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载有多重响应性聚(N-乙烯基己内酰胺-co-衣康酸-co-乙二醇二甲基丙烯酸酯)基水凝胶纳米颗粒的壳聚糖微球作为一种新型载体用于疏水性药物的递送。

Chitosan microparticles embedded with multi-responsive poly(N-vinylcaprolactam-co-itaconic acid-co-ethylene-glycol dimethacrylate)-based hydrogel nanoparticles as a new carrier for delivery of hydrophobic drugs.

机构信息

Laboratory of Polymers, Department of Chemical Engineering, Engineering School of Lorena, University of São Paulo, EEL-USP, Estrada Municipal do Campinho, s/n, 12602-810, Lorena, SP, Brazil.

Laboratory of Polymers, Department of Chemical Engineering, Engineering School of Lorena, University of São Paulo, EEL-USP, Estrada Municipal do Campinho, s/n, 12602-810, Lorena, SP, Brazil.

出版信息

Colloids Surf B Biointerfaces. 2019 Mar 1;175:73-83. doi: 10.1016/j.colsurfb.2018.11.042. Epub 2018 Nov 22.

DOI:10.1016/j.colsurfb.2018.11.042
PMID:30522010
Abstract

In this paper, chitosan was used as protective agent for dual temperature-/pH-sensitive poly(N-vinylcaprolactam-co-itaconic acid-co-ethylene- glycol dimethacrylate)- based hydrogel nanoparticles (poly(NVCL-co-IA-co-EGDMA)) aiming avoid their undesirable colloidal destabilization at different conditions of body human tissues. Thus, poly(NVCL-co-IA-co-EGDMA) was embedded into chitosan and a new solid dispersion was prepared via spray-drying and ketoprofen was used as carrier. Two different sizes of hydrogel nanoparticles (120.6 nm and 185.9 nm) were evaluated and they exhibited a drug encapsulation efficiency of the 39.6% and 57.8%, respectively. The smaller nanoparticles showed to be faster for releasing of ketoprofen at pH 7.4 and 37 °C due to their larger surface area and higher swelling ability. Chitosan played a role of a secondary barrier for the ketoprofen diffusion, extending its release compared to hydrogel nanoparticles alone. Among two concentrations (40 wt% and 70 wt%) of hydrogel nanoparticles related to chitosan, the first one induced higher percentages of ketoprofen release: 74.2% against 64.6%. In addition, the interactions between chitosan matrix and poly(NVCL-co-IA-co-EGDMA) did not change the multi-responsive behavior of hydrogels, suggesting the chitosan was efficient for keeping integrity of nanoparticles hydrogels. Chitosan/poly(NVCL-co-IA-co-EGDMA) hybrid microparticles seems to be a promising new carrier for release of hydrophobic drugs, such as ketoprofen.

摘要

本文使用壳聚糖作为双重温度-/pH 敏感的聚(N-乙烯基己内酰胺-co-衣康酸-co-乙二醇二甲基丙烯酸酯)基水凝胶纳米粒子(poly(NVCL-co-IA-co-EGDMA))的保护剂,旨在避免其在人体组织不同条件下的胶体不稳定。因此,将 poly(NVCL-co-IA-co-EGDMA)嵌入壳聚糖中,并通过喷雾干燥制备新的固体分散体,其中酮洛芬被用作载体。评估了两种不同尺寸的水凝胶纳米粒子(120.6nm 和 185.9nm),它们分别显示出 39.6%和 57.8%的药物包封效率。较小的纳米粒子在 pH 7.4 和 37°C 下显示出更快的酮洛芬释放速度,这是由于它们具有更大的表面积和更高的溶胀能力。壳聚糖在酮洛芬扩散方面起到了二级屏障的作用,与单独的水凝胶纳米粒子相比,延长了其释放时间。在与壳聚糖相关的两种浓度(40wt%和 70wt%)的水凝胶纳米粒子中,第一种浓度诱导了更高的酮洛芬释放百分比:74.2%对 64.6%。此外,壳聚糖基质与 poly(NVCL-co-IA-co-EGDMA)之间的相互作用并没有改变水凝胶的多响应行为,这表明壳聚糖有效地保持了纳米水凝胶的完整性。壳聚糖/poly(NVCL-co-IA-co-EGDMA)杂化微球似乎是一种有前途的新型载体,可用于释放疏水性药物,如酮洛芬。

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