Construction and evaluation of SAK-HV protein oral dosage form based on chitosan quaternary ammonium salt-PLGA microsphere
Construction and evaluation of SAK-HV protein oral dosage form based on chitosan quaternary ammonium salt-PLGA microsphere
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DOI：
10.1080/1061186x.2019.1605520
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发表时间：
2019-05
影响因子：
4.5
通讯作者：
Shiming He;Wenliang Fu;M. Zou;Wei-wei Xing;Zhongcheng Liu;Donggang Xu
中科院分区：
文献类型：
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作者：
Shiming He;Wenliang Fu;M. Zou;Wei-wei Xing;Zhongcheng Liu;Donggang Xu
摘要本研究旨在以壳聚糖季铵盐-PLGA微球为载体，实现SAK-HV蛋白的口服给药，提高其口服生物利用度。结果表明，SAK-HV微球可以克服口服吸收的多重障碍，并有效地黏附在大鼠空肠段上。大鼠口服载药微球的药动学分析表明，口服后4 h血药浓度达到峰值，相对生物利用度为3.4%。小鼠口服SAK-HV后，第21天产生的SAK-HV抗体水平高于对照组和注射组，抗体滴度是尾静脉注射组的7.2倍。本工作表明壳聚糖季铵盐-PLGA微球有望成为SAK-HV蛋白的口服给药系统。
Abstract The aim of this study was to realize the oral delivery of SAK-HV protein and improve its oral bioavailability based on chitosan quaternary ammonium salt-PLGA microsphere. The results showed that the SAK-HV-loaded microsphere can overcome the multiple obstacles for oral adsorption and adhere effectively to the jejunal segment of a rat. The pharmacokinetic analysis of the oral drug-loaded microspheres in rats showed that the blood drug concentration of SAK-HV reached the peak value at 4 h after oral administration, and the relative oral bioavailability of SAK-HV was 3.4%. Additionally, after oral administration to the mice, a higher level of antibody against SAK-HV was produced on day 21 compared with that in the control and injection groups, and the antibody titre was 7.2 times that of the tail vein group. This work suggests that the microsphere of the chitosan quaternary ammonium salt-PLGA may be a promising drug delivery system for the oral administration of SAK-HV protein.