title: Optimization and evaluation of thermoresponsive diclofenac sodium ophthalmic in situ gels.
abstract: This work was conducted to optimize and evaluate Pluronic F127-based thermoresponsive diclofenac sodium ophthalmic in situ gels (DS in situ gel). They were prepared by cold method and investigated their physicochemical properties i.e., pH, flow ability, sol-gel transition temperature, gelling capacity and rheological properties. An optimized formulation was selected and investigated its physicochemical properties before and after autoclaving, eye irritation potency in SIRC cells and rabbits. In vivo ophthalmic absorption was performed in rabbits. It was found that physicochemical properties of DS in situ gels were affected by formulation compositions. Increment of Pluronic F127 content decreased sol-gel transition temperature of the products while increase in Pluronic F68 concentration tended to increase sol-gel transition temperature. In this study, Carbopol 940 did not affect sol-gel transition temperature but it affected transparency, pH, and gelling capacity of the products. The optimized formulation exhibited sol-gel transition at 32.6 ± 1.1 °C with pseudoplastic flow behavior. It was lost diclofenac sodium content during autoclaving. However, it was accepted as safe for ophthalmic use and could increase diclofenac sodium bioavailability in aqueous humor significantly. In conclusion, the optimized DS in situ gel had potential for using as an alternative to the conventional diclofenac sodium eye drop. However, autoclaving was not a suitable sterilization method for this product.
authors: Department of Pharmaceutical Technology, Faculty of Pharmacy, Srinakharinwirot University, 63 Rangsit-Nakhonnayok Road, Nakhonnayok 26120, Thailand. rathapona@hotmail.com
authors: Rathapon
authors: R
authors: Asasutjarit
authors: Suthira
authors: S
authors: Thanasanchokpibull
authors: Asira
authors: A
authors: Fuongfuchat
authors: Sukitaya
authors: S
authors: Veeranondha
mesh_terms: D000180:Acrylic Resins / Q000737:chemistry; D060433:Administration, Ophthalmic; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000737:chemistry* / Q000494:pharmacology; D001082:Aqueous Humor / Q000187:drug effects; D055598:Chemical Phenomena; D004008:Diclofenac / Q000737:chemistry* / Q000494:pharmacology; D004333:Drug Administration Routes; D004339:Drug Compounding; D016503:Drug Delivery Systems / Q000379:methods*; D005079:Excipients / Q000737:chemistry*; D005123:Eye / Q000187:drug effects; D005782:Gels / Q000737:chemistry; D006358:Hot Temperature; D008297:Male; D009883:Ophthalmic Solutions / Q000737:chemistry; D044367:Phase Transition; D020442:Poloxamer / Q000737:chemistry*; D011817:Rabbits; D013242:Sterilization; D044366:Transition Temperature
chemical_list: D000180:Acrylic Resins; D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D005782:Gels; D009883:Ophthalmic Solutions; D020442:Poloxamer; D004008:Diclofenac; C006903:carbopol 940