Preparation and Characterization of Nicotine/Ca-alginate Composite Microcapsules for the Enteric Controlled Drug Release

用於腸道藥物控釋之尼古丁／藻酸鈣微粒膠囊的製備與特性研究

陳素容(Su-Jong Chen) ； 陳秋蘭(Chiu-Lan Chen) ； 林恆弘(Hung-Hong Lin)

《嘉南學報（科技類）》 38期 (2012/12) Pp. 21-29

https://doi.org/10.29540/CNABST.201212.0004

摘要

The aim of the present study was to develop drug-loaded microcapsules to increase drug bioavailability at target site especially for colon-targeted oral delivery. Nicotine was selected as a model lipophilic drug. Additives such as gelatin, glycerin and PEG 6000 were added into Ca-alginate composite to prepare microcapsules by using a modification of the emulsion technique. The effect of additives on process yield, encapsulation efficiency, physical-chemical properties of microcapsules as well as drug release was investigated. The results show that a mean particle size ranging from 40 μm to 500 μm was obtained and nicotine-loaded microcapsules were spherical in shape. The preparing condition would affect particle size but not additives added. Encapsulation efficiency of microcapsules is well relative to the particle size. The FTIR spectra of microcapsules indicated that the chemical interaction does not occur among the components of nicotine-loaded microcapsules. The effect of additives on retarding release of drug from microcapsules in pH 1.2 medium conformed to the following order: PEG 6000 ＞ glycerin ＞ gelatin. At pH 7.4, the degree of swelling increased dramatically even degradation that cause accelerated drug release. The properties of the microcapsules are suitable for bowel disease targeting. To get more control over the drug delivery the current composite of microcapsules could be improved by increasing alginate content and adding additives such as PEG 6000 or glycerin.

關鍵字

尼古丁 ； 藻酸鈣 ； 微粒膠囊 ； 腸道 ； 控制釋放

並列摘要

The aim of the present study was to develop drug-loaded microcapsules to increase drug bioavailability at target site especially for colon-targeted oral delivery. Nicotine was selected as a model lipophilic drug. Additives such as gelatin, glycerin and PEG 6000 were added into Ca-alginate composite to prepare microcapsules by using a modification of the emulsion technique. The effect of additives on process yield, encapsulation efficiency, physical-chemical properties of microcapsules as well as drug release was investigated. The results show that a mean particle size ranging from 40 μm to 500 μm was obtained and nicotine-loaded microcapsules were spherical in shape. The preparing condition would affect particle size but not additives added. Encapsulation efficiency of microcapsules is well relative to the particle size. The FTIR spectra of microcapsules indicated that the chemical interaction does not occur among the components of nicotine-loaded microcapsules. The effect of additives on retarding release of drug from microcapsules in pH 1.2 medium conformed to the following order: PEG 6000 ＞ glycerin ＞ gelatin. At pH 7.4, the degree of swelling increased dramatically even degradation that cause accelerated drug release. The properties of the microcapsules are suitable for bowel disease targeting. To get more control over the drug delivery the current composite of microcapsules could be improved by increasing alginate content and adding additives such as PEG 6000 or glycerin.

並列關鍵字

Nicotine ； Ca-alginate ； Microcapsules ； Enteric ； Controlled release