阳离子改性可吸入尼达尼布纳米囊泡:增强对非小细胞肺癌的治疗活性。

Cationically modified inhalable nintedanib niosomes: enhancing therapeutic activity against non-small-cell lung cancer.

机构信息

Department of Pharmaceutical Sciences, College of Pharmacy & Health Sciences, St. John's University, NY 11439, USA.

Current Affiliation: Pfizer Worldwide R&D, Groton, CT 06340, USA.

出版信息

Nanomedicine (Lond). 2022 Jun;17(13):935-958. doi: 10.2217/nnm-2022-0045. Epub 2022 Aug 25.

Abstract

This study was designed to develop and test nintedanib-loaded niosomes as inhalable carriers for enhancing its therapeutic efficacy via localized drug accumulation and addressing issues such as low bioavailability and severe toxicity. Niosomes were prepared by thin-film hydration method and were evaluated for therapeutic effectiveness in lung cancer cells. The optimized niosomal formulation displayed optimized vesicle size, controlled and extended release of drug, and efficient aerodynamic properties indicating its suitability as an aerosolized formulation. studies revealed significantly superior cytotoxicity of nintedanib-loaded niosomes which was further validated by 3D spheroids. These findings establish the effectiveness of niosomes as inhalable delivery carriers which could serve as a promising strategy for delivery of nintedanib to treat several lung cancers.

摘要

本研究旨在开发和测试尼达尼布负载的脂囊泡作为吸入载体,通过局部药物积累来提高其治疗效果,并解决生物利用度低和毒性严重等问题。脂囊泡采用薄膜水化法制备,并在肺癌细胞中评估其治疗效果。优化的脂囊泡制剂显示出优化的囊泡大小、药物的控制和延长释放以及高效的空气动力学特性,表明其适合作为气溶胶制剂。研究表明,尼达尼布负载的脂囊泡具有显著更高的细胞毒性,这一点通过 3D 球体进一步得到验证。这些发现确立了脂囊泡作为吸入式递药载体的有效性,可为将尼达尼布递送至治疗多种肺癌提供一种有前途的策略。

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