title: Hp-β-CD-voriconazole in situ gelling system for ocular drug delivery: in vitro, stability, and antifungal activities assessment.
abstract: The objective of the present study was to design ophthalmic delivery systems based on polymeric carriers that undergo sol-to-gel transition upon change in temperature or in the presence of cations so as to prolong the effect of HP- β -CD Voriconazole (VCZ) in situ gelling formulations. The in situ gelling formulations of Voriconazole were prepared by using pluronic F-127 (PF-127) or with combination of pluronic F-68 (PF-68) and sodium alginate by cold method technique. The prepared formulations were evaluated for their physical appearance, drug content, gelation temperature (T gel), in vitro permeation studies, rheological properties, mucoadhesion studies, antifungal studies, and stability studies. All batches of in situ formulations had satisfactory pH ranging from 6.8 to 7.4, drug content between 95% and 100%, showing uniform distribution of drug. As the concentration of each polymeric component was increased, that is, PF-68 and sodium alginate, there was a decrease in T gel with increase in viscosity and mucoadhesive strength. The in vitro drug release decreased with increase in polymeric concentrations. The stability data concluded that all formulations showed the low degradation and maximum shelf life of 2 years. The antifungal efficiency of the selected formulation against Candida albicans and Asperigillus fumigatus confirmed that designed formulation has prolonged effect and retained its properties against fungal infection.
authors.affiliation: Chitkara College of Pharmacy, Chitkara University, Chandigarh-Patiala National Highway, Rajpura, Patiala, Punjab 140401, India.
authors.forename: Pravin
authors.initials: P
authors.lastname: Pawar
authors.forename: Heena
authors.initials: H
authors.lastname: Kashyap
authors.forename: Sakshi
authors.initials: S
authors.lastname: Malhotra
authors.forename: Rakesh
authors.initials: R
authors.lastname: Sindhu
mesh_terms: D000073738:2-Hydroxypropyl-beta-cyclodextrin; D000268:Adhesiveness / Q000187:drug effects; D000818:Animals; D000935:Antifungal Agents / Q000008:administration & dosage* / Q000494:pharmacology*; D001232:Aspergillus fumigatus / Q000187:drug effects; D002176:Candida albicans / Q000187:drug effects; D003315:Cornea / Q000187:drug effects; D016503:Drug Delivery Systems; D004355:Drug Stability; D005123:Eye / Q000187:drug effects*; D005782:Gels / Q000737:chemistry*; D006041:Goats; D006863:Hydrogen-Ion Concentration; D066298:In Vitro Techniques; D007700:Kinetics; D008826:Microbial Sensitivity Tests; D010539:Permeability / Q000187:drug effects; D011743:Pyrimidines / Q000008:administration & dosage* / Q000494:pharmacology*; D012212:Rheology / Q000187:drug effects; D013696:Temperature; D014230:Triazoles / Q000008:administration & dosage* / Q000494:pharmacology*; D014783:Viscosity / Q000187:drug effects; D065819:Voriconazole; D047392:beta-Cyclodextrins / Q000737:chemistry*
chemical_list: D000935:Antifungal Agents; D005782:Gels; D011743:Pyrimidines; D014230:Triazoles; D047392:beta-Cyclodextrins; D000073738:2-Hydroxypropyl-beta-cyclodextrin; D065819:Voriconazole