Nanoparticle-based topical ophthalmic formulations for sustained celecoxib release

Mohammed Mostafa Ibrahim, Abd Elgawad Helmy Abd-Elgawad, Osama Abd Elazeem Soliman, Monica Jablonski

Research output: Contribution to journalArticle

33 Citations (Scopus)

Abstract

Celecoxib-loaded NPs were prepared from biodegradable polymers such as poly-ε-caprolactone (PCL), poly(l-lactide) (PLA), and poly(d,l-lactide-co-glycolide) (PLGA) by spontaneous emulsification solvent diffusion method. Different concentrations of polymers, emulsifier, and cosurfactants were used for formulation optimization. Nanoparticles (NPs) were characterized regarding their particle size, PDI, zeta potential, shape, morphology, and drug content. Celecoxib-loaded NPs were incorporated into eye drops, in situ gelling system, and gel and characterized regarding their pH, viscosity, uniformity of drug content, in vitro release, and cytotoxicity. The results of optimized celecoxib-loaded PCL-, PLGA-, and PLA-NPs, respectively, are particle size 119 ± 4, 126.67 ± 7.08, and 135.33 ± 4.15nm; zeta potential -22.43 ± 2.91, -25.46 ± 2.35, and -31.81 ± 2.54mV; and encapsulation efficiency 93.44 ± 3.6%, 86.00 ± 1.67%, and 79.04 ± 2.6%. TEM analyses revealed that NPs have spherical shapes with dense core and distinct coat. Formulations possessed uniform drug content with pH and viscosity compatible with the eye. Formulations showed sustained release without any burst effect with the Higuchi non-Fickian diffusion mechanism. Cytotoxicity studies revealed that all formulations are nontoxic. Our formulations provide a great deal of flexibility to formulation scientist whereby sizes and zeta potentials of our NPs can be tuned to suit the need using scalable and robust methodologies. These formulations can thus serve as a potential drug delivery system for both anterior and posterior eye diseases.

Original languageEnglish (US)
Pages (from-to)1036-1053
Number of pages18
JournalJournal of Pharmaceutical Sciences
Volume102
Issue number3
DOIs
StatePublished - Jan 1 2013

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Celecoxib
Nanoparticles
Particle Size
Viscosity
Polymers
Pharmaceutical Preparations
Eye Diseases
Ophthalmic Solutions
Drug Delivery Systems
Gels

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Nanoparticle-based topical ophthalmic formulations for sustained celecoxib release. / Ibrahim, Mohammed Mostafa; Abd-Elgawad, Abd Elgawad Helmy; Soliman, Osama Abd Elazeem; Jablonski, Monica.

In: Journal of Pharmaceutical Sciences, Vol. 102, No. 3, 01.01.2013, p. 1036-1053.

Research output: Contribution to journalArticle

Ibrahim, Mohammed Mostafa ; Abd-Elgawad, Abd Elgawad Helmy ; Soliman, Osama Abd Elazeem ; Jablonski, Monica. / Nanoparticle-based topical ophthalmic formulations for sustained celecoxib release. In: Journal of Pharmaceutical Sciences. 2013 ; Vol. 102, No. 3. pp. 1036-1053.
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