Coaxial Electrospinning with Mixed Solvents: From Flat to Round Eudragit L100 Nanofibers for Better Colon‐Targeted Sustained Drug Release Profiles

Deng-Guang Yu,Lin-Ping Du,Zan Li,Xia Wang,Ben-Guo Zhao,Ying Xu

doi:10.1155/2014/967295

Abstract

A modified coaxial electrospinning process was developed for creating drug‐loaded composite nanofibers. Using a mixed solvent of ethanol and N,N‐dimethylacetamide as a sheath fluid, the electrospinning of a codissolving solution of diclofenac sodium (DS) and Eudragit L100 (EL100) could run smoothly and continuously without any clogging. A series of analyses were undertaken to characterize the resultant nanofibers from both the modified coaxial process and a one‐fluid electrospinning in terms of their morphology, physical form of the components, and their functional performance. Compared with those from the one‐fluid electrospinning, the DS‐loaded EL100 fibers from the modified coaxial process were rounder and smoother and possessed higher quality in terms of diameter and distribution with the DS existing in the EL100 matrix in an amorphous state; they also provided a better colon‐targeted sustained drug release profile with a longer release time period. The modified coaxial process not only can smooth the electrospinning process to prevent clogging of spinneret, but also is a useful tool to tailor the shape of electrospun nanofibers and thus endow them improved functions.

Highlights

The physical properties, such as shape, size, mechanical properties, surface texture, and compartmentalization, profoundly impact the function of a nanobiomaterial and raise important questions for the design of its generation [1]
Electrospun nanofibers of some typical pharmaceutical polymers exhibit a flat morphology, which is undesired for providing sustained drug release profiles because the flat morphology aggravates the initial burst release effect and results in a shorter time sustained release [8,9,10]
A modified coaxial electrospinning process in which only an unspinnable mixed solvent system was used as a sheath fluid has been successfully developed to produce medicated Eudragit L100 (EL100) nanofibers

Summary

Introduction

The physical properties, such as shape, size, mechanical properties, surface texture, and compartmentalization, profoundly impact the function of a nanobiomaterial and raise important questions for the design of its generation [1]. Coaxial electrospinning is a power tool for generating core-sheath nanofibers through manipulating two fluids using a concentric spinneret [13, 14]. Different from above-mentioned applications, the modified coaxial electrospinning was exploited as a useful tool for manipulating the shape of resultant nanofibers and improving their functional performance of colon-targeted sustained release. Eudragit L-100 (EL100), a well-known methacrylate-based copolymer developed by the Rohm Company in Germany and a common excipient used in the pharmaceutical field, was exploited as the filament-forming matrix here. It has been widely used for the formulation of different oral dosage forms (e.g., tablet coating, tablet matrix, microspheres, and nanoparticles) for colon-targeted drug delivery [19]. It is taken or applied to reduce inflammation and as an analgesic reducing pain in certain conditions, supplied as or contained in medications under a variety of trade names [20]

Experimental

Results and Discussion

Conclusion