Eudragit RL 100-based nanoparticulate system of aceclofenac for ocular delivery

[Display omitted] ► Aceclofenac loaded Eudragit RL 100 nanoparticles were prepared by nanoprecipitation method. ► Physicochemical properties of the nanoparticles were evaluated. ► The anti-inflammatory activity was determined against arachidonic acid-induced ocular inflammation in rabbits. ► Promisi...

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Bibliographic Details
Published in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2013-03, Vol.103, p.455-462
Main Authors: Katara, Rajesh, Majumdar, Dipak K.
Format: Article
Language:English
Subjects:
Aceclofenac
Acrylic Resins - chemistry
Administration, Ophthalmic
ambient temperature
Animals
Anti-inflammatory
aqueous solutions
Arachidonic Acid
Calorimetry, Differential Scanning
cell movement
Chemistry, Pharmaceutical
colloids
cornea
Cornea - drug effects
crystal structure
Diclofenac - administration & dosage
Diclofenac - analogs & derivatives
Diclofenac - pharmacology
differential scanning calorimetry
Drug Delivery Systems
Drug Stability
drugs
Eye - drug effects
Goats
in vivo studies
inflammation
Inflammation - pathology
Nanoparticle
nanoparticles
Nanoparticles - chemistry
Nanoparticles - ultrastructure
neutrophils
Particle Size
Permeability - drug effects
PMN
Polymers - chemistry
Rabbits
shelf life
Solutions
Spectroscopy, Fourier Transform Infrared
Static Electricity
Surface Properties
Suspensions
X-Ray Diffraction
zeta potential
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Summary:[Display omitted] ► Aceclofenac loaded Eudragit RL 100 nanoparticles were prepared by nanoprecipitation method. ► Physicochemical properties of the nanoparticles were evaluated. ► The anti-inflammatory activity was determined against arachidonic acid-induced ocular inflammation in rabbits. ► Promising in reducing dose frequency and improving patient compliance for ocular delivery. The purpose of this study was to prepare Eudragit RL 100-based nanoparticles of aceclofenac by nanoprecipitation and evaluate the particle size, zeta potential, drug entrapment, particle morphology; in vitro drug release and in vivo efficacy. Change in drug–polymer ratio from 1:5 to 1:20 increased the particle size and entrapment efficiency. The particles showed sustained in vitro drug release which followed the Higuchi square-root kinetics. The results indicate that the nanoparticles release the drug by a combination of dissolution and diffusion. Based on the particle size (134.97nm) and entrapment efficiency (95.73%), the formulation made with 1:10 drug–polymer ratio was selected for further studies. The particles were spherical with a polydispersity index of 0.186 and zeta potential of +30.5mV. Powder X-ray diffraction and differential scanning calorimetry indicated decrease in crystallinity of drug in the nanoparticle formulation. In the in vitro permeation study, the nanoparticle formulation showed 2-fold higher permeation of drug through excised cornea compared to an aqueous solution of drug with no signs of corneal damage. The in vivo studies involving arachidonic acid-induced ocular inflammation in rabbits revealed significantly higher inhibition of polymorphonuclear leukocytes migration (p
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2012.10.056