Tropical Journal of Pharmaceutical Research

Original Research Article | OPEN ACCESS

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

Jian-Li Liu^1,2, Jie Li³, Ling-Yan Zhang², Pei-Li Zhang², Jun-Lin Zhou², Bin Liu^1,3

¹The School of Nuclear Science and Technology, Lanzhou University, Lanzhou 730000; ²Department of Radiology, Lanzhou University Second Hospital, Lanzhou; ³School of Stomatology, Lanzhou University, Lanzhou 730000, China.

For correspondence:- Bin Liu Email: liubin244@hotmail.com Tel:+869318913551

Received: 9 March 2017 Accepted: 21 July 2017 Published: 31 August 2017

Citation: Liu J, Li J, Zhang L, Zhang P, Zhou J, Liu B. Preparation of N, N, N-trimethyl chitosan-functionalized retinoic acid-loaded lipid nanoparticles for enhanced drug delivery to glioblastoma. Trop J Pharm Res 2017; 16(8):1765-1772 doi: 10.4314/tjpr.v16i8.3

© 2017 The authors.
This is an Open Access article that uses a funding model which does not charge readers or their institutions for access and distributed under the terms of the Creative Commons Attribution License (http://creativecommons.org/licenses/by/4.0) and the Budapest Open Access Initiative (http://www.budapestopenaccessinitiative.org/read), which permit unrestricted use, distribution, and reproduction in any medium, provided the original work is properly credited..

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