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

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

Abstract

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.

Keywords

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

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References

Honjo K, Black SE, Verhoeff NP. Alzheimer’s disease, cerebrovascular disease, and the ?-amyloid cascade. Can J Neurol Sci.2012;39:712–728.

Abbott A. Dementia: a problem for our age. Nature. 2011;475:S2–S4.

Greenwald RB, Choe YH, McGuire J, Conover CD. Effective drug delivery by PEGylated drug conjugates. Adv Drug Deliv Rev.2003;55:217–250.

Zorko M, Langel U. Cell-penetrating peptides: mechanism and kinetics of cargo delivery. Adv Drug Deliv Rev. 2005;57:529–545.

Demeule M, Régina A, Ché C, Poirier J, Nguyen T, Gabathuler R, et al. Identification and design of peptides as a new drug delivery system for the brain. J Pharmacol Exp Ther.2008;324:1064–1072.

Panyam J, Sahoo SK, Prabha S, Bargar T, Labhasetwar V.Fluorescence and electron microscopy probes for cellular and tissue uptake of poly(D,L-lactide-

co-glycolide) nanoparticles. Int J Pharm. 2003;262:1–11.

Shaner NC, Steinbach PA, Tsien RY. A guide to choosing fluorescent proteins. Nat Methods. 2005;2:905–909.

Shu X, Royant A, Lin MZ, Aguilera TA, Lev-Ram V, Steinbach PA, et al. Mammalian expression of infrared fluorescent proteins engineered from a bacterial phytochrome. Science. 2009;324:804–807.

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Journal of Pharmaceutical and Biomedical Sciences