Online citations, reference lists, and bibliographies.
← Back to Search

Formulation And Evaluation Of Neuroactive Drug Loaded Chitosan Nanoparticle For Nose To Brain Delivery: In-vitro Characterization And In-vivo Behavior Study.

M. Qureshi, M. Aqil, S. S. Imam, A. Ahad, Y. Sultana
Published 2019 · Chemistry, Medicine

Cite This
Download PDF
Analyze on Scholarcy
BACKGROUND The present work was designed to explore the efficacy of neuroactive drug (risperidone) loaded chitosan lipid nanoparticle (RIS-CH-LNPs) to enhance the bioactivity in schizophrenia via the nasal route. METHODS The three-factor and three-level formulation by design approach was used for optimization and their effects were observed on (Y1) size in nm, (Y2) % drug loading, and (Y3) % drug release. The optimized formulation RIS-CH-LNPopt was further evaluated for its surface morphology, ex-vivo permeation study, in-vivo behavior study, and stability study. The developed RIS-CH-LNPs showed nanometric size range with high drug loading and prolonged drug release. RESULTS The optimized formulation (RIS-CH-LNPopt) has shown the particle size (132.7 nm), drug loading (7.6 %), drug release (80.7 %) and further ex-vivo permeation study showed 2.32 fold enhancement over RIS-SUS(suspension). In-vivo behavior studies showed that RIS-CH-LNPopt is able to show significant greater bioefficacy as compared to RIS-SUS [intranasal (i.n), intravenous (i.v)]. The pharmacokinetic and brain/plasma ratio of developed chitosan nanoparticle was higher at all time-points as compared to RIS-SUS either given by intranasal or intravenous route that proves the direct nose to brain transport pathway of the drug via nasal administration. The developed chitosan nanoparticle increases nose to brain drug delivery as compared to the dispersion of equivalent dose. CONCLUSION The findings of this study substantiate the existence of a direct nose-to-brain delivery route for RIS-CH-LNPs.
This paper references
Optimization of mobile phase by 32-mixture design for the validation and quantification of risperidone in bulk and pharmaceutical formulations using RP-HPLC
S. S. Imam (2014)
Drug delivery to the central nervous system: a review.
A. Misra (2003)
Direct nose to brain drug delivery via integrated nerve pathways bypassing the blood–brain barrier: an excellent platform for brain targeting
C. Pardeshi (2013)
The blood-brain barrier in brain homeostasis and neurological diseases.
N. Weiss (2009)
Chitosan in nasal delivery systems for therapeutic drugs.
L. Casettari (2014)
Nanostructured lipid carriers as a potential vehicle for Carvedilol delivery: Application of factorial design approach
G. B. Patil (2016)
Formulation by design-based proniosome for accentuated transdermal delivery of risperidone: in vitro characterization and in vivo pharmacokinetic study
S. S. Imam (2015)
Formulation and optimization of lacidipine loaded niosomal gel for transdermal delivery: In-vitro characterization and in-vivo activity.
Mohd Qumbar (2017)
Brain Targeting of Temozolomide via the Intranasal Route Using Lipid-Based Nanoparticles: Brain Pharmacokinetic and Scintigraphic Analyses.
Anam Khan (2016)
"Application of Box-Behnken design for optimization and development of quetiapine fumarate loaded chitosan nanoparticles for brain delivery via intranasal route* ".
B. Shah (2016)
Modulatory effects of PLG and its peptidomimetics on haloperidol-induced catalepsy in rats
W. Costain (1999)
Nanostructured lipid carriers for parenteral delivery of silybin: Biodistribution and pharmacokinetic studies.
Lejiao Jia (2010)
Nose to Brain Targeting Potential of a ChitosanCoated Nano-Formulation: Pharmacodynamic and Pharmacoscintigraphic Evaluation
G. Mustafa (2013)
Bioadhesion of hydrated chitosans: An in vitro and in vivo study
I. Henriksen (1996)
Nasal Delivery of High Molecular Weight Drugs
Y. Ozsoy (2009)
The measurement of the influence of drugs on voluntary activity in mice.
P. Dews (1953)
Mapping Early Brain Development in Autism
E. Courchesne (2007)
Nanomedicine therapeutic approaches to overcome cancer drug resistance.
Janet L Markman (2013)
The antimicrobial activity of nanoparticles: present situation and prospects for the future
L. Wang (2017)
Nanoparticles for direct nose-to-brain delivery of drugs.
Alpesh Mistry (2009)
Analysis of Fickian and non-Fickian drug release from polymers.
N. Peppas (1985)
Pramipexole dihydrochloride loaded chitosan nanoparticles for nose to brain delivery: Development, characterization and in vivo anti-Parkinson activity.
Ruhi Raj (2018)
A review of nanocarrier-based CNS delivery systems.
S. Tiwari (2006)
Preparation and Characterization of Chitosan Microspheres Containing Doxifluridine
T. Yoshino (2003)
The big picture on nanomedicine: the state of investigational and approved nanomedicine products.
M. Etheridge (2013)
Adenosine antagonists reverse the cataleptic effects of haloperidol: Implications for the treatment of Parkinson's disease
J. Trevitt (2009)
Modeling and comparison of dissolution profiles.
P. Costa (2001)
Quality by design approach of a pharmaceutical gel manufacturing process, part 2: near infrared monitoring of composition and physical parameters.
J. Rosas (2011)
Formulation by design based risperidone nano soft lipid vesicle as a new strategy for enhanced transdermal drug delivery: In-vitro characterization, and in-vivo appraisal.
S. S. Imam (2017)
Application of Box-Behnken design for preparation of levofloxacin-loaded stearic acid solid lipid nanoparticles for ocular delivery: Optimization, in vitro release, ocular tolerance, and antibacterial activity.
Mirza Salman Baig (2016)
Quality by design approach of a pharmaceutical gel manufacturing process, part 1: determination of the design space.
J. Rosas (2011)
Nanostructured Lipid Carrier Containing CNS Acting Drug: Formulation, Optimization and Evaluation
M. I. Alam (2011)
Optimization and in vitro toxicity evaluation of G4 PAMAM dendrimer-risperidone complexes.
M. J. Prieto (2011)
Intranasal Piperine-Loaded Chitosan Nanoparticles as Brain-Targeted Therapy in Alzheimer's Disease: Optimization, Biological Efficacy, and Potential Toxicity.
Y. Elnaggar (2015)
Temozolomide loaded nano lipid based chitosan hydrogel for nose to brain delivery: Characterization, nasal absorption, histopathology and cell line study.
Anam Khan (2018)
Is nose‐to‐brain transport of drugs in man a reality?
L. Illum (2004)
Functionalization of Carbon Microcoils by Platinum-Loading Through Dendrimer Binder
A. Siriviriyanun (2013)
Evaluation of neuropeptide loaded trimethyl chitosan nanoparticles for nose to brain delivery.
M. Kumar (2013)
Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN) versus drug nanocrystals.
R. Mueller (2006)
Intranasal nanoemulsion based brain targeting drug delivery system of risperidone.
M. Kumar (2008)
Intranasal delivery: physicochemical and therapeutic aspects.
H. Costantino (2007)
Nasal Absorption Enhancers for Biosynthetic Human Growth Hormone in Rats
D. O'hagan (2004)
Challenges and strategies in anti-cancer nanomedicine development: An industry perspective.
J. I. Hare (2017)
Brain delivery of valproic acid via intranasal administration of nanostructured lipid carriers: in vivo pharmacodynamic studies using rat electroshock model
S. Eskandari (2011)
Formulation of sitagliptin-loaded oral polymeric nano scaffold: process parameters evaluation and enhanced anti-diabetic performance
Mohammed Asadullah Jahangir (2018)

This paper is referenced by
Semantic Scholar Logo Some data provided by SemanticScholar