TY - JOUR
T1 - Fabrication, optimization, and evaluation of rotigotine-loaded chitosan nanoparticles for nose-to-brain delivery
AU - Tzeyung, Angeline Shak
AU - Md, Shadab
AU - Bhattamisra, Subrat Kumar
AU - Madheswaran, Thiagarajan
AU - Alhakamy, Nabil A.
AU - Aldawsari, Hibah M.
AU - Radhakrishnan, Ammu K.
N1 - Funding Information:
Ministry of Science and Technology Innovation (MOSTI), Kuala Lumpur, Malaysia, grant number (02-02-09-SF0055), funded this research.
Publisher Copyright:
© 2019 by the authors. Licensee MDPI, Basel, Switzerland.
Copyright:
Copyright 2019 Elsevier B.V., All rights reserved.
PY - 2019/1/10
Y1 - 2019/1/10
N2 - The objective of the present study was to develop, optimize, and evaluate rotigotine-loaded chitosan nanoparticles (RNPs) for nose-to-brain delivery. Rotigotine-loaded chitosan nanoparticles were prepared by the ionic gelation method and optimized for various parameters such as the effect of chitosan, sodium tripolyphosphate, rotigotine concentration on particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using photon correlation spectroscopy, transmission electron microscopy, scanning electron microscopy, atomic force microscopy, fourier-transform infrared spectroscopy, and X-ray diffraction. The developed RNPs showed a small hydrodynamic particle size (75.37 ± 3.37 nm), small PDI (0.368 ± 0.02), satisfactory zeta potential (25.53 ± 0.45 mV), and very high entrapment efficiency (96.08 ± 0.01). The 24-h in vitro release and ex vivo nasal permeation of rotigotine from the nanoparticles were 49.45 ± 2.09% and 92.15 ± 4.74% while rotigotine solution showed corresponding values of 95.96 ± 1.79%and 58.22 ± 1.75%, respectively. The overall improvement ratio for flux and permeability coefficient were found to be 4.88 and 2.67 when compared with rotigotine solution. A histopathological study showed that the nanoparticulate formulation produced no toxicity or structural damage to nasal mucosa. Our results indicated that rotigotine-loaded chitosan nanoparticles provide an efficient carrier for nose-to-brain delivery.
AB - The objective of the present study was to develop, optimize, and evaluate rotigotine-loaded chitosan nanoparticles (RNPs) for nose-to-brain delivery. Rotigotine-loaded chitosan nanoparticles were prepared by the ionic gelation method and optimized for various parameters such as the effect of chitosan, sodium tripolyphosphate, rotigotine concentration on particle size, polydispersity index (PDI), zeta potential, and entrapment efficiency. The prepared nanoparticles were characterized using photon correlation spectroscopy, transmission electron microscopy, scanning electron microscopy, atomic force microscopy, fourier-transform infrared spectroscopy, and X-ray diffraction. The developed RNPs showed a small hydrodynamic particle size (75.37 ± 3.37 nm), small PDI (0.368 ± 0.02), satisfactory zeta potential (25.53 ± 0.45 mV), and very high entrapment efficiency (96.08 ± 0.01). The 24-h in vitro release and ex vivo nasal permeation of rotigotine from the nanoparticles were 49.45 ± 2.09% and 92.15 ± 4.74% while rotigotine solution showed corresponding values of 95.96 ± 1.79%and 58.22 ± 1.75%, respectively. The overall improvement ratio for flux and permeability coefficient were found to be 4.88 and 2.67 when compared with rotigotine solution. A histopathological study showed that the nanoparticulate formulation produced no toxicity or structural damage to nasal mucosa. Our results indicated that rotigotine-loaded chitosan nanoparticles provide an efficient carrier for nose-to-brain delivery.
KW - Chitosan
KW - Nanoparticles
KW - Nose to brain
KW - Parkinson disease
KW - Rotigotine
UR - http://www.scopus.com/inward/record.url?scp=85060650792&partnerID=8YFLogxK
U2 - 10.3390/pharmaceutics11010026
DO - 10.3390/pharmaceutics11010026
M3 - Article
C2 - 30634665
AN - SCOPUS:85060650792
SN - 1999-4923
VL - 11
JO - Pharmaceutics
JF - Pharmaceutics
IS - 1
M1 - 26
ER -