Abstract

Objective: The aim of this experiment was to develop ellagic acid (EA) loaded poly (D,L-lactide-co-glycolide) (PLGA) nanoparticles for tumour-specific drug delivery. The phytochemical EA is a potential antioxidant, anticarcinogenic and antimutagenic. Due to its low solubility and permeability, it falls under class IV of the BCS classification.
 Methods: PLGA nanoparticles were prepared by a method established on the concept of single emulsification–solvent evaporation by using TWEEN®20 as a cosolvent for solubilizing the drug. While developing this method, polyvinyl alcohol (PVA), was implemented. 
 Results: The stabilized formulation was with a particle size of 174.2 nm, which is ideal for tumour accumulation. The SEM images confirmed that the NPs have spherical shape. The resulting NPs were predominantly spherical and of uniform size and shape. Initial release of EA from nanoparticles in pH 7.4 phosphate buffer was quick, followed by a steady sustained release. The in vitro cytotoxicity study using MTT was also performed on the human breast cancer, MCF-7 cell line and EA-NPs were found to successively reduce the IC50 values which thereby revealed the pronounced cytotoxic effect of the formulation. 
 Conclusion: After performing this experiment, we can conclude that the polymeric nanoparticles are efficient and suitable form of drug delivery of ellagic acid exhibiting potential anti-tumour activity.

Highlights

  • Nanoparticles are coherent drug delivery systems for enhancing the bioavailability of poorly water-soluble drugs

  • The solution of ellagic acid (EA) and PLGA in acetone was sonicated for emulsification into an aqueous phase containing polyvinyl alcohol (PVA) as surfactant

  • The encapsulation efficiencies achieved with this method are very good considering the poor solubility profile of EA

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Summary

Introduction

Nanoparticles are coherent drug delivery systems for enhancing the bioavailability of poorly water-soluble drugs. There are several approaches to enhance drug bioavailability. Among these approaches, nano-encapsulation using PLGA (Polylactic-co-glycolic acid), which is a biocompatible polymeric nanocarrier, is a very favourable one. PLGA is a very well-known biodegradable and biocompatible polymer consented by the US Food and Drug Administration (FDA) and the European Medicine Agency (EMA). It has been used in a variety of biomedical devices and tissue engineering branches. PLGA-NPs bind drugs with poor solubility and extravasation through the tumour vasculature by the enhanced permeability and retention effect. Entrapment efficiency, in vitro release profile and in vitro cytotoxicity assay using MTT on the human breast cancer cell line, MCF-7 [2]

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Conclusion

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