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Construction of Brain-Targeted Nanoreactor System and Intracerebral Drug Delivery

Shan Wang, Yanci Chen, Feng Gao, Xi Li, Yiyun Huang, Ying Luo, QingPing, Zeng, Qing Zheng


Poly(lactic-co-glycolic acid (PLGA) copolymer) nanoparticles with an average particle diameter of 142.8 nm and a polydispersity of 0.161 were prepared and optimized by an emulsion solvent evaporation method. Blank nanoparticles were modified with the transmembrane peptide (trans-activator of transcription, TAT) and the brain-targeting peptide (Angiopep-2), and the modification rate was determined. It is obvious that the modification rates of TAT and Angiopep-2 were 65.4% and 71.1%. After the preparation of coumarin-6-loaded nanoparticles, high-performance liquid chromatography analysis method was established, the entrapment efficiency, drug loading capacity (DLC) and drug release properties of chaudoulen-6 nanoparticles were determined. It was indicated that the entrapment efficiency of coumarin-6 nanoparticles was 38.21%, DLC was 0.229%, with a sustained release effect within 48 h. Fluorescence imaging technology was used to explore the targeting of nanoparticles in mice. TAT and Angiopep-2 modified nanoparticles exhibited strong brain targeting effects.


nano-release system, polylactic acid-glycolic acid copolymer, brain-targeting peptides, cell-penetrating peptides

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