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旨在实现肺泡再生而研发的Am80包裹脂质纳米颗粒对肺气肿有改善作用。

Am80-Encapsulated Lipid Nanoparticles, Developed with the Aim of Achieving Alveolar Regeneration, Have an Improvement Effect on Pulmonary Emphysema.

作者信息

Akita Tomomi, Morita Yuki, Kawai Takehiro, Oda Kazuaki, Tange Kota, Nakai Yuta, Yamashita Chikamasa

机构信息

Department of Pharmaceutics and Drug Delivery, Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamazaki, Noda 278-8510, Japan.

DDS Research Laboratory, NOF CORPORATION, 3-3 Chidori-cho, Kawasaki-ku, Kawasaki City 210-0865, Japan.

出版信息

Pharmaceutics. 2022 Dec 22;15(1):37. doi: 10.3390/pharmaceutics15010037.

Abstract

Chronic obstructive pulmonary disease (COPD) is characterized by chronic bronchitis and emphysema, and current drug treatments target its symptoms. Thus, the development of a therapeutic drug to repair alveolar destruction is urgently needed. Our previous research revealed that the synthetic retinoic acid Am80 (1.0 mg/kg) showed a repairing effect on collapsed alveoli in a mouse model of elastase-induced emphysema. However, a further reduction in the dose is desirable to facilitate the development of a powder inhalation formulation for clinical application. We, therefore, focused on SS-OP to deliver Am80 efficiently. As a result, 0.01 mg/kg of Am80-encapsulated SS-OP nanoparticles repaired collapsed alveoli and improved the respiratory function in the mouse model of elastase induced emphysema. The results suggested that, with the use of SS-OP, the Am80 dose could be reduced. This could contribute to the development of a powder inhalation system as a curative medicine for COPD.

摘要

慢性阻塞性肺疾病(COPD)的特征为慢性支气管炎和肺气肿,目前的药物治疗针对其症状。因此,迫切需要开发一种修复肺泡破坏的治疗药物。我们之前的研究表明,合成视黄酸Am80(1.0毫克/千克)在弹性蛋白酶诱导的肺气肿小鼠模型中对塌陷的肺泡具有修复作用。然而,为了便于开发用于临床应用的粉末吸入制剂,需要进一步降低剂量。因此,我们专注于SS-OP以有效递送Am80。结果,0.01毫克/千克的包封Am80的SS-OP纳米颗粒修复了弹性蛋白酶诱导的肺气肿小鼠模型中的塌陷肺泡并改善了呼吸功能。结果表明,使用SS-OP可以降低Am80的剂量。这可能有助于开发作为COPD治疗药物的粉末吸入系统。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1c96/9860907/1fd2cce4042f/pharmaceutics-15-00037-g001.jpg

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