使用致孔剂配制肺部给药微粒的现代趋势:方法、原理和实例。

IF 2.6 4区 医学 Q2 PHARMACOLOGY & PHARMACY Pharmaceutical Development and Technology Pub Date : 2024-06-01 Epub Date: 2024-05-23 DOI:10.1080/10837450.2024.2350530
Andrea Peštálová, Jan Gajdziok
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引用次数: 0

摘要

吸入给药越来越多地用于肺部疾病的局部药物治疗,并作为全身给药的替代途径。现代吸入粉末系统的目标是将药物沉积在所需的作用部位。大孔颗粒(LPP)的特点是空气动力学直径超过 5 μm,密度低于 0.4 g/cm3,能够避免肺部保护机制,因此成为研究的重点。它们大多采用喷雾干燥或冻干等喷雾技术,使用成孔物质(致孔剂)制备而成。这些物质可以是气态、固态或液态,其选择取决于它们的极性、溶解性以及与载体材料和药物的相互兼容性。根据孔隙形成的机理,气孔剂可分为渗透型气孔剂、萃取型气孔剂和分解过程中产生气体的气孔剂等几类。这篇综述描述了用于肺部给药的固体微粒配方的现代趋势;介绍了最常用的致孔剂的作用机制,讨论了它们在各种配方方法中的适用性,强调了喷雾技术;并通过实验研究的实例记录了讨论的主题。
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Modern trends in the formulation of microparticles for lung delivery using porogens: methods, principles and examples.

Inhalation drug administration is increasingly used for local pharmacotherapy of lung disorders and as an alternative route for systemic drug delivery. Modern inhalation powder systems aim to target drug deposition in the required site of action. Large porous particles (LPP), characterized by an aerodynamic diameter over 5 μm, density below 0.4 g/cm3, and the ability to avoid protective lung mechanisms, come to the forefront of the research. They are mostly prepared by spray techniques such as spray drying or lyophilization using pore-forming substances (porogens). These substances could be gaseous, solid, or liquid, and their selection depends on their polarity, solubility, and mutual compatibility with the carrier material and the drug. According to the pores-forming mechanism, porogens can be divided into groups, such as osmogens, extractable porogens, and porogens developing gases during decomposition. This review characterizes modern trends in the formulation of solid microparticles for lung delivery; describes the mechanisms of action of the most often used porogens, discusses their applicability in various formulation methods, emphasizes spray techniques; and documents discussed topics by examples from experimental studies.

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来源期刊
CiteScore
5.90
自引率
2.90%
发文量
82
审稿时长
1 months
期刊介绍: Pharmaceutical Development & Technology publishes research on the design, development, manufacture, and evaluation of conventional and novel drug delivery systems, emphasizing practical solutions and applications to theoretical and research-based problems. The journal aims to publish significant, innovative and original research to advance the frontiers of pharmaceutical development and technology. Through original articles, reviews (where prior discussion with the EIC is encouraged), short reports, book reviews and technical notes, Pharmaceutical Development & Technology covers aspects such as: -Preformulation and pharmaceutical formulation studies -Pharmaceutical materials selection and characterization -Pharmaceutical process development, engineering, scale-up and industrialisation, and process validation -QbD in the form a risk assessment and DoE driven approaches -Design of dosage forms and drug delivery systems -Emerging pharmaceutical formulation and drug delivery technologies with a focus on personalised therapies -Drug delivery systems research and quality improvement -Pharmaceutical regulatory affairs This journal will not consider for publication manuscripts focusing purely on clinical evaluations, botanicals, or animal models.
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