Preparation, characterization, and cellular uptake of resveratrol-loaded trimethyl chitosan nanoparticles
The aim of the study was to encapsulate resveratrol (RV) in trimethyl chitosan (TMC) nanoparticles cross-linked with tripolyphosphate (TPP) and/or alginate to achieve controlled release and improved cellular uptake. TMC (degree of quaternization of 78%) was prepared by reacting purified chitosan with iodomethane. Three types of RV-loaded TMC nanoparticles were prepared: TMC–TPP (TP-NPs), TMC–alginate (TA-NPs), and TMC–alginate–TPP (TAP-NPs). TA-NPs and TAP-NPs showed lower particle size and encapsulation efficiency (EE), better distribution, and more sustained release than TP-NPs due to the high molecular weight and viscous property of alginate. Caco-2 cellular uptake of RV was improved by TMC nanoencapsulation, and TP-NPs showed the highest uptake due to its significantly higher EE. Compared with TAP-NPs, TA-NPs with higher positive surface charge showed higher cellular uptake. Moreover, Caco-2 cell growth-inhibiting activity of RV was significantly increased by TMC nanoencapsulation and TP-NPs showed the significantly highest activity with a good agreement with the permeability results.
KeywordsTrimethyl chitosan Nanoencapsulation Controlled release Cellular uptake Cytotoxicity
This research was supported by the Basic Science Research Program through the National Research Foundation of Korea (NRF), which is funded by the Ministry of Science, ICT, & Future Planning (No. 2014M3A7B4051898).
- 23.Sadeghi A, Dorkoosh F, Avadi M, Weinhold M, Bayat A, Delie F, Gurny R, Larijani B, Rafiee-Tehrani M, Junginger H. Permeation enhancer effect of chitosan and chitosan derivatives: comparison of formulations as soluble polymers and nanoparticulate systems on insulin absorption in Caco-2 cells. Eur. J. Pharm. Biopharm. 70:270–278 (2008)CrossRefGoogle Scholar