pH-Responsive nanoparticles composed of chitosan (CS) and poly-gamma-glutamic acid (gamma-PGA) blended with tripolyphosphate (TPP) and MgSO(4) (multi-ion-crosslinked NPs) were prepared and characterized to determine their effectiveness in the oral delivery of insulin. Their counterparts without TPP and MgSO(4) (NPs) were used as a control. FT-IR and XRD results indicated that the spontaneous interaction between CS, insulin, gamma-PGA, MgSO(4) and TPP can form an ionically crosslinked network-structure, leading to the formation of nanoparticles. Multi-ion-crosslinked NPs were more compact than NPs, while their zeta potential values were comparable. During storage, multi-ion-crosslinked NPs suspended in deionized water were stable for at least 10 weeks. Multi-ion-crosslinked NPs had a superior stability over a broader pH range than NPs. In the in vitro release study, NPs failed to provide an adequate retention of loaded insulin in dissolution media compared to multi-ion-crosslinked NPs. Transepithelial-electrical-resistance and transport experiments demonstrated that multi-ion-crosslinked NPs significantly more effectively transported insulin than NPs; confocal visualization further validated the enhanced permeation of insulin via the paracellular pathway. The aforementioned results suggest that multi-ion-crosslinked NPs are a promising carrier for improved transmucosal delivery of insulin in the small intestine.

译文

:制备了由壳聚糖(CS)和聚γ-谷氨酸(γ-PGA)与三聚磷酸盐(TPP)和MgSO(4)(多离子交联的NPs)混合而成的pH响应纳米颗粒在口服胰岛素中。没有TPP和MgSO(4)(NPs)的对应物用作对照。 FT-IR和XRD结果表明CS,胰岛素,γ-PGA,MgSO(4)和TPP之间的自发相互作用可以形成离子交联的网络结构,从而导致纳米颗粒的形成。多离子交联的NP比NP更紧凑,而它们的ζ电位值却相当。在储存过程中,悬浮在去离子水中的多离子交联NP稳定至少10周。与NP相比,多离子交联的NP在更宽的pH范围内具有出色的稳定性。在体外释放研究中,与多离子交联的NP相比,NP在溶解介质中未能提供足够的负载胰岛素保留。跨上皮电阻和转运实验表明,多离子交联的NPs转运胰岛素的效率明显高于NPs。共聚焦可视化进一步证实了胰岛素通过细胞旁途径的渗透性增强。前述结果表明,多离子交联的NP是改善小肠中胰岛素经粘膜递送的有希望的载体。

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