Title:Preparation of Ketoconazole-loaded Nanoemulsions for Ophthalmic
Delivery: Characterization and In-vitro Antifungal Activity Evaluation
Volume: 19
Issue: 3
Author(s): Mohammad Mehdi Mahboobian*, Negin Azadi and Shabnam Pourmoslemi
Affiliation:
- Department of Pharmaceutics, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran
Keywords:
Nanoemulsion, ketoconazole, ocular drug delivery, physicochemical characterization, release test, antifungal activity evaluation.
Abstract:
Background: Nanoemulsions (N.E.s) capable of ocular bioavailability elevation can be
used for poor water-soluble drugs such as ketoconazole (K.Z.). The current investigation was designed
for the purpose of overcoming this issue by developing K.Z. containing N.E.s for ophthalmic drug
delivery with appropriate therapeutic efficiency.
Methods: The preparation of ketoconazole N.E.s was performed by the low-energy technique.
According to the phase diagram, three stable formulations were selected for more physicochemical
analyses, including particle size, polydispersity index, pH, refractive index and viscosity. Finally, drug
release patterns and in-vitro antifungal activity were assessed for the final selected formulation.
Results: The developed N.E. formulations with droplet sizes less than 20 nm showed appropriate
physicochemical characteristics for ocular delivery. The selected formulation released 100% of the
encapsulated drug during 24 h. Moreover, antifungal assessments showed that prepared N.E. had
acceptable in-vitro antifungal activity.
Conclusions: Based on our findings, it can be concluded that N.E.s could be applied as effective
carriers for the ophthalmic delivery of ketoconazole.
