Background & Objectives Low penetration efficiency and retention time are the main therapeutic concerns that make it difficult for most of the drugs to be delivered to the intraocular tissues. These challenging issues are often related to those drugs, which have low or poor solubility and low permeability. The goal of this study was designed to develop nanostructured lipid carriers (NLCs) loaded with itraconazole (ITZ) with the objective of enhancing topical ocular permeation and thereby improving clinical efficacy. Materials and Methods ITZ-loaded NLCs were fabricated by a high-speed homogenization technique using surfactant (Poloxamer 407), and lipids (stearic acid and oleic acid). Optimization of formulations was performed by 3 level factorial design and the selected formulation (F6) was evaluated by differential scanning calorimetry and transmission electron microscopy. Antifungal activity was assessed by measuring the zone of inhibition and irritation potential using the HET-CAM test. Results The independent variables (lipid ratio-X 1 and percentage of emulsifier-X 2 ) have a positive impact on percentage entrapment efficiency (Y 2 ) and percentage release (Y 3 ) but have a negative impact on particle size (Y 1 ). Based on the better entrapment efficiency (94.65%), optimum particle size (150.67 nm), and percentage cumulative drug release (68.67%), batch F6 was selected for further evaluation. Electron microscopic images revealed that the prepared particles are spherical and have nano size. Antifungal studies demonstrated enhancement in the zone of inhibition by formulation F6 as compared to a commercial eye drop. The non-irritancy of optimized formulation (F6) was confirmed with a zero score. Interpretation & Conclusion In summary, the optimized NLCs seem to be a potent carrier for the effective delivery of itraconazole in ocular therapy.

Background: The low penetration power and the retention time into the intraocular tissue are the main problems that make difficult for most of the drugs for the ocular drug delivery system. This is for those drugs that are having the low or poor solubility and the low permeability. Objective: Nanostructured Lipid Carriers (NLCs) loaded with Itraconazole (ITZ) were formulated with the aim to increase the solubility and enhance the retention time in the intraocular tissue. Methods: The NLCs were prepared by using Pluronic (PF127), stearic acid and oleic acid. Itraconazole loaded Nanostructured lipid carrier were prepared by high-pressure homogenization method and the formulations were prepared and optimized by 3 Level Factorial Design. Results: F6 was selected on the basis of better entrapment efficiency (94.65), optimum particle size (310nm), and percentage cumulative release (68.67%). Scanning electron microscopy revealed spherical Nanostructured lipid carrier in the microemulsion. Nanostructured lipid carrier Irritation test showed the non-irritancy and antifungal activity showed a more inhibition zone as compared to the marketed formulation. Conclusion: Conclusively the optimized Formulation (F6) shows better results for the ocular drug delivery as compared to the marked formulation.