Cationic microemulsion of voriconazole for the treatment of fungal keratitis: in vitro and in vivo evaluation.

Aim: This investigation aimed to develop a voriconazole-loaded chitosan-coated cationic microemulsion (CVME) to treat fungal keratitis. Methods: Microemulsions were prepared using water titration, and the optimized microemulsion was coated with chitosan to prepare CVME. The physicochemical parameters, ocular irritation potential, in vitro antifungal efficacy and in vitro release studies were performed. The in vivo antifungal efficacy study was conducted in a fungal infection-induced rabbit eye model. Results: The developed CVME displayed acceptable physicochemical properties and excellent mucoadhesive behavior and showed a sustained release profile. Ex vivo and in vivo studies concluded that higher permeability and improved antifungal efficacy were observed for CVME than drug suspension (DS). Conclusion: The prepared CVME7 is a viable alternative to treating fungal keratitis with existing approaches.

Nanotechnology can help resolve problems that are currently associated with eye medications. Microemulsions (MEs) are mixtures containing tiny droplets of oil and water, which are made stable by ingredients called surfactants (meaning a type of soap) and co-surfactants. The ability for medications to be released slowly in MEs makes them suitable for eye medications because they reduce the number of times eye drops need to be used each day. This study wanted to create a medicine called voriconazole-loaded chitosan-coated cationic microemulsion (CVME) to treat a fungal infection in the eye called keratitis. We made MEs by gradually adding a combination of oil, surfactant, and water together. Then, we coated the best MEs with a substance called chitosan to make CVME. We tested its physical and chemical properties, whether it irritated the eyes, how well it could fight fungus, and how it released medicine. We tested CVME on rabbits with a fungal eye infection. CVME had good physical and chemical properties and stuck well to the mucus on the surface of the eyes. It released the medicine slowly. The system created in this study is very important for treating fungal infections because it helps the medicine stay on the eye surface longer and allows it to better reach the infected areas of the eye. CVME7 might be a better option for treating fungal keratitis instead of other methods that are currently used.

Cationic Chitosan/Pectin Polyelectrolyte Nanocapsules of Moxifloxacin as Novel Topical Management System for Bacterial Keratitis.

PURPOSE: Moxifloxacin (MOX) is a fourth-generation fluoroquinolone and a broad spectrum antibiotic used in the management of bacterial keratitis (BK). This investigation aimed to formulate MOX-loaded chitosan/pectin cationic polyelectrolyte nanocapsules (CPNCs) for the effective topical treatment of BK. METHODS: Physicochemical properties like nanocapsule size, charge, drug entrapment efficiency (EE), viscosity, pH, and in-vitro release profile of CPNCs were evaluated. The in-vitro antibacterial activity of CPNCs and marketed formulations (MFs) was studied against Staphylococcus aureus. Ex-vivo corneal permeation studies of CPNCs were evaluated with the help of a modified diffusion apparatus, which was used with goat cornea. The pharmacodynamic study was performed with optimized CPNCs on a BK-induced rabbit eye model and compared with MF. RESULTS: The optimized nanocapsules appeared as positive charge (+19.91 ± 0.66) with a nano size (242.0 ± 0.30 nm) as calculated by the dynamic light scattering method. The in-vitro release profile of CPNCs exhibited sustained release properties. The ex-vivo permeation pattern also supported the improved drug permeation through the cornea from CPNCs as compared with MF. Draize irritation studies confirmed that the prepared formulation is compatible with the corneal tissue. The in-vivo study concluded that the antibacterial activity of CPNCs was improved when evaluated with MF. CONCLUSION: The obtained results showed that CPNCs were the better choice for the management of BK therapy due to its capability to improve the corneal adhesion of CPNCs through direct interaction with the mucous membrane of the corneal tissue.

Cationic Polyelectrolyte Nanocapsules of Moxifloxacin for Microbial Keratitis Therapy: Development, Characterization, and Pharmacodynamic Study.

Microbial keratitis (MK) is a vision-threatening disease and the fourth leading cause of blindness worldwide. In this work, we aim to develop moxifloxacin (MXN)-loaded chitosan-based cationic mucoadhesive polyelectrolyte nanocapsules (PENs) for the effective treatment of MK. PENs were formulated by polyelectrolyte complex coacervation method and characterized for their particle size, surface charge, morphology, mucoadhesive property, in-vitro and ex-vivo release, ocular tolerance, and antimicrobial efficacy studies. The pharmacodynamic study was conducted on rabbit eye model of induced keratitis and it is compared with marketed formulation (MF). Developed PENs showed the size range from 230.7 ± 0.64 to 249.0 ± 0.49 nm and positive surface charge, spherical shape along with appropriate physico-chemical parameters. Both in-vitro and ex-vivo examination concludes that PENs having more efficiency in sustained release of MXN compared to MF. Ocular irritation studies demonstrated that no corneal damage or ocular irritation. The in-vivo study proved that the anti-bacterial efficacy of PENs was improved when compared with MF. These results suggested that PENs are a feasible choice for MK therapy because of their ability to enhance ocular retention of loaded MXN through interaction with the corneal surface of the mucous membrane.

Topical Ocular Delivery of Nanocarriers: A Feasible Choice for Glaucoma Management.

Topical ocular delivery is an acceptable and familiar approach for the treatment of common ocular diseases. Novel strategies for the treatment of inherited eye diseases include new pharmacologic agents, gene therapy and genome editing, which lead to the expansion of new management options for eye disorders. The topical ocular delivery of nanocarriers is a technique, which has the potential to facilitate novel treatments. Nanocarrier- based strategies have proven effective for site-targeted delivery. This review summarizes recent development in the area of topical delivery of different nanocarriers (Polymer, Vesicular and dispersed systems) for the management of glaucoma, a group of ocular disorders characterized by progressive and accelerated degeneration of the axons of retinal ganglion cells, which make up the optic nerve. Unique cellular targets for glaucoma treatment, primarily the trabecular meshwork of the anterior segment of the eye, make glaucoma facilitated by the use of nanocarriers an ideal disorder for novel molecular therapies.

Brinzolamide loaded chitosan-pectin mucoadhesive nanocapsules for management of glaucoma: Formulation, characterization and pharmacodynamic study.

AIM: Brinzolamide (BNZ) is a carbonic anhydrase inhibitor commonly used for the treatment of glaucoma. The aim of this study was to prepare BNZ loaded chitosan-pectin mucoadhesive nanocapsules (CPNCs) by polyelectrolyte complex coacervation method for ocular delivery and evaluated for its anti glaucoma efficacy. METHODS: The prepared CPNCs were characterized for their particle size, polydispersity index, zeta-potential, surface morphology, entrapment efficiency, drug loading efficiency, mucoadhesive strength in-vitro and ex-vivo release. The pharmacodynamic studies were conducted for CPNCs on glaucoma induced rabbit eye model and compared with marketed product. RESULT AND DISCUSSION: All the formulated CPNCs exhibited the size range from 217.01 ± 0.21 to 240.05 ± 0.08 nm and appropriate physico-chemical parameters, and depicted a couple of erosion- diffusion release of BNZ over a time of 8 h. Ex-vivo corneal permeation study concluded that BNZ loaded CPNCs crosses the cornea potentially higher rate as compared to the marketed product. In pharmacodynamic study, greater intraocular pressure lowering effect was achieved by CPNCs as compared to marketed drug product. CONCLUSION: The result concluded that CPNCs are a feasible choice to conventional eye drops because of its ability to improve the bioavailability via its longer precorneal retention time and its ability to sustained release of the drug.