Optimization of the interaction between Diclofenac and Ibuprofen with Benzalkonium chloride to prepare ocular nanosuspension.

The objective of the present study was to formulate non-irritating, compatible, microbiologically stable ophthalmic formulation with good corneal permeation characteristics. The interaction between diclofenac sodium or ibuprofen with benzalkonium chloride was optimized using central composite experimental design to prepare nanosuspensions by nanoprecipitation. The optimized batches of nanosuspensions were evaluated for ex vivo corneal permeation study, preservative challenge test and physical stability. The optimal concentrations of benzalkonium chloride for diclofenac sodium (0.1%, w/v) and ibuprofen (0.1% w/v) nanosuspensions were determined to be 0.002%(w/v), which had respective average particle size of 440 nm and 331 nm respectively. The nanosuspensions of diclofenac sodium and ibuprofen provided 1.6 and 2.1- fold higher ex vivo corneal permeation than their respective conventional aqueous solution dosage forms. Further, the concentration of benzalkonium chloride used in the formulations showed adequate preservative efficacy. The optimized nanosuspension formulations of diclofenac and ibuprofen were found to be physically stable and microbiologically safe with greater corneal penetration than the conventional solution dosage forms. PMID: 31849291 [PubMed - as supplied by publisher]
Source: Recent Patents on Drug Delivery and Formulation - Category: Drugs & Pharmacology Tags: Recent Pat Drug Deliv Formul Source Type: research