Chitosan/PLGA Particles for Controlled Release of α-Tocopherol in The GI Tract Via Oral Administration

Abstract

Aim: The physiochemical properties, controlled release characteristics, stability and cellular uptake of chitosan (Chi)/poly(D,L-lactide-co-glycolide) (PGLA) and PLGA particles with entrapped α-tocopherol were investigated to understand the behavior of these nanoparticles in the GI tract. Materials & Methods: Chi/PLGA and PLGA particles stabilized by lecithin were synthesized and fully characterized for oral gastrointestinal delivery via transmission electron microscopy, dynamic light scattering, high-performance liquid chromatography and fluorescence microscopy. Results: Particle stability was pH- and system-dependent. In vitro release profiles showed a higher percentage of drug released in the intestinal domain by Chi/PLGA as opposed to the PLGA nanoparticles. Fluorescent counterparts of these particles were confirmed to associate with the surface of the intestinal villi, and penetrate deep in the endothelial lining of rabbit intestinal explants, indicating uptake. Conclusion:In vitro and ex vivo results showed that PLGA and Chi/PLGA nanoparticles were efficiently taken up by the GI tract and could be optimized to deliver αtocopherol to the intestine and improve its bioavailability.

Keywords::

• α-tocopherol
• chitosan
• GI tract
• in vitro
• lecithin
• PLGA

Financial & competing interests disclosure

This work was funded by the USDA-NRI 75.0 Nanoscale Science and Engineering for Agriculture and Food Systems (Award # 2009-35603-05055). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Ethical conduct of research

The authors state that they have obtained appropriate institutional review board approval or have followed the principles outlined in the Declaration of Helsinki for all human or animal experimental investigations. In addition, for investigations involving human subjects, informed consent has been obtained from the participants involved.

Acknowledgements

The authors would like to thank undergraduate student Rebecca Adams for assistance with data collection.

Additional information

Funding

This work was funded by the USDA-NRI 75.0 Nanoscale Science and Engineering for Agriculture and Food Systems (Award # 2009-35603-05055). The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.