泊洛沙姆
黏膜黏附
泊洛沙姆407
离体
自愈水凝胶
体内
药物输送
化学
生物粘附
粘蛋白
Zeta电位
阴道内给药
药理学
生物医学工程
色谱法
生物物理学
材料科学
高分子化学
体外
纳米技术
聚合物
生物化学
纳米颗粒
有机化学
共聚物
医学
外科
阴道
生物技术
生物
作者
Li-qian Ci,Zhigang Huang,Yu Liu,Zhepeng Liu,Gang Wei,Weiyue Lu
标识
DOI:10.1016/j.apsb.2017.03.002
摘要
Lack of mucoadhesive properties is the major drawback to poloxamer 407 (F127)-based in situ hydrogels for mucosal administration. The objective of the present study was to construct a novel mucoadhesive and thermosensitive in situ hydrogel drug delivery system based on an amino-functionalized poloxamer for vaginal administration. First, amino-functionalized poloxamer 407 (F127-NH2) was synthesized and characterized with respect to its micellization behavior and interaction with mucin. Then using acetate gossypol (AG) as model drug, AG-loaded F127-NH2-based in situ hydrogels (NFGs) were evaluated with respect to rheology, drug release, ex vivo vaginal mucosal adhesion, in vivo intravaginal retention and local irritation after vaginal administration to healthy female mice. The results show that F127-NH2 is capable of forming a thermosensitive in situ hydrogel with sustained drug release properties. An interaction between positively charged F127-NH2 and negatively charged mucin was revealed by changes in the particle size and zeta potential of mucin particles as well as an increase in the complex modulus of NFG caused by mucin. Ex vivo and in vivo fluorescence imaging and quantitative analysis of the amount of AG remaining in mouse vaginal lavage all demonstrated greater intravaginal retention of NFG than that of an unmodified F127-based in situ hydrogel. In conclusion, amino group functionalization confers valuable mucoadhesive properties on poloxamer 407.
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