Coaxial Electrospray of Curcumin-Loaded Microparticles for Sustained Drug Release.

Shuai Yuan,Fan Lei,Qingping Tong,Zhongfa Liu,Ronald X Xu,Ting Si,Monica M Jablonski

doi:10.1371/journal.pone.0132609

Abstract

Curcumin exhibits superior anti-inflammatory, antiseptic and analgesic activities without significant side effects. However, clinical dissemination of this natural medicine is limited by its low solubility and poor bio-availability. To overcome this limitation, we propose to encapsulate curcumin in poly(lactic-co-glycolic acid) (PLGA) microparticles (MPs) by an improved coaxial electrospray (CES) process. This process is able to generate a stable cone-jet mode in a wide range of operation parameters in order to produce curcumin-loaded PLGA MPs with a clear core-shell structure and a designated size of several micrometers. In order to optimize the process outcome, the effects of primary operation parameters such as the applied electric voltages and the liquid flow rates are studied systemically. In vitro drug release experiments are also carried out for the CES-produced MPs in comparison with those by a single axial electrospray process. Our experimental results show that the CES process can be effectively controlled to encapsulate drugs of low aqueous solubility for high encapsulation efficiency and optimal drug release profiles.

Highlights

Curcumin (diferuloylmethane, 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5dione) is a yellow pigment derived from the Curcuma longa plant [1,2]
This paper reports our recent effort of optimizing the coaxial electrospray (CES) process parameters to encapsulate curcumin in poly(lactic-co-glycolic acid) (PLGA) MPs for the high encapsulation rate and the improved drug release profile
We have previously studied the different flow modes of a CES process affected by the process parameters, such as the applied electrical voltages [19]

Summary

Introduction

Curcumin (diferuloylmethane, 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5dione) is a yellow pigment derived from the Curcuma longa plant [1,2]. It was first isolated in 1815 and its chemical structure was first determined in 1910. In order to overcome the above limitations and to enhance the bio-availability of curcumin, many formulation techniques and carrier materials have been explored [5,6,7]. Poly(lactic-co-glycolic acid) (PLGA) microparticles and nanoparticles provide a biodegradable carrier platform for sustained release of curcumin with improved bio-availability [7,8]

Methods

Results

Conclusion