Exploring Penetration Ability of Carbonic Anhydrase Inhibitor-Loaded Ultradeformable Bilosome for Effective Ocular Application.

Brinzolamide is an effective carbonic anhydrase inhibitor widely used in glaucoma therapy but limits its application due to inadequate aqueous solubility and permeability. The aim of the present research work is the development and characterization of brinzolamide-loaded ultradeformable bilosomes to enhance the corneal permeation of the drug. These ultradeformable bilosomes were prepared by ethanol injection method and evaluated for physicochemical properties, particle size, morphology, drug release, ultra-deformability, corneal permeation, and irritation potential. The optimized formulation exhibited an average particle size of 205.4 ± 2.04 nm with mono-dispersity (0.109 ± 0.002) and showed entrapment efficiency of 75.02 ± 0.017%, deformability index of 3.91, and release the drug in a sustained manner. The brinzolamide-loaded ultradeformable bilosomes released 76.29 ± 3.77% of the drug in 10 h that is 2.25 times higher than the free drug solution. The bilosomes were found non-irritant to eyes with a potential irritancy score of 0 in Hen's egg-chorioallantoic membrane assay. Brinzolamide-loaded ultradeformable bilosomes showed 83.09 ± 5.1% of permeation in 6 h and trans-corneal permeability of 8.78 ± 0.14 cm/h during the ex vivo permeation study. The acquired findings clearly revealed that the brinzolamide-loaded ultradeformable bilosomes show promising output and are useful in glaucoma therapy.

Luliconazole-loaded nanostructured lipid carriers for topical treatment of superficial Tinea infections.

Tinea are superficial fungal infections caused by dermatophytes. Luliconazole exhibits highest antifungal activity against Trichophyton spp. which are major causative agents of dermatophytosis. However, luliconazole suffers from drawbacks such as less skin retention, low aqueous solubility and poor skin penetration. To overcome the limitations of luliconazole, nanostructured lipid carriers (NLCs) were formulated. NLCs are better permeation enhancers as they increase skin occlusion and hydration. The selection of various lipids and surfactants was based on the solubility of luliconazole in these components. Luliconazole NLC dispersion was prepared by hot melt emulsification technique followed by probe sonication. The dispersion was incorporated into a gel composed of Sepineo P 600 under magnetic stirring. in vitro antifungal studies were carried out with optimized luliconazole NLC gel, marketed luliconazole cream and control (luliconazole in gel base) against pathogenic Trichophyton rubrum. Ex-vivo diffusion study demonstrated that NLCs incorporated into gel exhibited greater retention on skin. In-vivo skin irritancy study showed no signs of erythema or edema post 24, 48, and 72 h at site of application. In comparison with marketed cream and based on the zone of inhibition diameters, NLC formulation was found to be very effective against Trichophyton rubrum.