Targeted delivery of mesoporous silica nanoparticles loaded monastrol into cancer cells: an in vitro study

Huzaifa Hanif,Shazia Bano,Samina Nazir,Muhammad Waseem,Kehkashan Mazhar,Umer Rashid

doi:10.1007/s13204-017-0593-8

Abstract

Monastrol is a simple low molecular weight dihydropyrimidine-based kinesin Eg5 inhibitor. Its low cellular activity and its non-drug-like properties have impeded its further development. In a previous report, we have reported various topological parameters to improve the pharmacokinetic properties of monastrol. The purpose of this study is to determine the loading and release feasibility of poorly water-soluble monastrol into the synthesized mesoporous silica nanoparticles (MSNs). The synthesis of MSNs was attained by the ammonia-catalysed hydrolysis and condensation of TEOS in ethanol using polysorbate-80 as surfactant. These were characterized by BET surface area and pore size distribution analyses, SEM, XRD, UV and FTIR spectroscopy. The synthesized monastrol was successfully loaded on MSNPs and coated by hydrogels for successful controlled drug delivery. In vitro release studies are done by simple dialysis method. Monastrol-loaded MSNPs were tested on human cervical epithelial malignant carcinoma (HeLa) cell lines for studying their anticancer activity. Our presented system described a reliable method for targeted delivery of monastrol into the cancer cells in vitro.

Highlights

Monastrol is a simple low molecular weight dihydropyrimidine-based kinesin Eg5 inhibitor
The surface area and pore size distribution studies of mesoporous silica nanoparticles (MSNPs) were performed by N2 adsorption method at 77 K by means of surface area analyser model Quantachrome NOVA 1200e
From the above-mentioned study, it can be concluded that the mesoporous silica nanoparticles were successfully synthesized by sol–gel method

Summary

Introduction

Monastrol is a simple low molecular weight dihydropyrimidine-based kinesin Eg5 inhibitor. The purpose of this study is to determine the loading and release feasibility of poorly water-soluble monastrol into the synthesized mesoporous silica nanoparticles (MSNs). Low solubility in aqueous media is shown by the hydrophobic anticancer drugs like monastrol. Their inability to dissolve readily affects their activity in cancer treatment. For the effective drug loading and its delivery to the targeted sites, MSNPs are selective to capture bigger bioactive molecules in substantial amount (Jong and Borm 2008; Jaganathana and Godin 2012). Further development of monastrol was halted due to its weak inhibitory activity as kinesin Eg5 inhibitor and non-drug-like properties (Schmidt and Bastians 2007)

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Conclusion