Synthesis of Eudragit® L100-coated chitosan-based nanoparticles for oral enoxaparin delivery

Enoxaparin is an effective biological molecule for prevention and treatment of coagulation disorders. However, it is poorly absorbed in the gastrointestinal tract. In this study, we developed an Eudragit® L100 coated chitosan core shell nanoparticles for enoxaparin oral delivery (Eud/CS/Enox NPs) through a completely eco-friendly method without employing any high-energy homogenizer technique and any organic solvents.

Spherical nanocarriers were successfully prepared with particle size lower than 300 nm, polydispersity index about 0.12 and zeta potential higher than +25 mV, entrapment efficiency greater than 95% and the in vitro release behavior confirms the good colloidal stability and the successful Eudragit® L100 coating process demonstrated by negligible cumulative enoxaparin release (<10%) when the particles are submitted to simulated gastric fluid conditions.

Finally, we demonstrated that the core-shell structure of the particle influenced the drug release mechanism of the formulations, indicating the presence of the Eudragit® L100 on the surface of the particles. These results suggested that enteric-coating approach and drug delivery nanotechnology can be successfully explored as potential tools for oral delivery of enoxaparin.

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Article information: Yuri Basilio Gomes Patriota, Igor Eduardo Silva Arruda, Antônia Carla de Jesus Oliveira, Thaisa Cardoso de Oliveira, Eliadna de Lemos Vasconcelos Silva, Luíse Lopes Chaves, Fábio de Oliveira Silva Ribeiro, Durcilene Alves da Silva, Mônica Felts de La Roca Soares, José Lamartine Soares-Sobrinho, Synthesis of Eudragit® L100-coated chitosan-based nanoparticles for oral enoxaparin delivery, International Journal of Biological Macromolecules, Volume 193, Part A, 2021. https://doi.org/10.1016/j.ijbiomac.2021.10.111.