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脂质包覆介孔二氧化硅纳米粒子的超声响应智能药物递送系统

Ultrasound-Responsive Smart Drug Delivery System of Lipid Coated Mesoporous Silica Nanoparticles.

作者信息

Amin Muhammad Umair, Ali Sajid, Tariq Imran, Ali Muhammad Yasir, Pinnapreddy Shashank Reddy, Preis Eduard, Wölk Christian, Harvey Richard D, Hause Gerd, Brüßler Jana, Bakowsky Udo

机构信息

Department of Pharmaceutics and Biopharmaceutics, University of Marburg, Robert-Koch-Str. 4, 35037 Marburg, Germany.

Angström Laboratory, Department of Chemistry, Uppsala University, 75123 Uppsala, Sweden.

出版信息

Pharmaceutics. 2021 Sep 3;13(9):1396. doi: 10.3390/pharmaceutics13091396.

Abstract

The immediate release of chemotherapeutics at the target site, along with no premature release in circulation is always challenging. The purpose of this study was to develop a stimuli responsive drug delivery system, composed of lipid supported mesoporous silica nanoparticles (MSNPs) for triggered drug release at the target site and simultaneously avoiding the premature release. MSNPs with a higher drug loading capacity and very slow release were designed so as to enhance release by FDA approved US-irradiation. Doxorubicin, as a model drug, and perfluoropentane (PFP) as a US responsive material, were entrapped in the porous structure of MSNPs. Lipid coating enhanced the cellular uptake and in addition provided a gatekeeping effect at the pore opening to reduce premature release. The mechanical and thermal effects of US induced the conversion of liquid PFP to a gaseous form that was able to rupture the lipid layer, resulting in triggered drug release. The prolonged stability profile and non-toxic behavior made them suitable candidate for the delivery of anticancer drugs. This smart system, with the abilities of better cellular uptake and higher cytotoxic effects on US-irradiation, would be a good addition to the applied side of chemotherapeutic advanced drug delivery systems.

摘要

在靶位点即时释放化疗药物,同时避免在循环中过早释放,一直是个挑战。本研究的目的是开发一种刺激响应型药物递送系统,该系统由脂质负载的介孔二氧化硅纳米颗粒(MSNP)组成,用于在靶位点触发药物释放,同时避免过早释放。设计了具有更高载药量和极缓慢释放特性的MSNP,以便通过美国食品药品监督管理局(FDA)批准的超声照射来增强释放。将阿霉素作为模型药物,全氟戊烷(PFP)作为超声响应材料,包封于MSNP的多孔结构中。脂质包衣增强了细胞摄取,此外在孔口起到了守门作用,以减少过早释放。超声的机械和热效应促使液态PFP转变为气态,从而能够破坏脂质层,导致触发药物释放。其延长的稳定性和无毒特性使其成为递送抗癌药物的合适候选物。这种智能系统具有更好的细胞摄取能力以及对超声照射更高的细胞毒性作用,将是化疗先进药物递送系统应用领域的一个很好补充。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/a7b1/8468042/3f531d334aa8/pharmaceutics-13-01396-sch001.jpg

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