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] |