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. 2019 Aug;24(8):1637–1643. doi: 10.1016/j.drudis.2019.03.004

Table 1.

Examples of nanoparticle application for intraocular drug delivery

Adm. route DDS Carrier composition Cargo Effect
Topical Polymeric nanoparticles [40] PLGA and PEG Dorzolamide • 2x increase in therapeutic duration
• 35% more effect in intraocular pressure (IOP) decrease
Solid lipid nanoparticles (SLN) [41] Stearic acid, Epikuron™ 200, sodium taurocholate Trobramycin • Higher drug conc. in all ocular tissues
• Greater bactericidal activity against intracellular Pseudomonas aeruginosa
Solubilising nanoparticles [23] γ-Cyclodextrin Dexamethasone, dorzolamide • Enhanced residence time on the eye surface
• Enhanced solubility in the tear fluid
• Up to about tenfold enhancement in bioavailability
Niosomes [42] Span 60, cholesterol, ethanol Prednisolone sodium phosphate • Ocular bioavailability 1.75x greater
• Healing time 2x faster
• Significantly less IOP elevation as side effect
Liposomes [43] Soybean phosphatidylcholine, cholesterol Timolol maleate • Longer retention time on corneal surface
• Faster reduction in IOP

Intravitreal Polymeric nanoparticles [19] Light-sensitive polymers Nintedanib (BIBF1120) • Carrier can release cargo up to 30 weeks post-intravitreal injection
• Release can be controlled by irradiation
SLN [44] Precirol® ATO5, DOTAP, Tween® 80, protamine, dextran Human Rs1 gene • Higher transfection level in photoreceptors
• Significant structural improvement in retinal layer
Niosomes [45] Cationic lipid, squalene, polysorbate 80 pCMSEGFP plasmid • Successfully transfected HEK-293 and ARPE-19 cells without affecting viability
Liposomes [46] Cholesterol derivatives, PEG, l-α-phosphatidylcholine Doxorubicin • Significantly improve drug stability
• More drug cargo delivered to retina

Systemic Polymeric nanoparticles [47] PLGA, tripeptide adhesion motif Arg-Gly-Asp (RGD) Flt23k plasmids • RGD modified nanoparticles localised in choroidal neovascularization (CNV) lesions
• No secondary CNV lesions in treated mice
• Vision function is restored exclusively after treatment
SLN [41] Stearic acid, Epikuron™ 200, sodium taurocholate Trobramycin • Using SLN, drug concentration after 1–3 h from intravenous administration is 10 x higher than those without SLN
Liposomes [48] Soybean phosphatidylcholine, cholesterol, glutathione-PEG Methylprednisolone hemisuccinate • Improved efficacy in a model of ocular inflammation
• Protection from experimental autoimmune uveitis
Liposomes [9] Soybean phosphatidylcholine, cholesterol, glutathione-PEG Cyclic nucleotide analogue CN03 • Neuroprotection of photoreceptors in three different animal models for retinal degeneration
• Preservation of cone photoreceptor function