Abstract

Albendazole (ABZ) is an antihelminthic drug used for the treatment of several parasitic infestations. In addition to this, there are reports on the anticancer activity of ABZ against a wide range of cancer types. However, its effect on glioma has not yet been reported. In the present study, cytotoxicity of ABZ and ABZ loaded solid lipid nanoparticles (ASLNs) was tested in human glioma/astrocytoma cell line (U-87 MG). Using glyceryl trimyristate as lipid carrier and tween 80 as surfactant spherical ASLNs with an average size of 218.4 ± 5.1 nm were prepared by a combination of high shear homogenization and probe sonication methods. A biphasic in vitro release pattern of ABZ from ASLNs was observed, where 82% of ABZ was released in 24 h. In vitro cell line studies have shown that ABZ in the form of ASLNs was more cytotoxic (IC50 = 4.90 µg/mL) to U-87 MG cells compared to ABZ in the free form (IC50 = 13.30 µg/mL) due to the efficient uptake of the former by these cells.

Highlights

  • Development of new drugs with increased activity against cancer cells is the major focus of the pharmaceutical industry

  • While the initial initial burst burst release release might might be due to the free drug the medium respectively adhered to the surface of ABZ loaded solid lipid nanoparticles (ASLNs), the later sustained release could be attributed to the slow release of ABZ encapsulated within the ASLNs

  • These results clearly show thatcytotoxicity the enhanced cytotoxicity of in cells compared to assay is due to the efficient uptake of observed in U-87 MG cells compared to ABZ in the MTT assay is due to the efficient uptake of ASLNs

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Summary

Introduction

Development of new drugs with increased activity against cancer cells is the major focus of the pharmaceutical industry. ABZ as and lipidsuspension nanocapsules approaches such as particle size reduction, complexation, enhanced the oral bioavailability and efficacy of cystic echinococcosis therapy in experimentally have been investigated [6,7]. Tumor cells could efficiently uptake SLNs. The and challenges by glioma and the aforementioned and incidence thereby systemic toxicity ofposed the drug could be minimized [16]. The and challenges by glioma and the aforementioned and incidence thereby systemic toxicity ofposed the drug could be minimized [16] All theadvantages more, they of areSLNs biodegradable, and economically motivated us to testnontoxic the cytotoxicity of ABZ both viable in the [17,18,19,20]. That the delivery of ABZ in the form of SLNs was cytotoxic to U-87 MG cells due to their efficient uptakeand by these cells

Results and Discussion
Particle
Graph the cytotoxic potentialofof control and inBSLNs against
Methods
Chemicals and Reagents
Preparation of SLNs
Morphological Characterization
Entrapment Efficiency of ASLNs
In Vitro Drug Release
In Vitro Cellular Uptake
Cytotoxicity of Nanoparticles
3.10. Statistical Analyses of Data
Conclusions
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