Pre-clinical safety of topically administered sunitinib-loaded lipid and polymeric nanocarriers targeting corneal...

Area of Science:

• Ophthalmology
• Nanotechnology
• Pharmacology

Background:

• Corneal neovascularization (CNV) poses a significant challenge in ophthalmic treatment.
• Sunitinib (SUN) is a potential therapeutic agent for CNV, requiring effective delivery systems.
• Nanocarrier systems offer promise for targeted topical ocular drug delivery.

Purpose of the Study:

• To compare three types of sunitinib-loaded nanocarriers for topical CNV treatment: polymeric nanospheres (NS), liposomes (LIP), and solid lipid nanoparticles (SLN).
• To identify the optimal nanocarrier formulation for enhanced corneal retention and therapeutic efficacy.

Main Methods:

• Formulation and optimization of SUN-loaded NS, LIP, and SLN.
• Characterization using nanoparticle tracking analysis (NTA), EPR spectroscopy, and zeta potential.
• In vitro drug release, ex vivo corneal permeability, and ocular tolerance assays (BCOP, HET-CAM, HP).

Main Results:

• Optimal NS, LIP, and SLN formulations were selected based on size, PdI, DL, and EE.
• All formulations exhibited no ocular toxicity or irritation.
• SLN demonstrated superior surface fluidity, suitable drug release kinetics, and enhanced SUN corneal retention compared to NS and LIP.

Conclusions:

• Solid lipid nanoparticles (SLN) represent the most promising nanocarrier for sunitinib delivery in topical CNV treatment.
• SLN show significant potential for clinical translation due to their favorable characteristics and efficacy.
• This study highlights the advantage of SLN over NS and LIP for ocular drug delivery applications.