Synthesis, characterization and in vitro studies of celecoxib-loaded poly(ortho ester) nanoparticles targeted for intraocular drug delivery

Mallika Palamoor, Monica Jablonski

Research output: Contribution to journalArticle

14 Citations (Scopus)

Abstract

The present investigation is aimed at improving the ocular bioavailability of a poorly water soluble drug, celecoxib, to offer new options in the treatment of chronic eye diseases, such as age-related macular degeneration and diabetic retinopathy. To do so, we developed a novel formulation of drug-loaded poly(ortho ester) nanoparticles (NPs). We characterized the NPs in terms of size, morphology, controlled-release, degradation and cytocompatibity. Stable and transparent NP emulsions were prepared following a double emulsion solvent diffusion method employing poloxamer 188 as a stabilizer. Physical properties showed a narrow range size distribution of 151-164. nm with spherical morphology, negative zeta potentials and remarkably high celecoxib encapsulation efficiency (98%) and loading (64%) of poly(ortho ester) NPs. Drug release followed a zero-order release by a surface erosion-controlled mechanism without any burst effect. Degradation of poly(ortho ester) NPs was observed by measuring the concentration of initial degradation product such as, lactic acid. MTT studies revealed minimal toxicity of NPs (up to 1. mg/ml) toward HEK 293 cells. Poly(ortho ester) NPs were not internalized by either Müller or HEK 293 cells, which is highly desirable for a drug carrier to deliver the drugs for prolonged periods to the back of eye. These features have the potential to decrease the number of intraocular injections required to treat chronic eye diseases.

Original languageEnglish (US)
Pages (from-to)474-482
Number of pages9
JournalColloids and Surfaces B: Biointerfaces
Volume112
DOIs
StatePublished - Dec 1 2013

Fingerprint

Celecoxib
Drug delivery
Nanoparticles
esters
delivery
Esters
drugs
nanoparticles
synthesis
Pharmaceutical Preparations
eye diseases
Eye Diseases
HEK293 Cells
degradation
Emulsions
Degradation
emulsions
Chronic Disease
Intraocular Injections
Stabilizers (agents)

All Science Journal Classification (ASJC) codes

  • Biotechnology
  • Surfaces and Interfaces
  • Physical and Theoretical Chemistry
  • Colloid and Surface Chemistry

Cite this

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abstract = "The present investigation is aimed at improving the ocular bioavailability of a poorly water soluble drug, celecoxib, to offer new options in the treatment of chronic eye diseases, such as age-related macular degeneration and diabetic retinopathy. To do so, we developed a novel formulation of drug-loaded poly(ortho ester) nanoparticles (NPs). We characterized the NPs in terms of size, morphology, controlled-release, degradation and cytocompatibity. Stable and transparent NP emulsions were prepared following a double emulsion solvent diffusion method employing poloxamer 188 as a stabilizer. Physical properties showed a narrow range size distribution of 151-164. nm with spherical morphology, negative zeta potentials and remarkably high celecoxib encapsulation efficiency (98{\%}) and loading (64{\%}) of poly(ortho ester) NPs. Drug release followed a zero-order release by a surface erosion-controlled mechanism without any burst effect. Degradation of poly(ortho ester) NPs was observed by measuring the concentration of initial degradation product such as, lactic acid. MTT studies revealed minimal toxicity of NPs (up to 1. mg/ml) toward HEK 293 cells. Poly(ortho ester) NPs were not internalized by either M{\"u}ller or HEK 293 cells, which is highly desirable for a drug carrier to deliver the drugs for prolonged periods to the back of eye. These features have the potential to decrease the number of intraocular injections required to treat chronic eye diseases.",
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