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可吸入性聚（乳酸-乙醇酸）微球的设计与特性研究，该微球由细乳液干燥工艺制备，用于鲑鱼降钙素的持续作用。

Design and Characterizations of Inhalable Poly(lactic--glycolic acid) Microspheres Prepared by the Fine Droplet Drying Process for a Sustained Effect of Salmon Calcitonin.

机构信息

Laboratory of Biopharmacy, School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-ku, Shizuoka 422-8526, Japan.

Functional Material Development Center, Imaging Engine Development Division, RICOH Company, Ltd., 16-1 Honda-machi, Numazu-shi, Shizuoka 410-1458, Japan.

出版信息

Molecules. 2020 Mar 13;25(6):1311. doi: 10.3390/molecules25061311.

DOI:10.3390/molecules25061311
PMID:32183032
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC7144118/
Abstract

The present study aimed to develop inhalable poly (lactic--glycolic acid) (PLGA)-based microparticles of salmon calcitonin (sCT) for sustained pharmacological action by the fine droplet drying (FDD) process, a novel powderization technique employing printing technologies. PLGA was selected as a biodegradable carrier polymer for sustained-release particles of sCT (sCT/SR), and physicochemical characterizations of sCT/SR were conducted. To estimate the in vivo efficacy of the sCT/SR respirable powder (sCT/SR-RP), plasma calcium levels were measured after intratracheal administration in rats. The particle size of sCT/SR was 3.6 µm, and the SPAN factor, one of the parameters to present the uniformity of particle size distribution, was calculated to be 0.65. In the evaluation of the conformational structure of sCT, no significant changes were observed in sCT/SR even after the FDD process. The drug release from sCT/SR showed a biphasic pattern with an initial burst and slow diffusion in simulated lung fluid. sCT/SR-RP showed fine inhalation performance, as evidenced by a fine particle fraction value of 28% in the cascade impactor analysis. After the insufflation of sCT samples (40 µg-sCT/kg) in rats, sCT/SR-RP could enhance and prolong the hypocalcemic action of sCT possibly due to the sustained release and pulmonary absorption of sCT. From these observations, the strategic application of the FDD process could be efficacious to provide PLGA-based inhalable formulations of sCT, as well as other therapeutic peptides, to enhance their biopharmaceutical potentials.

摘要

本研究旨在通过精细液滴干燥（FDD）工艺（一种采用印刷技术的新型粉末化技术）开发具有鲑鱼降钙素（sCT）持续药理作用的可吸入性聚（乳酸-乙醇酸）（PLGA）基微球。PLGA 被选为 sCT（sCT/SR）的可生物降解载体聚合物，以用于 sCT/SR 的持续释放颗粒，并对其进行理化特性分析。为了评估 sCT/SR 可吸入粉末（sCT/SR-RP）的体内疗效，在大鼠气管内给药后测量了血浆钙水平。sCT/SR 的粒径为 3.6 µm，SPAN 因子（表示粒径分布均匀性的参数之一）计算为 0.65。在 sCT 的构象结构评价中，即使在 FDD 工艺后，sCT/SR 也没有观察到明显的变化。sCT/SR 的药物释放呈双相模式，具有初始突释和在模拟肺液中的缓慢扩散。sCT/SR-RP 表现出良好的吸入性能，级联撞击器分析中的细颗粒分数值为 28%。在大鼠中（40 µg-sCT/kg）喷入 sCT 样品后，sCT/SR-RP 可能由于 sCT 的持续释放和肺吸收而增强和延长 sCT 的降血钙作用。从这些观察结果可以看出，FDD 工艺的战略应用可以有效地提供基于 PLGA 的 sCT 可吸入制剂，以及其他治疗性肽，以增强它们的生物制药潜力。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/6905e50266df/molecules-25-01311-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/1d0b836ff9d3/molecules-25-01311-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/8e2f8530fdfc/molecules-25-01311-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/9f732f27ab59/molecules-25-01311-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/87f3e1008a0e/molecules-25-01311-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/6905e50266df/molecules-25-01311-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/1d0b836ff9d3/molecules-25-01311-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/8e2f8530fdfc/molecules-25-01311-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/9f732f27ab59/molecules-25-01311-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/87f3e1008a0e/molecules-25-01311-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/48ae/7144118/6905e50266df/molecules-25-01311-g005.jpg

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2
Development of PLGA nanoparticles for sustained release of a connexin43 mimetic peptide to target glioblastoma cells.用于持续释放连接蛋白 43 模拟肽以靶向神经胶质瘤细胞的 PLGA 纳米粒的研制。
Mater Sci Eng C Mater Biol Appl. 2020 Mar;108:110191. doi: 10.1016/j.msec.2019.110191. Epub 2019 Sep 12.
3
[Inhalers and inhalation techniques in the treatment of asthma and chronic obstructive pulmonary disease].
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Pharmaceutics. 2023 Feb 8;15(2):571. doi: 10.3390/pharmaceutics15020571.
4
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Molecules. 2022 Oct 11;27(20):6775. doi: 10.3390/molecules27206775.
5
Poly(Lactic Acid)-Based Microparticles for Drug Delivery Applications: An Overview of Recent Advances.用于药物递送应用的聚乳酸基微粒：最新进展综述
Pharmaceutics. 2022 Feb 4;14(2):359. doi: 10.3390/pharmaceutics14020359.
[吸入器与吸入技术在哮喘和慢性阻塞性肺疾病治疗中的应用]
Ugeskr Laeger. 2019 Aug 12;181(33).
4
Protein misfolding, aggregation and mechanism of amyloid cytotoxicity: An overview and therapeutic strategies to inhibit aggregation.蛋白质错误折叠、聚集和淀粉样细胞毒性的机制：概述和抑制聚集的治疗策略。
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5
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6
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7
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Nat Rev Drug Discov. 2019 Jan;18(1):19-40. doi: 10.1038/nrd.2018.183. Epub 2018 Nov 30.
8
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