Formulation development, optimization and characterization of mucoadhesive minitablets of cefuroxime axetil: in vitro, ex vivo and in vivo pharmacokinetic evaluation

Abstract

Abstract Background The current study expands on the use of design of experiment in developing cefuroxime axetil mucoadhesive minitablets for treating antibiotic-associated colitis. A comprehensive QbD-based product development strategy was implemented, with the target product profile defined based on the desired product quality of mucoadhesive minitablets. The identified critical quality attributes are based on the target product profile. The goal was to find the optimum levels by using the concentrations of chitosan (mg) (X1), HPMC K100M (X2) and sodium carboxymethyl cellulose (X3) as the influential variables. The response surface methodology determines the dependent variables using 33 Box–Behnken design to optimize the selected critical factors. The friability (%), drug content (%) and mucoadhesive strength (%) characteristics of cefuroxime axetil mucoadhesive minitablets were evaluated using ANOVA for the observed responses or dependent variables. Results The study demonstrated that run 8 with optimum composition chitosan, HPMC K100M and sodium carboxy methyl cellulose, which are the mucoadhesive polymers, showed a desirable and promising drug release profile up to 24 h, higher percentage of drug content, mucoadhesion and swelling index. Conclusions The optimized mucoadhesive minitablets of cefuroxime axetil demonstrated desired formulation characteristics, including improved bioavailability and high control over the drug’s release rate and increased flexibility in adjusting both the dose and the drug’s release rate. In a nutshell, the studies support the successful development of mucoadhesive minitablets of cefuroxime axetil, which could be used to treat antibiotic-associated colitis.