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Updated: Sep 27, 2025
Spatio-Temporal In Vivo Imaging of Ocular Drug Delivery Systems using Fiberoptic Confocal Laser Microendoscopy
Published on: September 27, 2021
Liposomal sunitinib for ocular drug delivery: A potential treatment for choroidal neovascularization
Shirin Tavakoli1, Jooseppi Puranen2, Sina Bahrpeyma2
1Drug Research Program, Division of Pharmaceutical Biosciences, Faculty of Pharmacy, University of Helsinki, Viikinkaari 5 E, FI-00790 University of Helsinki, Finland.
Abstract:
Choroidal neovascularization (CNV) is a prevalent vision-threatening vascular disorder in aging population. CNV is associated with several diseases in the posterior segment of the eye such as age-related macular degeneration (AMD). In this study we developed sunitinib-loaded liposomes to block the neovascularization signalling pathway through inhibition of tyrosine kinase of vascular endothelial growth factor receptors (VEGFRs). Liposomal sunitinib formulations were prepared by thin film hydration method and studied for their encapsulation efficiency (EE), loading capacity (LC) and drug release profile in buffer andvitreous. Our finding showed that the liposomes (mean size 104 nm) could effectively entrap sunitinib (EE ≈ 95%) at relatively high loading capacity (LC ≈ 5%) and release sunitinib over at least 3 days. Intravitreal sunitinib-loaded liposomes revealed inhibitory effect on established neovascularization in laser-induced CNV mouse model while the intravitreal injection of sunitinib solubilized with cyclodextrin was inefficient in management of neovascularization. Accordingly, liposomal sunitinib is a promising drug delivery system that should be further studied to inhibit the CNV related to AMD.
Insights
Sunitinib-loaded liposomes effectively treat choroidal neovascularization (CNV), a major cause of vision loss in aging populations. This novel drug delivery system shows promise for age-related macular degeneration (AMD) treatment.
Area of Science:
- Ophthalmology
- Nanotechnology
- Pharmacology
Background:
- Choroidal neovascularization (CNV) is a leading cause of vision impairment, particularly in the aging population.
- CNV is a key factor in diseases like age-related macular degeneration (AMD).
- Current treatments face challenges in effectively managing neovascularization.
Purpose of the Study:
- To develop and evaluate sunitinib-loaded liposomes as a targeted drug delivery system.
- To inhibit the vascular endothelial growth factor receptor (VEGFR) signaling pathway.
- To assess the efficacy of liposomal sunitinib in an animal model of CNV.
Main Methods:
- Sunitinib-loaded liposomes were prepared using the thin film hydration method.
- Liposomal formulations were characterized for encapsulation efficiency (EE), loading capacity (LC), and drug release.
- The efficacy of intravitreal liposomal sunitinib was tested in a laser-induced CNV mouse model.
Main Results:
- Liposomes demonstrated high sunitinib entrapment (EE ≈ 95%) and loading capacity (LC ≈ 5%).
- Sunitinib release was sustained for at least 3 days.
- Intravitreal liposomal sunitinib significantly inhibited established neovascularization, outperforming solubilized sunitinib.
Conclusions:
- Liposomal sunitinib is a stable and effective drug delivery system for inhibiting CNV.
- This approach offers a promising therapeutic strategy for AMD and related neovascular disorders.
- Further research is warranted to explore the clinical potential of liposomal sunitinib for vision-threatening conditions.
