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

Abstract

Objective: 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 267.67 % and 166.29 % respectively. Conclusion: The prepared cubosomes significantly improved the In-vivo absorption of REB in comparison with drug powder and commercially available tablets (Mucosta ® ).

Formation of Self-Assembled Liquid Crystalline Nanoparticles and Absorption Enhancement of Ω-3s by Phospholipids and Oleic Acids

“…The hexagonal phase exhibited a fan-like or angular texture, while the lamellar phase showed an oily streak or Maltese cross texture [75]. Additionally, the FE-TEM images revealed cubosomes that were nearly spherical with rectangular shapes, consistent with the literature [76,77]. To analyze the internal structure of the cubosome more accurately, an evaluation using cryo-TEM that does not affect the internal structure is required.…”

Hispolon-Loaded Liquid Crystalline Nanoparticles: Development, Stability, In Vitro Delivery Profile, and Assessment of Hepatoprotective Activity in Hepatocellular Carcinoma

“…The size (hydrodynamic radius Rh, nm) and size distribution (PDI) of the developed HP-LCNPs were measured by dynamic light scattering (DLS) using a Zetasizer instrument (Malvern, Worcestershire, UK). 18 Before measurement, the aforementioned formulation was diluted 1:9 (v/v) in water and filtered through a membrane filter (0.45 μm). The measurements were taken in triplicate for each sample, and the results were reported as mean ± standard deviation.…”

Cubogel as potential platform for glaucoma management

“…Morphological investigation of the optimized DZ-loaded cubosomal dispersion was further confirmed using Transmission electron microscopy (TEM) (Joel, Jem-2100, Tokyo, Japan) run at 100 kV. A droplet of the optimized cubosomal dispersion was located on a 200 mesh carboncoated copper grid, and was stained with 1% sodium phosphotungstate solution before TEM investigation (Hashem et al, 2018).…”

“…DSC (DSC-60, Schimadzu, Kyoto, Japan) was carried out for pure DZ, F127, Carbopol 934 and the optimized DZ-loaded cubogel. Samples (5 mg) were sealed into aluminum pans under a nitrogen atmosphere flow (50 ml/min) and heated over a temperature range 30-450 C at a constant rate of 10 C/min (Hashem et al, 2018).…”