Rasagiline-encapsulated chitosan-coated PLGA nanoparticles targeted to the brain in the treatment of parkinson's disease

• Published in: Journal of liquid chromatography & related technologies Vol. 40; no. 13; pp. 677 - 690
• Main Author: Ahmad, Niyaz
• Format: Journal Article
• Language: English
• Published: Abingdon Taylor & Francis 09.08.2017; Taylor & Francis Ltd
• Subjects: AUC, area under curve; Bioavailability; Brain; Brain pharmacokinetics; Chitosan; CS, chitosan; CS-PLGA nanoparticles; Drug delivery systems; elimination rate constant; Emulsification; Encapsulation; ESI, electrospray ionization; Evaporation; half-life; High-performance liquid chromatography; HQC, high-quality control; Intravenous administration; LC-MS/MS method validation; Liquid chromatography; LLE, liquid-liquid extraction; LOD, lower limit of detection; LOQ, lower limit of quantification; LOQ, lower limit of quantitation; LOQQC, lower limit of quantification for quality control; LQC, low-quality control; Mass spectroscopy; max; maximum plasma concentration; Movement disorders; MQC, medium-quality control; Nanoparticles; Neurodegenerative diseases; Nose; Parkinson's disease; Particle size; Particle size distribution; PD, Parkinson's disease; Pharmacokinetics; Pharmacology; PLGA, poly(lactic-co-glycolic acid); Polydispersity; Polylactide-co-glycolide; PPT, protein precipitation; PVA, polyvinyl alcohol; Q-TOF, quadrupole time of flight; Rasagiline; RSG, rasagiline; Size distribution; SPE, solid-phase extraction; Spectroscopic analysis; Spectrum analysis; time to C; UHPLC-MS/MS, ultrahigh-performance liquid chromatography-mass spectroscopy and mass spectroscopy; Zeta potential
• ISSN: 1082-6076; 1520-572X
• DOI: 10.1080/10826076.2017.1343735

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.