NDLI: Novel surface modified polymer–lipid hybrid nanoparticles as intranasal carriers for ropinirole hydrochloride: in vitro, ex vivo and in vivo pharmacodynamic evaluation

Content Provider	Springer Nature Link
Author	Pardeshi, Chandrakantsing V. Belgamwar, Veena S. Tekade, Avinash R. Surana, Sanjay J.
Copyright Year	2013
Abstract	Here we report fabrication and evaluation of novel surface modified polymer–lipid hybrid nanoparticles (PLN) as robust carriers for intranasal delivery of ropinirole hydrochloride (ROPI HCl). Sustained release, avoidance of hepatic first pass metabolism, and improved therapeutic efficacy are the major objectives of this experiment. PLN were fabricated by emulsification-solvent diffusion technique and evaluated for physicochemical parameters, in vitro mucoadhesion, in vitro diffusion, ex vivo permeation, mucosal toxicity and stability studies. Box-Behnken experimental design approach has been employed to assess the influence of two independent variables, viz. surfactant (Pluronic F-68) and charge modifier (stearylamine) concentration on particle size, ζ-potential and entrapment efficiency of prepared PLN. Numerical optimization techniques were used for selecting optimized formulation sample, further confirmed by three dimensional response surface plots and regression equations. Results of ANOVA demonstrated the significance of suggested models. DSC and SEM analysis revealed the encapsulation of amorphous form of drug into PLN system, and spherical shape. PLN formulation had shown good retention with no severe signs of damage on integrity of nasal mucosa. Release pattern of drug-loaded sample was best fitted to zero order kinetic model with non-Fickian super case II diffusion mechanism. In vivo pharmacodynamic studies were executed to compare therapeutic efficacy of prepared nasal PLN formulation against marketed oral formulation of same drug. In summary, the PLN could be potentially used as safe and stable carrier for intranasal delivery of ROPI HCl, especially in treatment of Parkinson’s disease.
Starting Page	2101
Ending Page	2115
Page Count	15
File Format	PDF
ISSN	09574530
Journal	Journal of Materials Science: Materials in Medicine
Volume Number	24
Issue Number	9
e-ISSN	15734838
Language	English
Publisher	Springer US
Publisher Date	2013-06-01
Publisher Place	Boston
Access Restriction	Subscribed
Subject Keyword	Biomaterials Polymer Sciences Ceramics, Glass, Composites, Natural Methods Metallic Materials Characterization and Evaluation of Materials Surfaces and Interfaces, Thin Films
Content Type	Text
Resource Type	Article
Subject	Biomaterials Biophysics Bioengineering Biomedical Engineering

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