Bioavailability and foam cells permeability enhancement of Salvianolic acid B pellets based on drug–phospholipids complex technique

This study investigated phospholipids complex (PC) loaded pellets of poorly permeable Salvianolic acid B (SalB), in which PC was to improve the liposolubility and permeability of SalB. Transmission electron microscopy observation, differential scanning calorimetry measurement, infrared spectroscopy analysis, n-octanol/water partition coefficient study, and foam cell permeability research were employed to prove the complex formation. Pellets containing SalB phospholipids complex (SalB-PC) were prepared via extrusion/spheronization technique. The optimal pellets obtained with 30% SalB-PC, 15% Kollidon®CL-SF, 15% Flowlac®100, and 40% MCC exhibited a very homogeneous size distribution, the shortest disintegration time, highest crushing force, appreciable spherical shape, and a fast drug release behavior. Following hydration, the droplet size distribution of SalB-PC pellets was nearly same to its PC (85.4 ± 16 and 73.5 ± 12 nm). In vivo performance showed SalB-PC pellets presented significantly larger AUC0–t, which was 0.58 times more than that of physical mixtures (PMs) and 1.57 times more than that of SalB pellets. Cmax of SalB-PC pellets were also increased by 0.26-fold and 0.80-fold as that of PMs and SalB pellets, respectively. In conclusion, extrusion/spheronization could be a suitable technique to prepare PC loaded pellets, which could effectively preserve the properties of PC to improve the permeability and bioavailability of highly water-soluble drug.

Graphical abstractPhospholipids complex loaded pellets of poorly permeable Salvianolic acid B (SalB) were successfully prepared via extrusion/spheronization technique, in which the liposolubility, foam cell permeability, and oral bioavailability of SalB were all significantly improved. Moreover, the resulting pellets had a uniform size, a spherical shape and suitable hardness and well preserve the properties of phospholipids complex.Figure optionsDownload full-size imageDownload high-quality image (187 K)Download as PowerPoint slide