基于壳聚糖-g-聚（NiPAam）两亲性嵌段共聚物胶束离子交联的黏附性纳米凝胶作为新型药物纳米载体。
Mucoadhesive nanogels by ionotropic crosslinking of chitosan-g-oligo(NiPAam) polymeric micelles as novel drug nanocarriers.
机构信息
Laboratory of Pharmaceutical Nanomaterials Science, Department of Materials Science & Engineering, Technion-Israel Institute of Technology, Haifa, Israel.
Russell Berrie Nanotechnology Institute (RBNI), Technion-Israel Institute of Technology, Technion City, Haifa, Israel.
出版信息
Nanomedicine (Lond). 2016 Feb;11(3):217-33. doi: 10.2217/nnm.15.191. Epub 2016 Jan 20.
AIM
To investigate a novel kind of mucoadhesive nanogel based on the supramolecular aggregation of chitosan-g-oligo(N-isopropylacrylamide) copolymers.
MATERIALS & METHODS: Copolymers were synthesized by the graft-free radical polymerization of N-isopropylacrylamide on chitosan. The aggregation was studied by dynamic light scattering and nanoparticle tracking analysis (NTA), the nanostructure by transmission electron microscopy(TEM)/cryo-TEM, the mucoadhesiveness in vitro with mucin and the cytocompatibility in Caco2 cells.
RESULTS
Copolymers (36-74% w/w N-isopropylacrylamide content) showed critical micellar concentration between 2.0 and 40.0 × 10(-3)% w/v and micelles were nanometric and positively charged. Physical stabilization was achieved with ionotropic crosslinking. TEM/cryo-TEM revealed multimicellar aggregates with good mucoadhesion and cytocompatibility properties. Micellar systems (1-10% w/v) increased the solubility of efavirenz up to 1249-fold.
CONCLUSION
Results support the potential of these nano-drug delivery systems for improved mucosal administration of hydrophobic drugs.
目的
研究一种基于壳聚糖-g-聚（N-异丙基丙烯酰胺）共聚物超分子聚集的新型黏膜黏附纳米凝胶。
材料与方法
通过无自由基聚合将 N-异丙基丙烯酰胺接枝到壳聚糖上合成共聚物。通过动态光散射和纳米颗粒跟踪分析（NTA）研究聚集情况，通过透射电子显微镜（TEM）/冷冻透射电子显微镜（cryo-TEM）研究纳米结构，通过黏蛋白体外黏附研究黏膜黏附性，通过 Caco2 细胞研究细胞相容性。
结果
共聚物（N-异丙基丙烯酰胺含量 36-74%w/w）表现出 2.0 到 40.0×10(-3)%w/v 之间的临界胶束浓度，胶束为纳米级且带正电荷。通过离子交联实现物理稳定。TEM/cryo-TEM 显示出具有良好黏膜黏附性和细胞相容性的多胶束聚集物。胶束系统（1-10%w/v）将依非韦伦的溶解度提高了 1249 倍。
结论
这些结果支持这些纳米药物传递系统用于改善亲脂性药物的黏膜给药的潜力。
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