Promising synthesized bis (arylmethylidene) acetone -polymeric PCL emulsified nanoparticles with enhanced antimicrobial/antioxidant efficacy: in-vitro and in-vivo evaluation

Abstract

Introduction

Recently, bis(arylmethylidene)acetone drugs known as C5-curcumin, were acknowledged for their potent biological effects as a neoteric synthetic alternative to curcumin effectively used to treat many diseases.

Methods

In this study, new polymeric emulsified nanoparticles (PENS) carrying biodegradable polycaprolactone (PCL) polymer moieties within their framework were developed as promising carriers for a modern synthesized bis(arylmethylidene)acetone “(1E,4E)-1,5-di(thiophen-2-yl) penta-1,4dien-3-one” (TPO) with improved bioavailability. Such systems were evaluated by studying their; encapsulation efficiency, release behavior, physicochemical evaluations, TEM and SEM measurements and cytotoxicity, besides the in-vitro and in-vivo biological studies screening.

Results

The results revealed high encapsulation efficiency ranging between 99.31± 2.15 and 99.55 ± 2.03 %, and a sustained release behavior for up to 24 h with nanosized particle size. TPO emulsified nanoparticles (TPO-ENPs) showed effective antimicrobial activity against Candida albicans and Aspergillus brasiliensis as well as antioxidant efficacy with a higher scavenging activity of 177.6μg TE/ mg against free radicals of 2,2-diphenyl-1-picrylhydrazyl hydrate (DPPH) relatively to the control drug. F1’ and F2’ TPO-ENPs were safe on Vero-cells and proved a significant reduction of hepatocellular alterations and serum ALT levels in control groups.

Conclusion

In conclusion, these novel synthesized TPO-ENPs showed pronounced efficacy as antimicrobial/ antioxidant/ anti-inflammatory/ analgesic/ hepatoprotective therapeutic vehicles.