Abstract
Purpose :
The solubility and permeability of ocular therapeutics are the main challenges for topical ocular drug delivery. The poor water solubility of drugs limits their topical ocular delivery. Most of these drugs are formulated as suspensions and emulsions. However, they have drawbacks like high dosing frequency, minor discomfort upon administration, and poor corneal permeation. Nanomicelles are self-assembling vesicular delivery systems that can encapsulate poorly soluble drugs within their core. We aim to improve the solubility and permeability of water-insoluble drugs across the cornea using nanomicelles.
Methods :
Nanomicelles loaded with various water-insoluble ophthalmic drugs (Difluprednate loaded nanomicelles, Dicel; Latanoprost loaded nanomicelles, Latcel; and Resveratrol loaded nanomicelles, Recel) were prepared using the thin film hydration method. Biocompatible polymers were used for the preparation of nanomicelles. The prepared nanomicelles were characterized for particle size, zeta potential and polydispersity index using dynamic light scattering method, morphology was visualized by scanning electron microscopy, and ex vivo transcorneal permeation was performed using goat cornea. Additionally, pre-clinical evaluation of the nanomicelles was performed to evaluate their therapeutic outcome.
Results :
The prepared nanomicelles were characterized as given in Table 1. We found that nanomicelles delivery system improved the solubility by 170 folds (Recel), transcorneal permeability by 6 folds (Dicel), and ocular residence time by 4 folds (Latcel) compared to the marketed formulation. All the nanomicelles formulations were found to be biocompatible and safe for ocular use.
Conclusions :
Nanomicelles were established as a platform delivery technology to improve the solubility and permeability of water-insoluble drugs for ocular application. Additionally, the developed nanomicelles have shown the potential to deliver water insoluble drugs to various therapeutic target site in the anterior segment of the eye. The pre-clinical studies proved that nanomicelles could improve the therapeutic outcome, making it a promising drug delivery platform.
This abstract was presented at the 2024 ARVO Annual Meeting, held in Seattle, WA, May 5-9, 2024.