纳米复合物-纳米颗粒的简便制备用于增强阿霉素向脑内的装载和选择性递送。
Facile development of nanocomplex-in-nanoparticles for enhanced loading and selective delivery of doxorubicin to brain.
机构信息
Nanomaterials Lab, Center of Materials Science (CMS), Zewail City of Science & Technology, Giza, Egypt.
Department of Pharmaceutics & Industrial Pharmacy, College of Pharmacy & Drug Manufacturing, Misr University of Science & Technology (MUST), Giza, Egypt.
出版信息
Nanomedicine (Lond). 2017 Dec;12(24):2737-2761. doi: 10.2217/nnm-2017-0243. Epub 2017 Nov 14.
AIM
Facile development of polysaccharides-based carrier system for efficient delivery of doxorubicin (DOX) to the brain.
METHODS
DOX was nanocomplexed with alginate (Alg) followed by incorporation into chitosan (Cs) nanomatrices. The resulting carriers were optimized to have a net positive charge improving their delivery across the blood-brain barrier. The optimum DOX-loaded nanosystem was targeted to brain tissue via loading into various nasal dosage forms.
RESULTS
The pH-dependent ionization of both DOX and Alg was found to have a significant effect on DOX entrapment efficiency which was improved from 4% at slightly acidic media to 85% using different pHs. The nasal dosage forms, especially the insert, delivered the loaded DOX mostly to the brain tissue with targeting efficiency reaching 480%.
CONCLUSION
New intranasal carrier system was developed with efficient targeting of DOX to the brain. The carrier has potential to be used for delivery of other drugs acting on CNS. Graphical abstract: [Formula: see text].
目的
开发基于多糖的载体系统，以将阿霉素（DOX）高效递送至脑部。
方法
DOX 与海藻酸钠（Alg）纳米复合，然后掺入壳聚糖（Cs）纳米基质中。所得载体经优化后带正电荷，从而提高其穿过血脑屏障的递送能力。通过将其装入各种鼻腔给药剂型，将最佳 DOX 载药纳米系统靶向递送至脑组织。
结果
发现 DOX 和 Alg 的 pH 依赖性离解对 DOX 的包封效率有显著影响，通过使用不同 pH 值，将 DOX 的包封效率从酸性介质中的 4%提高到 85%。鼻腔给药剂型，特别是插入剂，将负载的 DOX 主要递送至脑组织，靶向效率达到 480%。
结论
开发了一种新的鼻腔载体系统，可将 DOX 高效靶向递送至脑部。该载体有可能用于递送至中枢神经系统的其他药物。
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