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. 2023 Jul 22;15(7):2005. doi: 10.3390/pharmaceutics15072005

Table 5.

Liposome preparation methods and potential applications in retinal diseases.

Liposomes Method of the Preparation Characterization Applications Refs.
1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocoline (POPC), DSPE-mPEG2000, DSPE-N-[maleimide (PEG)2000], cholesterol, monocarboxylate Thin-film hydration

  • Monocarboxylate-conjugated liposomes were prepared to achieve high drug uptake of CN04 in the retina for treating retinal degeneration.

  • The liposomes had a particle size of approximately 142–145 nm, with an encapsulation efficiency of more than 75%.

  • The formulation was injected intravitreally into the mouse model.

  • The pyruvate-conjugated liposomes significantly enhanced uptake up to 4-fold in HEK293T cells due to the monocarboxylate transporter conjugated to liposomes.

  • The CN04-loaded liposomes reduced cell death in the rd1 murine retinal degeneration model.

 [140]
DSPE-PEG2000-NHS, DSPE-PEG2000-TAT, egg phosphatidylcholine, cholesterol Thin-film evaporation

  • Intelligent liposomes were developed to efficiently deliver ellagic acid and oxygen into the retinopathy tissue.

  • The liposomes were functionalized with TAT/isoDGR peptides to protect the retinal cells from damage caused by high glucose induction.

  • The formulation was developed to co-deliver ellagic acid and oxygen via intravenous administration or as eye drops.

  • The liposomes blocked the VEGF-p-VEGFR2 signaling pathway.

  • In a DR mouse model, after topically administering the drug-loaded liposomes, downregulation of GFAP and HIF-1α was observed, along with the elimination of ROS in the retina.

 [141]
1,2-oleoyl-3-trimethylammonium-propane (DOTAP), 1,2-dioleoyl-sn-glycero-3-phosphocholine (DOPC), cholesterol, LipoTrust Ex Oligo (short oligonucleotides) Thin-film evaporation

  • SiRNA-loaded cytoplasm-responsive stearylated-peptide was added to the surface of liposomes and prepared to treat retinal diseases such as AMD.

  • The siRNA-loaded liposomes displayed a particle size of approximately 70–80 nm, with an encapsulation efficiency of approximately 80–100%.

  • A non-invasive delivery was developed for siRNA delivery and administered to the rat eye as eyedrops.

  • The intracellular uptake of liposomes was enhanced significantly due to peptides on the liposomal surface, and significant suppression of VEGF expression was observed in rat retinal pigment epithelial cells.

 [142]
DSPC, DOPC, DSPE-PEG2000, 1,2-distearoyl-sn-glycero-3-phosphoglycerol (DSPG) Thin-film hydration

  • A liposomal formulation loaded with sunitinib was developed to treat choroidal neovascularization (CNV) by blocking the signalling pathway through inhibition of the tyrosine kinase of VEGF receptors.

  • The liposomal formulations had a mean particle size of 104 nm, and sunitinib was entrapped efficiently up to 95%.

  • The liposomal formulation was administered intravitreally to the mice.

  • After intravitreal injection, drug-loaded liposomes reduced vascular leakage in the CNV mouse model.

 [143]
Soybean phosphatidylcholine, diacetyl phosphate, cholesterol, chitosan Hydration

  • Chitosan-coated liposomes were prepared and loaded with triamcinolone acetonide (TA) to improve the prognosis of macular edema (ME) in retinal diseases.

  • The drug-loaded liposomes had a mean particle size of approximately 100–105 nm, and the drug was entrapped with an encapsulation efficiency of 98%.

  • TA-loaded chitosan-loaded liposomes were administered to rats as eye drops.

  • The formulation was topically administered as eye drops, and significant therapeutic efficacy in reducing retinal edema was observed.

 [144]
DSPC,DSPE-PEG2000, DSPE-PEG-Mal, cholesterol Reverse-phase evaporation technique

  • Transferrin-conjugated Ganciclovir-loaded liposomes were prepared for cytomegalovirus (CMV) retinitis treatment.

  • The optimized formulation has a particle size lower than 100 nm.

  • The drug-loaded liposomal formulation was developed as an intravitreal injection and topical instillation.

  • Human retinal pigment epithelial (ARPE-19) cells demonstrated good uptake of liposomes via transferrin receptors and inhibited the CMV-infected cells.

 [145]
DSPE-PEG2000,
HSPC (hydrogenated soy phosphatidylcholine), DMPC, DOTAP		 Thin-film hydration

  • Ranibizumab-labeled AlexaFluor555-conjugated liposomes was synthesized to pass through the vitreous humor and adhere to the retina.

  • The lipophilic payload-loaded liposomes had particle sizes of approximately 110–135 nm.

  • The liposomal formulation was administered intravitreally to mice.

  • The findings revealed that the liposomes spread well without premature clearance in the vitreous humor and interacted effectively with the inner retinal layers.

 [146]