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工程化合适的制剂以增强药物传递。

Engineering the right formulation for enhanced drug delivery.

机构信息

School of Pharmacy, College of Medicine, National Taiwan University, Taipei 100, Taiwan.

Advanced Drug Delivery Group, Sydney Pharmacy School, Faculty of Medicine and Health, The University of Sydney, NSW 2006, Australia.

出版信息

Adv Drug Deliv Rev. 2022 Dec;191:114561. doi: 10.1016/j.addr.2022.114561. Epub 2022 Oct 1.

Abstract

Dry powder inhalers (DPIs) can be used with a wide range of drugs such as small molecules and biologics and offer several advantages for inhaled therapy. Early DPI products were intended to treat asthma and lung chronic inflammatory disease by administering low-dose, high-potency drugs blended with lactose carrier particles. The use of lactose blends is still the most common approach to aid powder flowability and dose metering in DPI products. However, this conventional approach may not meet the high demand for formulation physical stability, aerosolisation performance, and bioavailability. To overcome these issues, innovative techniques coupled with modification of the traditional methods have been explored to engineer particles for enhanced drug delivery. Different particle engineering techniques have been utilised depending on the types of the active pharmaceutical ingredient (e.g., small molecules, peptides, proteins, cells) and the inhaled dose. This review discusses the challenges of formulating DPI formulations of low-dose and high-dose small molecule drugs, and biologics, followed by recent and emerging particle engineering strategies utilised in developing the right inhalable powder formulations for enhanced drug delivery.

摘要

干粉吸入器(DPIs)可与多种药物一起使用,如小分子和生物制剂,并为吸入治疗提供多种优势。早期的 DPI 产品旨在通过给予与乳糖载体颗粒混合的低剂量、高效力药物来治疗哮喘和肺部慢性炎症性疾病。使用乳糖混合物仍然是最常见的方法,以帮助 DPI 产品中的粉末流动性和剂量计量。然而,这种传统方法可能无法满足对制剂物理稳定性、气溶胶化性能和生物利用度的高要求。为了克服这些问题,人们已经探索了创新技术并结合传统方法的改进,以用于设计用于增强药物递送的颗粒。根据活性药物成分(例如小分子、肽、蛋白质、细胞)的类型和吸入剂量,使用了不同的颗粒工程技术。本文综述了低剂量和高剂量小分子药物和生物制剂的 DPI 制剂配方的挑战,以及最近和新兴的颗粒工程策略,用于开发用于增强药物递送的合适可吸入粉末制剂。

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