In Vitro Small Intestinal Absorption Enhancement of S-164 by Monoolein Cubic Phase Nanoparticles

Abstract

In order to promote the gastrointestinal (GI) track absorption of S-164, which is known to be efficacious in the treatment of thrombotic and liver protection. S-164 suspension, liposomal suspensions containing S-164, and cubosomal suspensions containing the same were prepared by a sonication method. The particles in the suspensions exhibited multi-modal distribution and the mean diameters were hundreds of nanometer. The zeta potentials of particles contained in the S-164 suspension, the liposomal suspension and the cubosomal suspension were all negative, ranging from −10 mV to −22 mV, and no significant agglomeration and sedimentation were observed for couples of weeks. The fluctuation in particle size with the pH change of medium and the time lapse was significantly damped by the liposome and the cubosome. On TEM photos, S-164 exhibited no structural feature, liposomal S-164 was spherical lamellar particles, and cubosomal S-164 exhibited stripes on their particles. Liposomes had little effect on the in vitro small intestinal absorption of S-164, but cubosomes enhanced the intestinal absorption significantly. It is believed that the cubosomes interact with the GI tract epithelial cell lipids and it can enhance of S-164 through the transcellular route.