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Polymeric Lids for Microcontainers for Oral Protein Delivery
Chiara Mazzoni1, Rasmus Due Jacobsen1, Jacob Mortensen1
1Department of Health Technology, Technical University of Denmark, Ørsteds Plads 345C, Kgs. Lyngby, 2800, Denmark.
Macromolecular Bioscience
|April 3, 2019
Summary
Developing novel polymeric microcontainers for oral protein delivery. Functionalized with chitosan or PEG, these microdevices enhance mucoadhesion and offer tunable release, overcoming key pharmaceutical challenges.
Area of Science:
- Pharmaceutical Drug Development
- Biomaterials Science
- Nanotechnology
Background:
- Oral delivery of proteins and peptides faces significant challenges due to degradation.
- Polymeric microcontainers offer a protective strategy for therapeutics.
- Lysozyme was selected as a model protein for this study.
Purpose of the Study:
- To develop and characterize functionalized polymeric microcontainers for oral protein delivery.
- To evaluate the impact of different polymeric coatings on drug release and mucoadhesion.
- To assess the in vitro and ex vivo performance of these microcontainers.
Main Methods:
- Loading lysozyme and sodium decanoate into microcontainers.
- Functionalizing microcontainers with poly(lactic-co-glycolic) acid (PLGA) combined with polyethylene glycol (PEG) or chitosan.
- In vitro evaluation of morphology, drug release, and mucoadhesive properties.
- In vitro and ex vivo studies using cell cultures and porcine intestinal tissue.
Main Results:
- PLGA+chitosan coatings exhibited slower drug release compared to PLGA+PEG or uncoated PLGA.
- Chitosan or PEG coatings significantly enhanced ex vivo mucoadhesion (threefold increase).
- No enhancement in lysozyme transport across cell cultures was observed compared to bulk powder.
Conclusions:
- Functionalized microcontainers with mucoadhesive properties were successfully developed for oral protein delivery.
- Tunable release profiles can be achieved through specific polymeric functionalization.
- These microcontainers show promise for improving oral peptide and protein therapeutics.
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