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Microencapsulated chitosan nanoparticles for lung protein delivery.

机译:微囊化的壳聚糖纳米颗粒用于肺部蛋白质的递送。

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It has already been demonstrated that spray drying is a very valuable technique for producing dry powders adequate for pulmonary delivery of drugs. We have developed chitosan/tripolyphosphate nanoparticles that promote peptide absorption across mucosal surfaces. The aim of this work was to microencapsulate protein-loaded chitosan nanoparticles using typical aerosol excipients, such as mannitol and lactose, producing microspheres as carriers of protein-loaded nanoparticles to the lung. The results showed that the obtained microspheres are mostly spherical and possess appropriate aerodynamic properties for pulmonary delivery (aerodynamic diameters between 2 and 3 microm, apparent density lower than 0.45 g/cm3). Moreover, microspheres morphology was strongly affected by the content of chitosan nanoparticles. These nanoparticles show a good protein loading capacity (65-80%), providing the release of 75-80% insulin within 15 min, and can be easily recovered from microspheres after contact with an aqueous medium with no significant changes in their size and zeta potential values. Therefore, this work demonstrated that protein-loaded nanoparticles could be successfully incorporated into microspheres with adequate characteristics to reach the deep lung, which after contact with its aqueous environment are expected to be able to release the nanoparticles, and thus, the therapeutic macromolecule.
机译:已经证明喷雾干燥是生产适于肺部输送药物的干粉的非常有价值的技术。我们已经开发了壳聚糖/三聚磷酸盐纳米颗粒,可促进肽在粘膜表面的吸收。这项工作的目的是使用典型的气溶胶赋形剂(如甘露醇和乳糖)微囊化负载蛋白的壳聚糖纳米颗粒,从而产生微球作为肺中载有蛋白负载的纳米颗粒的载体。结果表明,所获得的微球大部分为球形,并具有适合肺部递送的空气动力学特性(空气动力学直径为2至3微米,表观密度低于0.45 g / cm3)。此外,壳聚糖纳米粒子的含量强烈影响微球的形态。这些纳米颗粒显示出良好的蛋白质负载能力(65-80%),可在15分钟内释放75-80%的胰岛素,并且在与水性介质接触后可轻松从微球中回收,其大小和Zeta均无明显变化。潜在价值。因此,这项工作表明,负载蛋白的纳米颗粒可以成功地掺入具有足够特性的微球,以到达深部肺部,该深部肺部在与其水性环境接触后有望释放出纳米颗粒,从而释放出治疗性大分子。

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