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用于经鼻向脑递送以治疗抑郁症的新型优化生物聚合物基纳米颗粒。

Novel optimized biopolymer-based nanoparticles for nose-to-brain delivery in the treatment of depressive diseases.

作者信息

Sorrentino Alessandro, Cataldo Antonino, Curatolo Riccardo, Tagliatesta Pietro, Mosca Luciana, Bellucci Stefano

机构信息

INFN-Laboratori Nazionali di Frascati Frascati Rome Italy

Raithor Srl Rome Italy.

出版信息

RSC Adv. 2020 Aug 4;10(48):28941-28949. doi: 10.1039/d0ra04212a. eCollection 2020 Aug 3.

Abstract

A valid option to bypass the obstacle represented by the blood-brain barrier (BBB) in brain delivery is the use of the unconventional intranasal route of administration. The treatment of depressive diseases, resulting from the depletion of a neurotransmitter in the inter-synaptic space, such as serotonin, is indirectly treated using molecules that can permeate the BBB unlike the latter. In the present article, a set of nanovectors were produced using a mucoadhesive biopolymer, alginate (Alg). Optimizing the reaction, polymeric nanoparticles having diameter of 30-70 nm were produced, and water stable multi-walled carbon nanotubes functionalized (MWCNT-COOH)/Alg complexes were obtained. These nanovectors were loaded with serotonin, evaluating drug loading/release. By means of Raman microscopy, the cellular internalization of the (MWCNT-COOH)/Alg complex was demonstrated. A complete biocompatibility on neuronal cells was proved for the whole set of nanovectors. Finally, a method of self-administration was tested, which involves the use of a household apparatus, such as an aerosol machine, observing a fine particulate, able to deliver the nanovectors through the nose.

摘要

在脑内给药中,绕过血脑屏障(BBB)这一障碍的有效方法是采用非常规的鼻内给药途径。对于因突触间隙中神经递质(如血清素)耗竭而导致的抑郁症,可使用能够穿透血脑屏障的分子进行间接治疗。在本文中,使用一种粘膜粘附生物聚合物藻酸盐(Alg)制备了一组纳米载体。通过优化反应,制备出了直径为30 - 70 nm的聚合物纳米颗粒,并获得了水稳定的功能化多壁碳纳米管(MWCNT-COOH)/Alg复合物。这些纳米载体负载了血清素,并对药物负载/释放进行了评估。通过拉曼显微镜,证明了(MWCNT-COOH)/Alg复合物的细胞内化。证明了这组纳米载体对神经元细胞具有完全的生物相容性。最后,测试了一种自我给药方法,该方法涉及使用家用设备,如气溶胶机,观察一种能够通过鼻腔递送纳米载体的细颗粒。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/cf57/9055835/93ec9fed66c3/d0ra04212a-f1.jpg

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