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具有泵送控释性能的肠靶向Janus型双腔室海藻酸钙基微胶囊
Shuang Wen, Xiaojie Ju, Wenying Liu, Yuqiong Liu, Xingqun Pu, Zhuang Liu, Wei Wang, Rui Xie, Yousef Faraj, Liangyin Chu
工程（英文） ›› 2023, Vol. 24 ›› Issue (5) : 114-125.
PDF(3549 KB)
PDF(3549 KB)
具有泵送控释性能的肠靶向Janus型双腔室海藻酸钙基微胶囊
Ca-Alginate-Based Janus Capsules with a Pumping Effect for Intestinal-Targeted Controlled Release
本文成功开发了一种具有泵送控释特性的θ形双腔室肠靶向海藻酸钙基微胶囊，囊壁为海藻酸钙-壳聚糖/精蛋白/二氧化硅（ACPSi）复合壳，为封装的药物在胃环境中提供了良好保护，实现药物的肠靶向释放。该θ形微胶囊由含药室和助推室两个腔室组成：含药室负载疏水药物吲哚美辛，其囊壁内嵌肠溶性
羟丙甲基纤维素邻苯二甲酸酯（HPMCP）微球，作为“微阀门”（micro-valves）；助推室包封助推剂聚丙烯酸（PAA），在肠液环境中，PAA发生溶胀，可提高吲哚美辛释放速率。结果显示，载药的θ-ACPSi 微胶囊在模拟胃液（pH值为2.5）中，吲哚美辛的释放率小于1%。然而，进入模拟肠液（pH值为6.8）时，含药室囊壁中的HPMCP微球溶解，释药“微通道”（microchannel）被打开，同时助推室中的PAA发生溶胀，为药物的释放提供推动力。结果，吲哚美辛在小肠中以恒定的速度释放60%以上。因此，该θ-ACPSi 微胶囊具有良好的泵送和肠靶向控释性能，为口服肠道靶向给药系统的开发提供了一种新策略。
A novel intestinal-targeted θ-shaped capsule with a pumping effect for the controlled release of hydrophobic drugs is successfully developed. The proposed capsule is composed of a Ca-alginate–chitosan/protamine/silica (ACPSi) composite shell and two chambers forming an θ-shape (θ-ACPSi), which respectively encapsulate drugs and booster agents. Enteric hydroxypropyl methylcellulose phthalate (HPMCP) microspheres are embedded into the drug chamber shell. The θ-ACPSi composite shell offers improved protection for the encapsulated drug in the stomach environment and excellent intestinal-targeted drug release. Using indomethacin as the model drug and polyacrylic acid (PAA) as the booster agent, both the opening of ″microchannels″ in the drug chamber and the swelling of PAA in the booster chamber increase the release rate of high-concentration indomethacin and ensure a constant release of indomethacin in the small intestine. In the stomach (pH 2.5), less than 1% of the indomethacin is released. However, when the θ-ACPSi capsules enter the small intestine (pH 6.8), the HPMCP microspheres in the drug chamber shell dissolve to open the ″microchannels,″ while the PAA swells to provide pumping impetus. As a result, more than 60% of the indomethacin is released at a constant speed in the small intestine. The proposed θ-ACPSi capsules provide a potential and novel model for developing responsive pumping controlled-release systems and intestinal-targeted drug delivery systems.
微胶囊 / 海藻酸钙 / 肠靶向递送 / 泵送性能 / 控制释放
Capsules / Ca-alginate / Intestinal-targeted delivery / Pumping effects / Controlled release
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