Abstract
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
Highlights
Glioblastoma is a harmful and often fatal brain malignancy, with approximately 23, 000 cases diagnosed in adults in the US each year [1,2]
After the trimethyl chitosan (TMC) coating was applied to the surface of solid lipid nanoparticles (SLNs), the particle size was increased to 214 ± 3.45 nm and the polydispersity index (PDI)
The surface-modified TR-SLNs exerted an in vitro anti-tumor inhibitory effect of 48.2 ± 2.84 % at 10 μg/mL and 32.4 ± 3.5 % at 25 μg/mL, which was higher than those observed with free drug and Retinoic acid-loaded solid lipid nanoparticles (R-SLNs) at all tested concentrations (p < 0.01)
Summary
Glioblastoma is a harmful and often fatal brain malignancy, with approximately 23, 000 cases diagnosed in adults in the US each year [1,2]. Glioblastoma is regarded as a Grade IV tumor by the World Health Organization (WHO) [3,4]. Lipid-based carriers are within the submicron range in size (i.e., 100–300 nm); we developed a lipid-based carrier to deliver molecular therapeutics across the BBB to tumors [6,7]. Solid lipid nanoparticles (SLNs) have a solid lipid core that can effectively incorporate hydrophobic drugs. Lipid nanoparticles are non-toxic and biocompatible, with a good loading capacity, resulting in increased solubility and stability of the loaded drugs; sustained delivery of hydrophobic drugs using lipid nanoparticles has been reported [8,9]. We designed surface-modified SLNs, which have been used as a system to successfully deliver drugs across the BBB to tumor tissues with high specificity [10]
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