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Alginate microparticles for enzyme peroral administration
G Coppi1, V Iannuccelli, M Bernabei
1Department of Pharmaceutical Sciences, University of Modena and Reggio Emilia, Via G. Campi 183, 41100, Modena, Italy. coppi.gilberto@unimo.it
International Journal of Pharmaceutics
|August 15, 2002
Summary
Alginate microparticles protect L-lactate dehydrogenase but require additives for stability and structure. Polyacrylic acid sodium salt is crucial for targeting Peyer
Area of Science:
- Biopharmaceutics
- Drug Delivery Systems
- Enzyme Stabilization
Background:
- Protein and peptide drugs face inactivation in the gastro-intestinal tract.
- Alginate microparticles are explored as carriers for oral delivery.
- Enzyme activity loss is a challenge during alginate microencapsulation.
Purpose of the Study:
- To develop alginate microparticles for L-lactate dehydrogenase delivery.
- To overcome enzyme activity loss during spray-drying.
- To achieve microparticulate structures for Peyer's patch targeting.
Main Methods:
- Spray-drying technique for alginate microparticle fabrication.
- Incorporation of protectant additives: carboxymethylcellulose sodium salt, polyacrylic acid sodium salt, and lactose.
- Evaluation of enzyme activity and microparticle structure.
Main Results:
- Spray-drying and alginate complexation caused L-lactate dehydrogenase activity loss.
- Protectant additives (especially lactose) significantly prevented enzyme inactivation.
- Polyacrylic acid sodium salt was essential for achieving the desired microparticulate structure for Peyer's patch targeting.
Conclusions:
- Additives are necessary to maintain enzyme activity in alginate microparticles.
- Polyacrylic acid sodium salt is critical for functional microparticle design for intestinal targeting.
- Optimized alginate microparticles show potential for oral delivery of protein and peptide drugs.