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Design, characterization, and evaluation of aceclofenac-loaded Eudragit RS 100 nanoparticulate system for ocular delivery.
- Source :
-
Pharmaceutical development and technology [Pharm Dev Technol] 2019 Mar; Vol. 24 (3), pp. 368-379. Date of Electronic Publication: 2018 Jul 13. - Publication Year :
- 2019
-
Abstract
- The aim of the present study was to develop and evaluate positively charged nanoparticles of aceclofenac for ocular delivery. The nanoparticles were prepared by the nanoprecipitation method using Eudragit RS 100. The optimized nanoparticles were found to have narrow particle size range (238.9 ± 8 nm) with nearly spherical shape, positive zeta potential (40.3 ± 3.8). Higher entrapment efficiency of aceclofenac (94.53 ± 1.0%) with prolonged in vitro drug release profiles was also observed. Powder X-ray diffraction and differential scanning calorimetry studies indicated decrease in crystallinity of drug within the nanoparticulate polymeric matrix. The formulation was found to have higher permeation as compared to aceclofenac aqueous solution. Nanoparticle formulation was found to be quite stable and well tolerated with no signs of corneal damage. The in vivo studies involving the arachidonic acid-induced ocular inflammation in rabbits showed optimal efficacy of the nanoparticles with significantly higher inhibition of polymorphonuclear leukocytes migration (p < 0.05) and lid closure scores.
- Subjects :
- Acrylic Resins chemistry
Administration, Ophthalmic
Animals
Anti-Inflammatory Agents, Non-Steroidal pharmacology
Anti-Inflammatory Agents, Non-Steroidal toxicity
Cell Movement drug effects
Chemistry, Pharmaceutical methods
Crystallization
Diclofenac administration & dosage
Diclofenac pharmacology
Diclofenac toxicity
Disease Models, Animal
Drug Carriers chemistry
Drug Liberation
Drug Stability
Eye Diseases drug therapy
Eye Diseases pathology
Inflammation drug therapy
Inflammation pathology
Neutrophils drug effects
Neutrophils metabolism
Particle Size
Rabbits
Anti-Inflammatory Agents, Non-Steroidal administration & dosage
Diclofenac analogs & derivatives
Drug Delivery Systems
Nanoparticles
Subjects
Details
- Language :
- English
- ISSN :
- 1097-9867
- Volume :
- 24
- Issue :
- 3
- Database :
- MEDLINE
- Journal :
- Pharmaceutical development and technology
- Publication Type :
- Academic Journal
- Accession number :
- 29897843
- Full Text :
- https://doi.org/10.1080/10837450.2018.1486424