Release behavior and kinetic evaluation of berberine hydrochloride from ethyl cellulose/chitosan microspheres

doi:10.1007/s11706-014-0269-1

Front. Mater. Sci.

2014, Vol. 8

Issue (4) : 373-382 https://doi.org/10.1007/s11706-014-0269-1

RESEARCH ARTICLE

Release behavior and kinetic evaluation of berberine hydrochloride from ethyl cellulose/chitosan microspheres

Hui-Yun ZHOU(

),Pei-Pei CAO,Jie ZHAO,Zhi-Ying WANG,Jun-Bo LI,Fa-Liang ZHANG

Chemical Engineering & Pharmaceutics College, Henan University of Science and Technology, Luoyang 471023, China

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Abstract

Novel ethyl cellulose/chitosan microspheres (ECCMs) were prepared by the method of w/o/w emulsion and solvent evaporation. The microspheres were spherical, adhesive, and aggregated loosely with a size not bigger than 5 μm. The drug loading efficiency of berberine hydrochloride (BH) loaded in microspheres were affected by chitosan (CS) concentration, EC concentration and the volume ratio of V(CS)/V(EC). ECCMs prepared had sustained release efficiency on BH which was changed with different preparation parameters. In addition, the pH value of release media had obvious effect on the release character of ECCMs. The release rate of BH from sample B was only a little more than 30% in diluted hydrochloric acid (dHCl) and that was almost 90% in PBS during 24 h. Furthermore, the drug release data were fitted to different kinetic models to analyze the release kinetics and the mechanism from the microspheres. The released results of BH indicated that ECCMs exhibited non-Fickian diffusion mechanism in dHCl and diffusion-controlled drug release based on Fickian diffusion in PBS. So the ECCMs might be an ideal sustained release system especially in dHCl and the drug release was governed by both diffusion of the drug and dissolution of the polymeric network.

Keywords ethyl cellulose (EC) chitosan (CS) microsphere release in vitro release kinetics

Corresponding Author(s): Hui-Yun ZHOU

Online First Date: 19 November 2014 Issue Date: 04 December 2014

Cite this article:

Hui-Yun ZHOU,Pei-Pei CAO,Jie ZHAO, et al. Release behavior and kinetic evaluation of berberine hydrochloride from ethyl cellulose/chitosan microspheres[J]. Front. Mater. Sci., 2014, 8(4): 373-382.

URL:

https://academic.hep.com.cn/foms/EN/10.1007/s11706-014-0269-1
https://academic.hep.com.cn/foms/EN/Y2014/V8/I4/373

Tab.1 Different preparation conditions and corresponding values of drug loading efficiency (φ_dl) and entrapment efficiency (φ_e) of ECCM

Fig.1 SEM images of ECCMs (×1000): (a) blank microspheres with CS 2.0% (w/v), EC 2.0% (w/v), V(CS)/V(EC) = 1/2; (b) ECCM-loaded BH with CS 2.0% (w/v), EC 2.0% (w/v), V(CS)/V(EC) = 1/2; (c) ECCM-loaded BH with CS 1.0% (w/v), EC 2.0% (w/v), V(CS)/V(EC) = 1/2; (d) ECCM-loaded BH with CS 2.0% (w/v), EC 1.5% (w/v), V(CS)/V(EC) = 1/3.

Fig.2 BH release profile from ECCMs prepared with different CS concentrations (A: 2.0%, w/v; B: 1.5%, w/v; C: 1.0%, w/v) in different release media (date shown were the mean ± SD, n = 3 for each sample): (a) released in PBS; (b) released in dHCl.

Fig.3 BH release profile from ECCMs prepared with different EC concentrations (A: 2.0%, w/v; D: 1.5%, w/v; E: 1.0%, w/v) in different release media (date shown were the mean ± SD, n = 3 for each sample): (a) released in PBS; (b) released in dHCl.

Fig.4 BH release profile from ECCMs prepared with different ratios of V(CS)/V(EC) (D: 1/2; F: 1/1; G: 1/3) in different release medium (date shown were the mean ± SD, n = 3 for each sample): (a) released in PBS; (b) released in dHCl.

Fig.5 Release profiles of BH from ECCMs in different dissolution media: (a) ECCMs A; (b) ECCMs B; (c) ECCMs C.

Fig.6 Kinetics of ECCMs A (prepared with 2.0% (w/v) of c(CS), 2.0% (w/v) of c(EC) and 1/2 of V(CS)/V(EC)) in PBS (pH 6.8) and dHCl (pH 1.0): (a) zero order release kinetics; (b) first order release kinetics; (c) Higuchi kinetics; (d) Peppas kinetics.

Tab.2 Fitting results and relative parameters of in vitro release of BH from ECCMs in different release media

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