Table 2.
In vivo and in vitro studies of niosomes in ocular drug delivery.
| Disease | Surfactant(s) | Additive(s) | Drug | Production Method(s) | Results | Year, Ref. |
|---|---|---|---|---|---|---|
| Glaucoma | Span 20, 40, 60 Tween 20, 40 |
Cholesterol | Timolol maleate | TFH | Highest EE% found in niosomes prepared with span60 and Tween 40 (>90%), and niosomes prolonged drug release and IOP-lowering activity up to 24 h. | 2020, [28] |
| Span 60 Brij 52 |
Cholesterol Soybean α-lecithin |
Brimonidine tartrate | Proniosome | Highest EE% obtained be span60 formulations (>64%) as compared to brij52 niosomes. Niosomes extended drug release up to 24 h and showed higher IOP-lowering activity than marketed drug. | 2019, [55] | |
| Span 60 | Cholesterol | Dorzolamide HCl | TFH | EE% of remote loaded niosomes was higher (>31%) than passive loaded niosomes, and prolonged drug release more than 8 h was observed. | 2017, [56] | |
| Span 60 | Cholesterol | Atenolol | TFH | Maximum EE% between formulated niosomes was 80.7%. When inside the in situ gel, niosomes prolonged drug release and IOP-lowering activity more than 8 h. | 2014, [57] | |
| Span 60 | Cholesterol | Brimonidine tartrate | TFH | EE% of the niosomes were in >32, and niosomes showed IOP-lowering activity 3 h longer than commercial drug. | 2010, [58] | |
| Span 60 | Cholesterol Chitosan |
Timolol maleate | REV | EE% of niosomes was 24.3%, and niosomes extended drug release more than 10 h and IOP-lowering activity up to 8 h with peak at 3 h. | 2009, [59] | |
| Span 60 | Cholesterol Carbopol |
Acetazolamide | REV | EE% of prepared niosomes was 43.75%, and carbopol coated niosomes showed more sustained and higher IOP-lowering activity than marketed drug. | 2007, [60] | |
| Span 40, 60 | Cholesterol | Acetazolamide | TFH, REV |
Span60:chol (7:6) MLV niosomes are the highest entrapment efficiency (>32%), and these niosomes prolonged IOP-lowering activity compared to Span60:Chol (7:4) MLV niosomes. | 2005, [36] | |
| Span 60 | Cholesterol Chitosan Carbopol |
Timolol maleate | REV | Chitosan coated niosomes formulation showed prolonged decrease in IOP compared to carbopol coated niosomes | 2005, [61] | |
| Conjunctivitis | Span 60 | Cholesterol | Azithromycin-β-CD | SI, TFH, Hand shaking |
EE% of prepared niosomes (>30%) and niosomal in situ gel formulations (>63%) were high, and niosomes prolonged drug release up to 12 h with increased corneal permeation. | 2017, [62] |
| Span 20, 60, 80 Tween 40, 60, 80 |
Cholesterol | Lomefloxacin HCI | TFH | EE% of the tween niosomes (>41%) and drug release rate were higher than spans niosomes (>40%), and niosomal formulation healed the infected eyes better than marketed drug. | 2017, [63] | |
| Span 60 | Cholesterol | Chloramphenicol | SI | EE% of niosomal formulations were >83%, and niosomes prolonged drug release up to 10 h. Niosomes cured disease with less administration than marketed eye drop. | 2012, [64] | |
| Fungal keratitis | Span 60 | Cholesterol Dicetyl phospate N-Trimethyl chitosan |
Natamycin | TFH | Both uncoated and TMC coated niosomes extended drug release up to 12 h., and TMC coated niosomes are higher mucoadhesion and corneal permeability than uncoated niosomes. | 2019, [65] |
| Span 60 | Cholesterol Chitosan |
Fluconazole-hydroxypropyl-β-CD | TFH | EE% of the chitosan-coated niosomes were 61.7%, and chitosan coated niosomes prolonged drug release up to 24 h. | 2019, [66] | |
| Span 60 | Cholesterol | Natamycin | TFH | EE% of niosome formulations were high (>65%), and niosomes extended drug release up to 24 h with increased corneal permeation. | 2017, [67] | |
| Span 40, 60 | Cholesterol Pluronic L64 Pluronic F127 |
Voriconazole | TFH | EE% of the prepared formulations was >49%, also niosomes and niosomal in situ gel formulations prolonged drug release up to 8 h. | 2016, [68] | |
| Span 60, 80 | Cholesterol | Fluconazole | TFH | Span60:chol (2:1) niosomes had the highest EE% (>84%) and better release kinetics. Niosome incorporated into poloxamer gel showed better antifungal activity than niosomes incorporated into chitosan gel. | 2016, [69] | |
| Span 60 | Cholesterol Bile salts Edge activator |
Tercanazole | SI | Increased edge activator concentration was decreased EE% of niosomes, and selected formulation had EE% of 95.47%. Niosomes increased corneal permeation of drug. | 2016, [70] | |
| Span 40, 60, 80 | Edge activators Cholesterol |
Fluconazole | SI | In the prepared formulations highest EE% was 65.73%, and corneal permeation of niosomes were higher than marketed drug. | 2012, [71] | |
| Genetic retinal disorders | Tween 80 Poloxamer 188 |
Chloroquine (CQ) Cationic lipid 2,3-di(tetra decyloxy)propan-1-amine |
pCMS-EGFP plasmid |
REV | Transfection efficiency of pristine nioplexes was higher than CQ-nioplexes but efficiency of both nioplexes were lower compared to Lipofectamine 2000, and CQ-nioplexes transfected cells in inner layers of retina. | 2019, [72] |
| Tween 20, 80, 85 | Cationic lipid DOTMA Squalene |
pCMS-EGFP reporter plasmid |
REV | Cell viability was higher for nioplexes transfected cells, but transfection efficiency was lower compared to Lipofectamine 2000, and Tween 20 nioplexes was the highest transfection efficiency (>24.5%) for ARPE-19 cells | 2018, [38] | |
| Tween 60 | Lycopene Cationic lipid DOTMA |
pCMS-EGFP plasmid |
REV | Lycopene was increased transfection efficiency of nioplexes, but the efficiency was lower than lipofectamine 2000. Nioplexes were transfected cells in inner layers of retina. | 2017, [73] | |
| Tween 80 | Cationic lipid 2,3-di(tetradecyloxy)propan-1-amine Squalene |
pCMS-EGFP plasmid |
REV | Cell viability was higher for nioplexes compared to Lipofectamine 2000. in vivo transfection was depending administration route; subretinal injection transfected RPE layer cells but intravitreal injection transfected cells in inner layers of retina. |
2014, [74] | |
| Corneal graft rejection | Span 60 Tween 80 |
Hyaluronic acid | Cyclosporine A | SI | HA-coated elastic niosomes had EE% of >92%, and HA-coated formulations were higher corneal permeability than drug emulsion and Span60 niosomes. | 2019, [75] |
| Poloxamer 188 Soybean phophadithylcoline |
Cholesterol Hyaluronic acid |
Tacrolimus (FK506) | Proniosome | HA improved the mucoadhesion niosomes, prolonged the residency of drug, and decreased clearance rate of drug in aqueous humor. | 2016, [54] | |
| Poloxamer 188 Lecithin |
Cholesterol | Tacrolimus (FK506) | Proniosome | Drug loaded with EE% of 95.32%, and niosomes enhanced the precorneal permeation with prolonged corneal graft survival | 2014, [76] | |
| Ocular infections | Span 60 Tween 40 |
Cholesterol | Vancomycin | TFH | EE% of niosomes was >46%, and niosomes prolonged drug release more than 24 h with increased antibacterial activity. | 2019, [77] |
| Span 20, 60, 80 | Cholesterol | Lomefloxacin HCI | TFH | Drug EE% of niosomes were >78.1%, and niosomes prolonged drug release up to 8 h with higher antimicrobial activity than free drug. | 2017, [78] | |
| Span 60 | Cholesterol Chitosan |
Gatifloxacin | SI | EE% of chitosan coated niosomes was >68.9%, and chitosan coating was further improved corneal permeability of niosomes | 2015, [79] | |
| Tween 60, 80 Brij 35 |
Cholesterol Dicetyl phospate |
Gentamicin sulfate | TFH | Drug EE% of prepared niosomes was changed in wide range, but all of the niosomes prolonged drug release up to 8 h. | 2008, [80] | |
| Ocular surface diseases | Span 20, 60, 80 Tween 60 |
Cholesterol | Doxycycline hyclate | TFH with extrusion, REV |
Span60 niosomes had the highest EE% (>50%), and niosomes extended release of drug more than 20 h. | 2019, [81] |
| Ocular inflammation | Span 60 | Cholesterol | Flurbiprofen | TFH | Niosomal in situ gel formulation extended drug release more than 7 h and maintained drug concentration in the aqueous humor up to 12 h. | 2016, [82] |
| Span 60 | Cholesterol Ethanol |
Prednisolone | TFH, SI |
EE% of niosomes prepared by TFH was higher than SI, and niosomes extended drug release up to 8 h. Also, niosomes decreased the inflammation more than drug solution. | 2014, [83] | |
| Diabetic keratopathy | Span 60 Solulan C24 Sodium cholate |
Cholesterol Dicetyl phospate |
Naltrexone | REV | All of the niosomal formulations showed no irritation and have good corneal tolerability. | 2012, [84] |
| Span 60 Solulan C24 Sodium cholate |
DCP Stearyl amine Cholesterol |
Naltrexone | TFH, REV, DRV, Freeze/thaw |
EE% of niosomes prepared from different methods compared, and Rev. niosomes showed highest EE%, and niosomes prolonged drug release up to 12 h. | 2011, [42] |
Abbreviations: Thin-film hydration method (TFH); reverse phase evaporation method (REV); dehydration–rehydration vesicles method (DRV); solvent injection method (SI); dicetylphosphate (DCP); cyclodextrin (CD); hyaluronic acid (HA); voriconazole (VCZ); N-Trimethyl chitosan (TMC); chloroquine (CQ); encapsulation efficiency (EE%); brimonidine tartrate (BRT); intraocular pressure (IOP); retinal pigment epithelium (RPE); cholesterol (chol).