Design and elaboration of freeze-dried PLGA nanoparticles for the transcorneal permeation of carprofen: Ocular anti-inflammatory applications

[Display omitted] •Central rotatable composite design 23+ star was performed for nanoparticles design.•PLGA nanoparticles were elaborated by the solvent displacement technique.•Optimized carprofen ocular nanoparticles were lyophilized and sterilized.•All studied confirmed no ocular irritation or tox...

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Bibliographic Details
Published in:Colloids and surfaces, B, Biointerfaces B, Biointerfaces, 2015-12, Vol.136, p.935-943
Main Authors: Parra, Alexander, Mallandrich, Mireia, Clares, Beatriz, Egea, María A., Espina, Marta, García, María L., Calpena, Ana C.
Format: Article
Language:English
Subjects:
Animals
Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics
Biomedical materials
Carbazoles - pharmacokinetics
Carprofen
Cornea - metabolism
Design engineering
Effectiveness
Eye surgery
Factorial design
Freeze Drying
In vivo testing
In vivo tests
Lactic Acid - chemistry
Male
Microscopy, Electron, Transmission
Nanoparticles
Penetration
Permeation
PLGA
Polyglycolic Acid - chemistry
Rabbits
Surgical implants
X-Ray Diffraction
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Summary:[Display omitted] •Central rotatable composite design 23+ star was performed for nanoparticles design.•PLGA nanoparticles were elaborated by the solvent displacement technique.•Optimized carprofen ocular nanoparticles were lyophilized and sterilized.•All studied confirmed no ocular irritation or toxicity of nanoparticles.•In vivo studies showed successful ocular anti-inflammatory efficacy. This work aimed the design and development of poly(lactic-co-glycolic) acid (PLGA) nanoparticles (NPs) for the ocular delivery of Carprofen (CP) by a central rotatable composite design 23+ star. NPs showed adequate size for ocular administration (189.50±1.67nm), low polydispersity (0.01±0.01), negative charge surface (–22.80±0.66mV) and optimal entrapment efficiency (74.70±0.95%). Physicochemical analysis confirmed that CP was dispersed inside the NPs. The drug release followed a first order kinetic model providing greater sustained CP release after lyophilization. Ex vivo permeation analysis through isolated rabbit cornea revealed that a sufficient amount of CP was retained in the tissue avoiding excessive permeation and thus, potential systemic levels. Ex vivo ocular tolerance results showed no signs of ocular irritancy, which was also confirmed by in vivo Draize test. In vivo ocular anti-inflammatory efficacy test confirmed an optimal efficacy of NPs and its potential application in eye surgery.
ISSN:0927-7765
1873-4367
DOI:10.1016/j.colsurfb.2015.10.026