期刊
JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES
卷 40, 期 13, 页码 677-690出版社
TAYLOR & FRANCIS INC
DOI: 10.1080/10826076.2017.1343735
关键词
Brain pharmacokinetics; CS-PLGA nanoparticles; LC-MS/MS method validation; Parkinson's disease; rasagiline
The aim of this study was to investigate the brain targeting potential of rasagiline-encapsulated chitosan-coated PLGA nanoparticles (RSG-CS-PLGA-NPs) delivered intranasally into the brain. Chitosan-coated PLGA nanoparticles (RSG-CS-PLGA-NPs) were developed through double emulsification-solvent evaporation technique. RSG-CS-PLGA-NPs were characterized for particle size, zeta potential, size distribution, encapsulation efficiency, and in vitro drug release. The mean particle size, polydispersity index, and encapsulation efficiency were found to be 122.38 +/- 3.64, 0.212 +/- 0.009, and 75.83 +/- 3.76, respectively. High-performance liquid chromatography-mass spectroscopy and mass spectroscopy study showed a significantly high mucoadhesive potential of RSG-CS-PLGA-NPs and least for conventional and homogenized nanoformulation. Pharmacokinetic results of RSG-CS-PLGA-NPs in Wistar rat brain and plasma showed a significantly high (**p<0.005) AUC(0-24) and amplified C-max over intravenous treatment group. Finally, the investigation demonstrated that intranasal delivery of mucoadhesive nanocarrier showed significant enhancement of bioavailability in brain, after administration of the RSG-CS-PLGA-NPs which could be a substantial achievement of direct nose to brain targeting in Parkinson's disease therapy and related brain disorders.
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