Antitumoral Drug-Loaded Biocompatible Polymeric Nanoparticles Obtained by Non-Aqueous Emulsion Polymerization.

Oana Maria Daraba,Gabriela Vochita,Leonard Ionut Atanase,Delia Mihaela Rata,Anca Niculina Cadinoiu

doi:10.3390/polym12051018

Abstract

Non-aqueous dispersions (NAD) with two types of polymeric nanoparticles (NPs), such as hydrophobic poly(ε-caprolactone) (PCL) and hydrophilic cross-linked poly(vinylpyrrolidone) (PNVP), were synthesized in the present study starting from monomer-in-silicone oil (PDMS) polymerizable non-aqueous emulsions stabilized with the same tailor-made PDMS-based block copolymer. These NPs were loaded with CCisplatin, an antitumoral model drug, directly from the emulsion polymerization step, and it was observed that the presence of the drug leads only to a slight increase of the NPs size, from 120 to 150 nm. The drug release kinetics was evaluated at 37 °C in phosphate buffer at pH = 7.4 and it appeared that the drug release rate from the hydrophilic cross-linked PNVP-based NPs is higher than that from the hydrophobic PCL-based NPs. Moreover, haemolysis tests revealed the fact that these two types of NPs have a good compatibility with the blood. Furthermore, for both the free and drug-loaded NPs, the in vitro cytotoxicity and apoptosis was studied on two types of cancer cell lines, such as MCF-7 (breast cancer cell line) and A-375 (skin cancer cell line). Both types of NPs had no cytotoxic effect but, at a concentration of 500 μg/mL, presented an apoptotic effect similar to that of the free drug.

Highlights

Controlled drug delivery (CDD) has become one of the important research areas in polymeric biomaterials during the past few years [1,2,3,4,5]
A series of drug-loaded non-aqueous dispersions, based on PCL and PNVP nanoparticles, were different cell populations is similar to that of the control obtained starting from polymerizable non-aqueous monomer-in-silicone oil emulsions stabilized with in the case of samples without encapsulated drug NPs1 and NPs5
The increasing of the concentration at 500 μg/mL has as consequence the reduction in Cisplatin, an antitumoral model drug, directly in the polymerization step, and it was observed that the cell viability which was evidenced by the increase in the number of dead cells

Summary

Introduction

Controlled drug delivery (CDD) has become one of the important research areas in polymeric biomaterials during the past few years [1,2,3,4,5] Such delivery systems offer numerous advantages compared to conventional dosage forms including improved efficiency, reduced toxicity, and increased patient compliance [3,4]. In this respect, a wide range of drug-loaded nanoparticles, with diameters between 10 and 1000 nm, have been used as CDD systems and their advantages over the microparticles are well highlighted [6,7]. The drug release rate from these biodegradable polymeric NPs is controlled by the biodegradation kinetics of the polymers, the physicochemical properties of the polymers and drugs, the thermodynamic compatibility between the polymers and drugs.

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Conclusion