Multiparticulate drug delivery system based on carbomer-ciprofloxacin Complex

PALENA, MC.; BERMUDEZ, JM.; MANZO, RH.; JIMENEZ KAIRUZ, AF.

Rosario

Congreso; 4ta. Reunión Internacional de Ciencias Farmacéuticoas RICiFa 2016; 2016

Fac. de Farmacia y Bioquímica de la UNRos y FCQ-UNC.

Complexes of a polyelectrolyte (PE) fully or partially neutralized with an ionizable drug (D) have several unique and favorable properties as drug carrier systems such as drug delivery modulation, drug compatibility and stability improvement, among others. Besides multiparticulate drug delivery systems may improve oral pharmacotherapy due to their more regular and predictable gastrointestinal transit.Therefore, the aim of this study is the preparation of PE-D multiparticles by extrusion-spheronization, loaded with ciprofloxacin (Cip), to assess the potential utility of these systems in drug delivery design for oral route.PE-D complex was prepared by mixing appropriate amounts of Carbomer-974P (Cb), Cip, NaOH and ethanol to get a semisolid paste of Cb?Cip.A 23 factorial design was employed to estimate the effects of simultaneously modifying multiple formulation variables. Formulation and process variables, and the ranges for each, were based on information obtained in preliminary experiments. The independent variables investigated were the microcrystalline cellulose (MC) and polyvinylpyrrolidone-K30 (PVP) concentration and moisture content. Screw speed, temperature, spheronization load, speed and time remained constant. For the evaluation of the quality of the pellets size distribution, shape and granule strength were studied. Release profiles of Cip from the pellets were performed in a USP-dissolution apparatus1 using simulated gastric fluid without pepsine as dissolution medium (pH=1.20±0.05).Eight batches of Cb-Cip pellets were obtain with different excipients proportions. Size range between 1 and 1.5 mm was observed. Results suggest that combining the conditions of high CM (20%) and water (50%) and low PVP (2%) levels with 10 min of spheronization time conduce to highest quality bead. Beads delivered 90% of Cip dose in simulated gastric fluid in about 120 min and the profile is similar than the comercially controlled release tablets. Such behavior would allow the intragastric release of Cip, which can reach the first portion of the intestine as a solution and might contribute to improve its bioavailability.