Sato Takumi, Murakami Yoshihiko
Department of Organic and Polymer Materials Chemistry, Tokyo University of Agriculture and Technology, Naka-cho, Koganei-shi 2-24-16, Tokyo 184-8588, Japan.
Materials (Basel). 2022 Jul 5;15(13):4717. doi: 10.3390/ma15134717.
Most drug carriers used in pulmonary administration are microparticles with diameters over 1 µm. Only a few examples involving nanoparticles have been reported because such small particles are readily exhaled. Consequently, the development of microparticles capable of encapsulating nanoparticles and a wide range of compounds for pulmonary drug-delivery applications is an important objective. In this study, we investigated the development of polysaccharide microparticles containing nanoparticles for the temperature-responsive and two-step release of inclusions. The prepared microparticles containing nanoparticles can release two differently charged compounds in a stepwise manner. The particles have two different drug release pathways: one is the release of nanoparticle inclusions from the nanoparticles and the other is the release of microparticle inclusions during microparticle collapse. The nanoparticles can be efficiently delivered deep into the lungs and a wide range of compounds are released in a charge-independent manner, owing to the suitable roughness of the microparticle surface. These polysaccharide microparticles containing nanoparticles are expected to be used as temperature-responsive drug carriers, not only for pulmonary administration but also for various administration routes, including transpulmonary, intramuscular, and transdermal routes, that can release multiple drugs in a controlled manner.
大多数用于肺部给药的药物载体是直径超过1微米的微粒。由于这种小颗粒很容易被呼出，因此只有少数涉及纳米颗粒的例子被报道。因此，开发能够包裹纳米颗粒和多种化合物用于肺部药物递送应用的微粒是一个重要目标。在本研究中，我们研究了含有纳米颗粒的多糖微粒的开发，用于内含物的温度响应和两步释放。制备的含有纳米颗粒的微粒可以逐步释放两种带不同电荷的化合物。这些颗粒有两种不同的药物释放途径：一种是纳米颗粒内含物从纳米颗粒中的释放，另一种是微粒内含物在微粒塌陷过程中的释放。由于微粒表面具有合适的粗糙度，纳米颗粒可以有效地深入肺部，并且多种化合物以与电荷无关的方式释放。这些含有纳米颗粒的多糖微粒有望用作温度响应性药物载体，不仅用于肺部给药，还可用于包括经肺、肌肉和透皮途径在内的各种给药途径，能够以可控方式释放多种药物。
