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首页> 外文期刊>International Journal of Pharmaceutics >Preparation, characterization and antibacterial activities of chitosan, N-trimethyl chitosan (TMC) and N-diethylmethyl chitosan (DEMC) nanoparticles loaded with insulin using both the ionotropic gelation and polyelectrolyte complexation methods.
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Preparation, characterization and antibacterial activities of chitosan, N-trimethyl chitosan (TMC) and N-diethylmethyl chitosan (DEMC) nanoparticles loaded with insulin using both the ionotropic gelation and polyelectrolyte complexation methods.

机译：壳聚糖，N-三甲基壳聚糖（TMC）和负载有胰岛素的N-二乙基甲基壳聚糖（DEMC）纳米颗粒的制备，表征和抗菌活性均采用离子凝胶法和聚电解质络合方法。

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摘要

TMC and DEMC, quaternized derivatives of chitosan, have been shown to have penetration enhancement properties and able to open the tight junctions of the intestinal epithelia at neutral and alkaline pH environments. The use of the nanoparticulate systems has the advantage of protecting the peptidic drugs from the harsh environment of the gastrointestinal tract. Hence, the aim of this study was to synthesize and characterize TMC and DEMC, both with quaternization degrees of 50+/-5%, which were then used to prepare insulin nanoparticles with two different methods: ionotropic gelation and the polyelectrolyte complexation (PEC) techniques. The obtained nanoparticles were then characterized for size, zeta potential, insulin loading and release as well as antibacterial activities. The results showed that nanoparticles prepared by the PEC method had higher insulin loading efficiency and zeta potential than those made by the ionotropic gelation method and may subsequently be used for further in vitro, ex vivo and in vivo studies. Moreover, the antibacterial studies suggest that the polymers in free form have higher antibacterial activity against Gram-positive bacteria than in the nanoparticulate form.
机译：TMC和DEMC（壳聚糖的季铵化衍生物）已显示具有渗透增强性能，并能够在中性和碱性pH环境下打开肠上皮的紧密连接。纳米颗粒系统的使用具有保护肽类药物免受胃肠道恶劣环境影响的优点。因此，本研究的目的是合成和表征季铵化度为50 +/- 5％的TMC和DEMC，然后将其用于通过两种不同的方法制备胰岛素纳米颗粒：离子凝胶法和聚电解质络合物（PEC）技术。然后表征获得的纳米颗粒的大小，ζ电位，胰岛素负载和释放以及抗菌活性。结果表明，通过PEC方法制备的纳米粒子比通过离子电凝胶法制备的纳米粒子具有更高的胰岛素加载效率和Zeta电位，随后可用于进一步的体外，离体和体内研究。而且，抗菌研究表明，与纳米颗粒形式相比，游离形式的聚合物对革兰氏阳性细菌具有更高的抗菌活性。

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