Tropical Journal of Pharmaceutical Research

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Preparation of N, N, N-trimethyl chitosan-functionalized retinoic acid-loaded lipid nanoparticles for enhanced drug delivery to glioblastoma

Jian-Li Liu, Jie Li, Ling-Yan Zhang, Pei-Li Zhang, Jun-Lin Zhou, Bin Liu


Purpose: To formulate trimethyl chitosan-functionalized retinoic acid-encapsulated solid lipid nanoparticles for the effective treatment of glioma.

Methods: Retinoic acid-loaded solid lipid nanoparticles (R-SLNs) were prepared using homogenization followed by sonication. R-SLN surfaces were functionalized electrostatically with trimethyl chitosan as a nanocarrier (TR-SLNs) with enhanced anti-cancer activity. They were evaluated by dynamic light scattering (DLS), scanning electron microscopy, in vitro drug release, and cell cytotoxicity and apoptosis studies.

Results: Morphological images showed spherical and uniformly dispersed nanoparticles. A sustained monophasic release pattern was observed throughout the study period. Furthermore, the anti-cancer effect of TR-SLNs was demonstrated by increased cell killing activity compared with the free drug (p < 0.01); negligible cytotoxicity was observed with blank carriers. Apoptosis assay showed increased cell populations in early/late apoptotic and necrotic phases.

Conclusion: This study showed the potential application of surface-modified solid lipid nanoparticles for the effective treatment of brain cancer.

Keywords: Lipid nanoparticles, Trimethyl chitosan, Retinoic acid, Glioma, Anti-cancer, Cytotoxicity, Apoptosis
AJOL African Journals Online