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Design and Development of Dasatinib Nanoemulsions for Ocular Delivery: In vitro Characterization, Biocompatibility,
Richa Khadke1, Amol Shete1, Akanksha Dashawant1
1Department of Pharmaceutics, Krishna Vishwa Vidyapeeth (Deemed to Be University), Krishna Institute of Pharmacy, Karad, MS 415539, India.
Abstract:
Dasatinib, a potent tyrosine kinase inhibitor with dual anti-inflammatory and anti-angiogenic properties, holds significant potential for treating ocular diseases such as Corneal Neovascularization (CNV), uveitis, and diabetic retinopathy. However, its low aqueous solubility and limited ocular retention present major formulation challenges. This study concentrated on the design and evaluation of Dasatinib nanoemulsions (Dasa NEs) for ocular delivery, utilizing nanotechnology to enhance solubility, stability, and therapeutic efficacy. The Dasa NEs were prepared using Oleic acid (lipid phase), Tween 80, Propylene Glycol (PG) (Smix), with component ratios optimized through pseudo-ternary phase diagrams. The resulting formulations exhibited nanoscale droplet sizes (<100 nm), low polydispersity indices, and stable zeta potential, ensuring colloidal stability and efficient delivery. Comprehensive physicochemical evaluations confirmed that the NEs possessed ideal pH, refractive index, surface tension, and viscosity for ophthalmic applications. Biocompatibility assessments using the MTT assay on SIRC cells demonstrated high cell viability, while HET-CAM tests confirmed the absence of significant ocular irritation. In vitro diffusion studies indicated improved drug permeation, highlighting the potential for prolonged therapeutic effects. Stability studies further validated the robustness of the formulations under various conditions. The developed nanoemulsions offer a promising, non-invasive platform for ocular drug delivery, improving patient compliance and therapeutic outcomes. Future studies should focus on in vivo evaluations and long-term safety to advance the clinical translation of this novel formulation.
Insights
New Dasatinib nanoemulsions improve ocular drug delivery. These formulations enhance solubility and retention for treating eye conditions like corneal neovascularization, offering a promising non-invasive treatment option.
Area of Science:
- Ophthalmic Drug Delivery
- Nanotechnology in Pharmaceuticals
- Formulation Science
Background:
- Dasatinib, a tyrosine kinase inhibitor, has anti-inflammatory and anti-angiogenic potential for ocular diseases.
- Challenges in ocular delivery include low solubility and poor retention of Dasatinib.
- Novel formulations are needed to overcome these limitations for effective treatment.
Purpose of the Study:
- To design and evaluate Dasatinib nanoemulsions (Dasa NEs) for enhanced ocular delivery.
- To improve Dasatinib's solubility, stability, and therapeutic efficacy using nanotechnology.
- To assess the physicochemical properties, biocompatibility, and in vitro performance of the developed nanoemulsions.
Main Methods:
- Nanoemulsions (NEs) prepared using Oleic acid, Tween 80, and Propylene Glycol (PG).
- Component ratios optimized via pseudo-ternary phase diagrams.
- Characterization included droplet size, zeta potential, pH, viscosity, and in vitro diffusion studies. Biocompatibility assessed using MTT assay and HET-CAM tests.
Main Results:
- Optimized Dasa NEs exhibited nanoscale droplet sizes (<100 nm) and excellent colloidal stability.
- Formulations showed ideal physicochemical properties for ophthalmic applications.
- High cell viability and no significant ocular irritation observed; enhanced in vitro drug permeation demonstrated.
Conclusions:
- Developed Dasatinib nanoemulsions provide a stable, effective, and non-invasive platform for ocular drug delivery.
- This formulation approach significantly improves drug solubility and retention, enhancing therapeutic potential.
- Further in vivo studies are warranted to support clinical translation for ocular diseases.

