulate and evaluate enteric-coated dextran microspheres designed for site-specific delivery of 5-fluorouracil to the colon.
Fabricated dextran microspheres via emulsification-crosslinking, systematically evaluating variables including dextran molecular weight, drug-to-polymer ratio, crosslinking agent volume, and stirring speed.
Coated the core microspheres with Eudragit S-100 via oil-in-oil solvent evaporation at 4:1 and 8:1 coat:core ratios.
Characterized formulations by size, morphology, entrapment efficiency, differential scanning calorimetry (DSC), in vitro release (with dextranase and 2% rat cecal contents), and organ distribution.
Coated microspheres exhibited strictly pH-dependent release, showing zero drug release under acidic gastric conditions and rapid release upon Eudragit solubilization at elevated pH.
Continuous drug release in the colon was driven by enzymatic degradation of the dextran core by colonic enzymes and dextranase.
Organ distribution studies confirmed that the formulation resisted premature release in gastric and upper intestinal environments while successfully releasing 5-fluorouracil in the colon.

Cite This Study

Rai et al. (2014) studied this question.

synapsesocial.com/papers/69dd43ee99c691022d99b9ad https://doi.org/10.3109/10717544.2014.913733

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May 20, 2014Drug DeliveryOpen Access

Eudragit-coated dextran microspheres of 5-fluorouracil for site-specific delivery to colon

View Full Paper

Ask AI

Bookmark

Authors

GRG. RaiIndian Institute of Information Technology Design and Manufacturing Jabalpur AYAwesh K. YadavNational Institute of Pharmaceutical Education and Research NJNilesh JainIpca Laboratories (India)

Discussion

Member takes

Implication

Preclinical formulation study demonstrates targeted release of 5-fluorouracil in colonic conditions using enteric-coated dextran microspheres, suggesting a viable site-specific drug delivery system.

Key Points

To formulate and evaluate enteric-coated dextran microspheres designed for site-specific delivery of 5-fluorouracil to the colon.
Fabricated dextran microspheres via emulsification-crosslinking, systematically evaluating variables including dextran molecular weight, drug-to-polymer ratio, crosslinking agent volume, and stirring speed.
Coated the core microspheres with Eudragit S-100 via oil-in-oil solvent evaporation at 4:1 and 8:1 coat:core ratios.
Characterized formulations by size, morphology, entrapment efficiency, differential scanning calorimetry (DSC), in vitro release (with dextranase and 2% rat cecal contents), and organ distribution.
Coated microspheres exhibited strictly pH-dependent release, showing zero drug release under acidic gastric conditions and rapid release upon Eudragit solubilization at elevated pH.
Continuous drug release in the colon was driven by enzymatic degradation of the dextran core by colonic enzymes and dextranase.
Organ distribution studies confirmed that the formulation resisted premature release in gastric and upper intestinal environments while successfully releasing 5-fluorouracil in the colon.

Cite This Study

Rai et al. (2014) studied this question.

synapsesocial.com/papers/69dd43ee99c691022d99b9ad https://doi.org/10.3109/10717544.2014.913733

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