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伊立替康负载聚己内酯纳米粒的研发与优化及其对原发性高级别胶质瘤细胞的细胞毒性

Development and Optimization of Irinotecan-Loaded PCL Nanoparticles and Their Cytotoxicity against Primary High-Grade Glioma Cells.

作者信息

Mahmoud Basant Salah, McConville Christopher

机构信息

College of Medical and Dental Sciences, School of Pharmacy, University of Birmingham, Birmingham B15 2TT, UK.

Hormones Department, Medical Research Division, National Research Centre, El Buhouth St., Dokki, Cairo 12622, Egypt.

出版信息

Pharmaceutics. 2021 Apr 13;13(4):541. doi: 10.3390/pharmaceutics13040541.

DOI:10.3390/pharmaceutics13040541
PMID:33924355
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC8068837/
Abstract

BACKGROUND

High-grade gliomas (HGGs) are highly malignant tumors with a poor survival rate. The inability of free drugs to cross the blood-brain barrier and their off-target accumulation result in dose-limiting side effects. This study aimed at enhancing the encapsulation efficiency (EE) of irinotecan hydrochloride trihydrate (IRH) within polycaprolactone (PCL) nanoparticles with optimized size and charge.

MATERIALS AND METHODS

IRH-loaded PCL nanoparticles were formulated using either the single emulsion (O/W, W/O and O/O) or double emulsion (W/O/O and W/O/W) solvent evaporation techniques. The nanoparticles were characterized for their size, zeta potential and EE, with the optimized nanoparticles being characterized for their drug release and cytotoxicity.

RESULTS

The amorphization of PCL and the addition of electrolytes to the aqueous phases of the W/O/W emulsion produced spherical nanoparticles with a mean diameter of 202.1 ± 2.0 nm and an EE of 65.0%. The IRH-loaded nanoparticles exhibited zero-order release and were cytotoxic against primary HGG cells.

CONCLUSION

The amorphization of PCL improves its EE of hydrophilic drugs, while the addition of electrolytes to the aqueous phases of the W/O/W emulsion enhances their EE further. IRH-loaded PCL nanoparticles have the potential to deliver cytotoxic levels of IRH over a sustained period of time, enhancing the cell death of HGGs.

摘要

背景

高级别胶质瘤（HGGs）是高恶性肿瘤，生存率低。游离药物无法穿过血脑屏障且会出现非靶向性蓄积，导致剂量限制性副作用。本研究旨在提高三水合盐酸伊立替康（IRH）在具有优化尺寸和电荷的聚己内酯（PCL）纳米颗粒中的包封效率（EE）。

材料与方法

采用单乳液（油包水、水包油和油包油）或双乳液（水包油包水和水包油包油）溶剂蒸发技术制备负载IRH的PCL纳米颗粒。对纳米颗粒的尺寸、zeta电位和EE进行表征，对优化后的纳米颗粒进行药物释放和细胞毒性表征。

结果

PCL的非晶化以及向水包油包水乳液的水相中添加电解质产生了平均直径为202.1±2.0nm、EE为65.0%的球形纳米颗粒。负载IRH的纳米颗粒表现出零级释放，对原发性HGG细胞具有细胞毒性。

结论

PCL的非晶化提高了其对亲水性药物的EE，而向水包油包水乳液的水相中添加电解质进一步提高了其EE。负载IRH的PCL纳米颗粒有潜力在一段时间内持续递送细胞毒性水平的IRH，增强HGGs的细胞死亡。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/35e329beae5b/pharmaceutics-13-00541-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/00fa1f61b933/pharmaceutics-13-00541-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/87b70ecb6fe6/pharmaceutics-13-00541-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/9da32514426e/pharmaceutics-13-00541-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/aa8c465fd680/pharmaceutics-13-00541-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/2cba3caa6380/pharmaceutics-13-00541-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/9cbdcad00511/pharmaceutics-13-00541-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/35e329beae5b/pharmaceutics-13-00541-g007.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/00fa1f61b933/pharmaceutics-13-00541-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/87b70ecb6fe6/pharmaceutics-13-00541-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/9da32514426e/pharmaceutics-13-00541-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/aa8c465fd680/pharmaceutics-13-00541-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/2cba3caa6380/pharmaceutics-13-00541-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/9cbdcad00511/pharmaceutics-13-00541-g006.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/c067/8068837/35e329beae5b/pharmaceutics-13-00541-g007.jpg

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