Stability and Ocular Pharmacokinetics of Celecoxib-Loaded Nanoparticles Topical Ophthalmic Formulations

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

Research output: Contribution to journalArticle

9 Citations (Scopus)

Abstract

A spontaneous emulsification and/or solvent diffusion method was used for the preparation of celecoxib-loaded nanoparticles (NPs) using polymers, including chitosan (CS), sodium alginate, poly-ε-caprolactone (PCL), poly-L-lactide, and poly-D,L-lactide-co-glycolide. NPs were incorporated into vehicles (eye drops, in situ gelling system, and gel). Formulations were subjected to an accelerated stability study by storing them at elevated temperatures of 30, 35, and 45°C for 6 months. Formulations were evaluated monthly for general appearance, pH, viscosity, particle size, polydispersity index, zeta potential, and drug content. Gels containing CS-NPs and PCL-NPs were selected for an ocular pharmacokinetics study using Sprague-Dawley rats due to their high stability and long shelf lives (24.56 and 33.76 months, respectively). The gel improved NP stability by keeping it inside its network structure, which protected them from aggregation and interacting with water. Our formulations improved celecoxib bioavailability due to their bioadhesivness, thus preventing their rapid removal. Also, NPs acted as drug reservoirs that adhered to eye surface and continuously released the drug. The availability of celecoxib in all eye tissues and its absence in plasma suggests that our formulation could be used for anterior eye disorders and also for treatment of diseases associated with the posterior eye with no systemic side effects.

Original languageEnglish (US)
Pages (from-to)3691-3701
Number of pages11
JournalJournal of Pharmaceutical Sciences
Volume105
Issue number12
DOIs
StatePublished - Dec 1 2016

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Celecoxib
Nanoparticles
Pharmacokinetics
Gels
Chitosan
Pharmaceutical Preparations
Ophthalmic Solutions
Particle Size
Viscosity
Biological Availability
Sprague Dawley Rats
Polymers

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Stability and Ocular Pharmacokinetics of Celecoxib-Loaded Nanoparticles Topical Ophthalmic Formulations. / Ibrahim, Mohammed Mostafa; Abd-Elgawad, Abd Elgawad Helmy; Soliman, Osama Abd Elazeem; Jablonski, Monica.

In: Journal of Pharmaceutical Sciences, Vol. 105, No. 12, 01.12.2016, p. 3691-3701.

Research output: Contribution to journalArticle

Ibrahim, Mohammed Mostafa ; Abd-Elgawad, Abd Elgawad Helmy ; Soliman, Osama Abd Elazeem ; Jablonski, Monica. / Stability and Ocular Pharmacokinetics of Celecoxib-Loaded Nanoparticles Topical Ophthalmic Formulations. In: Journal of Pharmaceutical Sciences. 2016 ; Vol. 105, No. 12. pp. 3691-3701.
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