Ocular drug-delivery systems investigated for anterior segment disorders (inflammation) (Cholkar et al., 2013)

Delivery SystemDrugPolymeric ComponentRemarksReferences
NanoparticlesIbuprofenEudragit RS100Significant improvement of drug bioavailability in rabbit model compared with control aqueous dropsPignatello et al., 2002
FlurbiprofenEudragit RS100Improved ocular bioavailability due to strong interaction between positive charged nanoparticle to the anionic corneal surfacePignatello et al., 2002
FlurbiprofenPLGA, PCLColloidal systems enhance ocular bioavailability; PLGA nanoparticles showed ∼2-fold higher drug transport than that of PCL nanoparticlesValls et al., 2008
IndomethacinPCL, Miglyol 840, poloxamer 188Colloidal formulation shows 3-fold higher ex vivo penetration than commercial eye dropsCalvo et al., 1996
Cyclosporine-AChitosan and cholesterol-conjugated chitosanBoth nanoparticles deliver higher amount of drugs in cornea and conjunctiva as compared with cyclosporine-A suspensionDe Campos et al., 2001
NanomicellesDexamethasonePluronic/chitosan systemNanomicelles entrapping dexamethasone significantly improved bioavailability to anterior ocular tissues by 2.4-fold relative to unformulated dexamethasonePepic et al., 2010
Voclosporin, dexamethasone, rapamycinVitamin E TPGS and octoxynol-40 nanomicellesIn vivo studies showed mixed nanomicellar system have higher bioavailability with topical dosing of dexamethasone and rapamycinPepic et al., 2010
Cyclosporine-AMethoxy poly(ethylene glycol)-hexylsubstituted poly(lactide)Transparent, highly stable, biocompatible formulationDi Tommaso et al., 2011
Plasmid DNA with lacZ genePEO-PPO-PEOSignificant elevation of β-gal activity, transgene expression marker, elevated mRNA levels of bcl-x(L) by 2.2-fold, and reduced corneal apoptosis in mouse and rabbit cornea.Tong et al., 2007
LiposomesC6-ceramideMethoxy PEG(2000) and PEG(750)-C6-ceramideSignificantly efficacious in reducing corneal inflammationSun et al., 2008
DexamethasoneHuman serum albumin; bis(sulfosuccinimidyl) suberate; tris(hydroxymethyl) aminomethane; 3,3-dithiobis-(sulfosuccinimidylpropionate)Significantly higher drug accumulation in the eye (∼13.5 ng/mg tissue) than unformulated drug (2.4 ng/mg tissue)Arakawa et al., 2007
  • PEO-PPO-PEO, poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide); TPGS, tocopheryl polyethylene glycol succinate.