Formulation and Characterization of Cubosomes Containing REB for Improvement of Oral Absorption of the Drug in Human Volunteers

Objectives: To prepare rebamipide (REB) -loaded cubosomal nanoparticles to improve the oral bioavailability of the drug in human volunteers. Methodology: The poorly water soluble drug REB was incorporated into cubosomal nanoparticles by solvent dilution method. The prepared REB-loaded cubosomes were in vitro characterized for particle size, polydispersity index (PDI), zeta potential, drug crystallinity and in vitro drug release. In vivo absorption of REB-loaded cubosomes was compared with drug powder and commercially available tablets Mucosta® (Egypt Otsuka Pharmaceutical Company) in healthy human volunteers. Results: In vitro, REB-loaded cubosomes entrapped about 82.44 % drug and revealed nanometer-size ranged from 303.1 ± 4.9 to 444.9 ± 6 nm. In vitro REB release from cubosomes exhibited a phase of rapid and high release of the drug during the first hour followed by a slower and complete drug release over a period of 3 hrs. The results of bioavailability study in healthy human volunteers showed that cubosomes significantly improved the rate and extent of REB absorption. The mean relative bioavailability of the REB loaded cubosomes compared to the drug powder and commercially available tablets (Mucosta®) was 191.23 ± 1.24 % and 166.29 ± 1.14 % respectively. Conclusion: The prepared cubosomes significantly improved the In-vivo absorption of REB in comparison with drug powder and commercially available tablets (Mucosta®).