同轴电喷雾法制备的聚-(D,L-乳酸-共聚乙二醇)(PLGA)纳米粒子可控释放多柔比星。

IF 5.3 2区 医学 Q1 PHARMACOLOGY & PHARMACY International Journal of Pharmaceutics Pub Date : 2024-09-21 DOI:10.1016/j.ijpharm.2024.124724
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引用次数: 0

摘要

提高多柔比星(DOX)等化疗药物的疗效并降低其毒性对癌症治疗至关重要。通过同轴电喷法制造的核壳纳米粒子(NPs)可控制抗癌药物的释放,其聚合物外壳可保护药物分子不被快速降解,从而延长治疗效果。本研究开发了负载 DOX 的聚(乳酸-共聚乙醇酸)(PLGA)NPs。通过单针或同轴电喷法分别制备了基质或核壳结构的 NPs。核壳 NPs 具有很高的包封效率(>80%),并能控制 DOX 的分布。与基质 NPs 相比,核壳 NPs 在减少初始猝灭(8 小时内释放 22%)后,表现出更慢的持续释放速度(144 小时内释放 69%)。与游离药物和基质 DOX 负载 NPs 相比,释放动力学遵循扩散机制。体外实验表明,核壳 NPs 对乳腺癌细胞 MCF-7 的细胞毒性增强,荧光显微镜和流式细胞仪观察到的吸收率更高。72 小时后,与基质 NPs(0.235 μg/mL)和游离 DOX(1.482 μg/mL)相比,核壳 NPs 的 IC50 显著下降(0.115 μg/mL)。同轴电喷雾技术能够生产出具有治疗优势的核壳 NPs,药物释放可控且封装效率高,有望改善临床抗癌化疗。
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Controlled release of doxorubicin from Poly-(D,L-lactide-co-glycolide) (PLGA) nanoparticles prepared by coaxial electrospraying
Enhancing the efficacy and reducing the toxicity of chemotherapeutic agents like doxorubicin (DOX) is crucial in cancer treatment. Core-shell nanoparticles (NPs) fabricated by coaxial electrospraying offer controlled release of anticancer agents with the polymer shell protecting drug molecules from rapid degradation, prolonging therapeutic effect. This study developed DOX-loaded poly(lactic-co-glycolic acid) (PLGA) NPs. NPs were fabricated with matrix or core–shell structure via single needle or coaxial electrospraying, respectively. Core-shell NPs exhibited high encapsulation efficiency (>80 %) with controlled DOX distribution. Compared to matrix NPs, core–shell NPs demonstrated slower sustained release (69 % in 144 h) after reduced initial burst (22 % in 8 h). Release kinetics followed a diffusion mechanism when compared to free drug and matrix DOX-loaded NPs. In vitro assays showed core–shell NPs’ enhanced cytotoxicity against breast cancer cells MCF-7, with higher uptake observed by fluorescence microscopy and flow cytometry. The IC50 for core-shell NPs displayed a significant drop (0.115 μg/mL) compared to matrix NPs (0.235 μg/mL) and free DOX (1.482 μg/mL) after 72 h. Coaxial electrospraying enables the production of therapeutically advantageous core–shell NPs, offering controlled drug release with high encapsulation efficiency, potentially improving clinical anticancer chemotherapy.
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来源期刊
CiteScore
10.70
自引率
8.60%
发文量
951
审稿时长
72 days
期刊介绍: The International Journal of Pharmaceutics is the third most cited journal in the "Pharmacy & Pharmacology" category out of 366 journals, being the true home for pharmaceutical scientists concerned with the physical, chemical and biological properties of devices and delivery systems for drugs, vaccines and biologicals, including their design, manufacture and evaluation. This includes evaluation of the properties of drugs, excipients such as surfactants and polymers and novel materials. The journal has special sections on pharmaceutical nanotechnology and personalized medicines, and publishes research papers, reviews, commentaries and letters to the editor as well as special issues.
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