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. 2021 Mar 10;9(2):e00723. doi: 10.1002/prp2.723

TABLE 1.

Polymeric nanoparticles for delivery of anti‐VEGF agents

Active molecule Main polymer Nanoparticulate system Components Mean particle size (nm) Main results in ocular delivery Preparation method Refs.
Bevacizumab and dexamethasone PLGA PLGA‐nanoparticles

PLGA and polyethylenimine

PVA

 190–222

  • in vitro sustained release

  • Enhanced efficacy inhibiting tube formation and VEGF secretion in HUVEC.

  • Increased antiangiogenic efficacy of choroidal neovascularization in a rabbit model

 Emulsion‐solvent evaporation 107
Bevacizumab PLGA and Chitosan Chitosan‐coated PLGA nanoparticles PLGA, chitosan and

222

  • Increased drug transscleral permeation (ex vivo, goat)

  • Enhanced bioadhesion in pig mucin suspension

 Emulsion‐solvent evaporation 108
Bevacizumab PLGA PLGA‐nanoparticles PLGA, ethyl acetate and PVA 198

  • pH‐dependent bevacizumab release (in vitro)

Double‐emulsion solvent evaporation 103, 111
Bevacizumab PLGA PLGA‐albumin nanoparticles PLGA, PVA and albumin

  • Sustained release formulation of bevacizumab for about 2 months, after intravitreal injection in rabbits

  • Increased half‐life of drug in rabbit vitreous and aqueous humor

 Double‐emulsion solvent evaporation 106, 113
Bevacizumab PLGA PLGA‐nanoparticles PLGA, PVA and Tween® 80 133

  • in vitro sustained drug release

  • Increased half‐life of drug in mice vitreous and aqueous humor

  • Enhanced antiangiogenic properties in HUVEC

  • Enhanced antiangiogenic efficacy in an oxygen‐induced retinopathy mice model and a corneal neovascularization mice model

 Double‐emulsion solvent evaporation 109
Bevacizumab PLGA Nanoparticles in porous microparticles PLGA and PVA 265

  • in vitro sustained release

  • in vivo sustained release and high drug levels in vitreous humor at 2 months after intravitreal injection in a rat model

 Emulsion‐solvent evaporation 110
Bevacizumab Mesoporous silica Mesoporous silica nanoparticles

Tetraethyl orthosilicate, cetyltrimethylammonium chloride, triethanolamine,3‐aminopropyltriethoxysilane (3‐aminopropyl) triethoxysilane, and mPEG‐succinimidyl carboxymethyl ester

 140

  • Prolonged drug residency in vitreous and aqueous humor

  • Enhanced antiangiogenic properties in HUVEC

  • Enhanced antiangiogenic efficacy in an alkaline burn‐induced corneal neovascularization mice model and an oxygen‐induced retinopathy model

 Nanocasting 114
Ranibizumab PLGA‐PEG copolymer PLGA‐PEGylated magnetic nanoparticles Iron oxide, PEG and PLGA 5–10

  • Inhibition of the tube formation in HUVEC

Ring opening polymerization, following addition of iron oxide nanoparticles

 115
Bevacizumab Chitosan Chitosan grafted‐polyethylene glycol) methacrylate nanoparticles

Chitosan, polyethylene glycol methacrylate, Tween® 80 and Span® 80

200–900

  • in vitro slow release rate

  • Enhanced efficacy as antiangiogenic in a rabbit model of diabetes

 Double cross‐linking (ionic and covalent) process in reverse emulsion 118
Bevacizumab Chitosan Chitosan nanoparticles Chitosan and tripolyphosphate 188

  • in vitro sustained release

  • High intravitreal drug concentration after subtenon injection in rabbit

 Ionic gelation 119
Bevacizumab Chitosan Chitosan nanoparticles Unspecified 88.9

  • in vivo sustained release after intravitreal injection in rats

  • Inhibition of VEGF expression in retina after an intravitreal injection and longer duration of action in a diabetic retinopathy rat model

 Unspecified 120
Ranibizumab PLGA and chitosan

PLGA microparticles entrapping chitosan nanoparticles

 PLGA, chitosan, hyaluronic acid, among others. 17–350

  • in vitro sustained release

  • Enhanced antiangiogenic properties in HUVEC

 Chitosan crosslinking ‐modified double emulsion method 122
Bevacizumab Human serum albumin Human serum albumin nanoparticles Human serum albumin and glutaraldehyde 310

  • in vitro sustained release

  • Formulation is remained in the eye for more than 4 hours post‐topical administration

  • Improved antiangiogenic efficacy in a rat corneal neovascularization model

 Desolvation followed by freeze‐drying 123, 124
Bevacizumab and suramin Human serum albumin Human serum albumin nanoparticles Human serum albumin, glutaraldehyde and Gantrez® ES‐425 158–210

  • in vitro sustained release

 Desolvation 125

Abbreviations: HUVEC, Human umbilical vein endothelial cells; PEG, polyethylene glycol; PLGA, poly(lactide‐co‐glycolic acid; PVA, polyvinyl alcohol; VEGF, vascular endothelial growth factor.