title: Ophthalmic controlled release in situ gelling systems for ciprofloxacin based on polymeric carriers.
abstract: The objective of the present study was to design controlled release ophthalmic delivery systems for ciprofloxacin based on polymeric carriers that undergo sol-to-gel transition upon change in pH or in the presence of cations in an attempt to prolong the effect of ciprofloxacin and improve its ocular bioavailability. Carbopol and alginates polymers were used to confer gelation properties to the formulations. Hydroxypropyl methylcellulose and methylcellulose were combined with carbopol to increase the viscosity of the gels and to reduce the concentration of the incorporated carbopol. The release exponents (n) for the designed systems were close to 1, indicating that the drug release occurred by zero-order kinetics. Controlled release in situ gels consisting of carbopol and cellulose derivatives showed an increase in viscosity, gelling capacity, and adhesiveness as the concentration of each polymeric component was increased. On the other hand, these parameters possessed lowest values when alginate was used as an in situ gelling agent. The antimicrobial efficiency of the selected formulation against gram-positive and gram-negative organisms including Echerichia coli, staphylococcus strains and Pseudomonas aeruginosa confirmed that the designed formulation has prolonged the antimicrobial effect of ciprofloxacin and retained its properties against bacteria.
authors.affiliation: Department of Pharmaceutics, College of Pharmacy, King Saud University, PO Box 17221, Riyadh 11484, Saudi Arabia. kassas_r2@yahoo.com
authors.forename: Raida S
authors.initials: RS
authors.lastname: Al-Kassas
authors.forename: Mona M
authors.initials: MM
authors.lastname: El-Khatib
mesh_terms: D000464:Alginates / Q000737:chemistry; D000900:Anti-Bacterial Agents / Q000008:administration & dosage*; D000890:Anti-Infective Agents / Q000008:administration & dosage*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D002939:Ciprofloxacin / Q000008:administration & dosage* / Q000493:pharmacokinetics; D004333:Drug Administration Routes; D004337:Drug Carriers / Q000008:administration & dosage / Q000737:chemistry; D016503:Drug Delivery Systems; D004926:Escherichia coli / Q000187:drug effects; D005123:Eye / Q000187:drug effects* / Q000378:metabolism; D005782:Gels / Q000737:chemistry; D008747:Methylcellulose / Q000737:chemistry; D009883:Ophthalmic Solutions / Q000737:chemistry; D011108:Polymers / Q000737:chemistry
chemical_list: D000464:Alginates; D000900:Anti-Bacterial Agents; D000890:Anti-Infective Agents; D004337:Drug Carriers; D005782:Gels; D009883:Ophthalmic Solutions; D011108:Polymers; D002939:Ciprofloxacin; D008747:Methylcellulose