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Table 2 Polymeric- and lipid-based conjugated NPs as carriers of ophthalmic substances

From: Nanoparticles for the treatment of glaucoma-associated neuroinflammation

Nanoparticle’s formulation Substances Size of NPs (nm) Surface charge (mV) Route of delivery Platform Advantages Refs.
Polymeric-based NPs
 PLGA Sparfloxacin 181 to 232 + 22 Topical instillation (nanosuspension) In vitro
In vivo
Reduced IOP, improved precorneal residence time, enhanced ocular penetration, and good eye tolerance [231]
 PLGA coated-chitosan gel Sparfloxacin 181 NR Topical instillation (laden in situ gel) In vivo Reduced IOP, improved drug penetration, promoted sustained drug release, and prolonged drug retention time [232]
 PLA coated-PEG Acyclovir 51.2 to 131.5 − 14.7 Topical instillation (conjunctival sac) In vitro
In vivo
Reduced IOP, prolonged retention time, and improved drug efficacy [233]
 Poly(amidoamine) (PAMAM) coated-PLGA Brimonidine tartrate; timolol maleate 258 − 28.8 Topical instillation In vitro
In vivo
Reduced IOP (≥ 18%), non-toxic, prolonged time, increased drug bioavailability, controlled and slow release (~ 5 weeks) [234]
 PLGA-vitamin E-tocopheryl polyethylene glycol 1000 succinate Brimonidine tartrate 115.72 ± 4.18 − 11.80 ± 2.24 Topical instillation (in situ gel) In vitro
Ex vivo
In vivo
Reduced IOP (~ 8 h), improved precorneal residence time, non-irritant, and sustained corneal release [235]
 PLGA-phosphatidylserine (PSA) (core shell NP) Brinzolamide 571.00 ± 27.02 − 27.45 ± 2.98 Subconjunctival injection In vitro
Ex vivo
In vivo
Reduced IOP, enhanced coronial drug penetration, sustained release, high encapsulation efficiency, and non-toxic [175]
 Chitosan Brimonidine tartrate 270 to 370 + 26.2 to + 29.8 Topical instillation In vitro
In vivo
Reduced IOP, non-irritant and safe, provided mucoadhesive effect, prolonged retention time, and sustained drug release [236]
 Chitosan coated-carbopol Pilocarpine 294 + 55.78 Topical instillation In vitro
In vivo
Prolonged drug release with high bioavailability (unloaded > 90% drug in ~ 4 h) [237]
 Chitosan coated-PLA Rapamycin 300 + 30.3 Topical instillation In vitro
In vivo
High precorneal retention time (50% within 12 h), prolonged drug release, and significant immunosuppressive effects [238]
 Chitosan coated-PLGA Triamcinolone acetonide 334.00 ± 67.95 to 386.00 ± 15.14 + 26 to + 33 Topical instillation In vitro High drug encapsulation (55–57%) and controlled drug released (27 h) [185]
 Chitosan coated-sodium alginate Gatifloxacin 205 to 572 + 17.6 to + 47.8 NR In vitro Rapid drug release in the first hour but prolonged release over 24 h [239]
 Chitosan coated-cyclodextrin Econazole nitrate 90 to 673 + 22 to + 33 Conjunctival sac (instillation) In vitro
In vivo
Prolonged drug release (~ 50% within 8 h) and high bioavailability [240]
 Chitosan-coated sodium alginate/chitosan 5-Fluorouracil 329 to 505 + 18.5 to + 28.9 Topical instillation In vitro
In vivo
Increased drug bioavailability and prolonged release (~ 8 h) [241]
 Lecithin coated-chitosan Natamycin 213 + 43 Conjunctival sac (instillation) In vitro
In vivo
Increased drug retention time (> 64% released over ~ 7 h), reduced clearance, improved mucoadhesive properties, and fewer doses required [242]
 HA-modified chitosan Timolol maleate; dorzolamide hydrochloride 118.4 to 143.9 + 29.0 ± 8.7 Topical instillation In vitro
Ex vivo
In vivo
Reduced IOP, improved mucoadhesive properties (~ 91%), provided controlled drug delivery, slow but sustained release, and non-irritant [243]
 Poly(γ-glutamic acid) (γ-PGA)-l-phenylalanine (-Phe) Dexamethasone 200 − 25 Topical instillation In vitro
In vivo
Efficient drug uptake by cultured macrophages/microglia and inhibited microglia at 24 h post-treatment [244]
 Ethylcellulose Melatonin 147.4 to 179.6 − 25 to − 30 Topical instillation In vivo Greater cornea penetration and RGC survival at 9 days post-treatment [245]
 Eudragit Brimonidine tartrate 143.9 to 702.2 NR Topical instillation In vitro
Ex vivo
In vivo
Reduced IOP (~ 2 to 3 h longer than 1 h of commercialized eye drop) and prolonged drug release [246]
Lipid-based NPs
 SLNs Tobramycin 70 to 80 NR Topical instillation (lower conjunctival sac) In vivo Prolonged drug release and retention (~ 4 h) and high bioavailability [247]
Baicalin 91.42 ± 1.02 − 33.50 ± 1.28 Topical instillation In vitro
In vivo
Prolonged drug release (~ 62% after 3 h and the remaining gradually within 10 h) and high corneal permeability [248]
 SLNs-coated modified Chitosan Methazolamide 143.9 to 702.2 + 31.3 ± 1.7 Topical instillation In vitro
Ex vivo
In vivo
High ocular penetration, sustained drug release (~ 8 h), fewer doses required, and enhanced patients’ adherence [249]
 SLNs modified phospholipids Timolol maleate 37.7 to 47.2 NR NR In vitro
Human cornea construct
Enhanced drug bioavailability and encapsulation rate (> 44%) [250]
 SLN-PEGylated Latanoprost 105 to 132 − 29.1 to − 26.7 Topical (contact lens) In vitro
In vivo
High drug uptake, sustained drug release, and safe [251]
Travoprost 221 to 257 − 27.3 to − 20.4 Topical (contact lens) In vitro
In vivo
High drug uptake, sustained release (> 144 h), safe and non-irritant [178]
 SLN-coated Poloxamer 188 and glycerol monostearate (solid lipid) Chloramphenicol 248 − 8.74 NR In vitro Increased encapsulation efficacy (> 83%) controlled and prolonged drug release (> 48 h) [252]
 SLN-coated glycerol monostearate Bimatoprost 148.4 ± 1.25 − 20.8 to − 14.1 Topical instillation (in situ gel) In vitro
Ex vivo
In vivo
Prolonged drug release, increase in precorneal residence time, non-irritant, safe with low corneal toxicity, and stable (> 1 month) [253]
 SLNs-coated Compritol 888 Indomethacin 140 ± 5 + 21.0 ± 1.8 NR In vitro Increased drug stability, encapsulation (72%), and corneal permeability; stable (> 1 month) [254]
 NLCs Mangiferin 51.39 − 36.5 ± 1.5 Probe implantation In vitro
In vivo
Prolonged drug release (~ 3 months), increased corneal permeability and pericorneal retention time, high encapsulation efficacy (> 88%), and bioavailability [255]
Brimonidine 100 to 140 − 31.1 to − 33.7 Topical (contact lens) In vitro
In vivo
High drug uptake, sustained release (> 144 h), and safe [177]
 NLCs coated-Lutrol F 68 (surfactant), squalene (lipid) and Precirol ATO 5 (lipid) Triamcinolone 198.73 − 29.30 to − 45.60 Conjunctival sac (instillation) In vivo No signs of ocular toxicity and improved encapsulation efficacy (94.82 ± 1.12%) [256]
 NLCs-coated Miglyol 812, castor oil, and stearic acid (lipid) Flurbiprofen 228.3 − 33.3 Topical instillation In vitro
In vivo
Prolonged drug release, high encapsulation efficacy (~ 90%) and minimal irritation [257]
 NLCs-coated Chitosan, with ethanol (co-surfactant), Tween 80 (surfactant), oleic acid (liquid lipid), and Compritol HD 5 ATO (solid lipid) Ofloxacin 244 − 4.630 ± 0.259 Topical (Ocular inserts in cul de sac) In vitro, microbiological test
Ex vivo
In vivo
Enhanced precorneal permeation, retention time (~ 24 h) and enhanced drug efficacy, and reduced frequency application [258]
 Lipid NPs coated-phospholipids Diclofenac sodium 276 − 12 to − 42.6 NR In vitro
Human cornea construct
Increased drug encapsulation (~ 94%), corneal penetration, and prolonged drug release [259]
 Lipoamino acid-modified NPs Connexin43 mimetic peptide NR NR Intravitreal injection In vivo Enhanced neuroprotection after retinal ischemia [260]
  1. ATO = atomic grade; IOP = intraocular pressure; NPs = nanoparticles; NR = not reported; PEG = poly(ethylene glycol); PLA = poly(lactic) acid; PLGA = poly lactic-co-glycolic acid; NLCs = nanostructured lipid carriers; SLN = solid lipid NPs