Brain targeted nanoparticulate drug delivery system of rasagiline via intranasal route

Abstract

The aim of the present study was to prepare and evaluate a rasagiline-loaded chitosan glutamate nanoparticles (RAS-CG-NPs) by ionic gelation of CG with tripolyphosphate anions (TPP). RAS-loaded CG-NPs were characterized for particle size, size distribution, encapsulation efficiency and in vitro drug release. The mean particles size, polydispersity index (PDI) and encapsulation efficiency was found to be 151.1 ± 10.31, 0.380 ± 0.01 and 96.43 ± 4.23, respectively. Biodistribution of RAS formulations in the brain and blood of mice following intranasal (i.n.) and intravenous (i.v.) administration was performed using HPLC analytical method. The drug concentrations in brain following the i.n. of CG-NPs were found to be significantly higher at all the time points compared to both drug (i.n.) and drug CG-NPs (i.v.). The Cmax (999.25 ng/ml) and AUC (2086.60 ng h/ml) of formulation CG-NPs (i.n) were found to be significantly higher than CG-NPs (i.v.) and RAS solution (i.n.). The direct transport percentage (DTP%) values of RAS-loaded CG-NPs (i.n.) as compared to drug solution (i.n.) increased from 66.27 ± 1.8 to 69.27 ± 2.1%. The results showed significant enhancement of bioavailability in brain, after administration of the RAS-loaded CG-NPs which could be a substantial achievement of direct nose to brain targeting in Parkinson's disease therapy.

Brain delivery of buspirone hydrochloride chitosan nanoparticles for the treatment of general anxiety disorder

“…It was recorded that BUH TCS NPs showed the highest DTE % and DTP % of (78.94 ± 15.31 %) and (95.97 ±11.31 %) respectively as compared to BUH solution administered i.v. Similar types of result have also been reported by various groups [12,14,20,49,50].…”

“…route also has the potential for direct CNS delivery [12][13][14][15]. Drugs administered to the nasal cavity can travel along the olfactory and trigeminal nerves to reach brain within the CNS.…”

Application of quality by design approach for intranasal delivery of rivastigmine loaded solid lipid nanoparticles: Effect on formulation and characterization parameters

“…These systems are efficiently taken up by nasal mucosa thereby increasing their specificity, bioavailability, duration of therapeutic effect, besides offering higher drug loading and protection against enzymatic and/or chemical degradation Mittal et al, 2014). Nanoparticulate carriers (lipid emulsions, polymeric nanoparticles, liposomes and micelles etc.…”

Lactoferrin-modified rotigotine nanoparticles for enhanced nose-to-brain delivery: LESA-MS/MS-based drug biodistribution, pharmacodynamics, and neuroprotective effects

“…9,10 Furthermore, nose-to-brain drug delivery has been performed because of its advantages, including reduced drug delivery to nontarget sites, avoidance of hepatic first-pass metabolism, and convenience, for drugs such as rasagiline, alginate, tarenflurbil, and piperine. [11][12][13][14] Therefore, nose-to-brain drug delivery was used in the present study to improve the brainspecific targeting of rotigotine.…”