title: Bioavailability and foam cells permeability enhancement of Salvianolic acid B pellets based on drug-phospholipids complex technique.
abstract: 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±12nm). In vivo performance showed SalB-PC pellets presented significantly larger AUC(0-)(t), which was 0.58 times more than that of physical mixtures (PMs) and 1.57 times more than that of SalB pellets. C(max) 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.
authors.affiliation: Department of Pharmacy, Xuzhou Medical College, Xuzhou, PR China.
authors.forename: Jin
authors.initials: J
authors.lastname: Li
authors.forename: Pan
authors.initials: P
authors.lastname: Liu
authors.forename: Jian-Ping
authors.initials: JP
authors.lastname: Liu
authors.forename: Ji-Kun
authors.initials: JK
authors.lastname: Yang
authors.forename: Wen-Li
authors.initials: WL
authors.lastname: Zhang
authors.forename: Yong-Qing
authors.initials: YQ
authors.lastname: Fan
authors.forename: Shu-Ling
authors.initials: SL
authors.lastname: Kan
authors.forename: Yan
authors.initials: Y
authors.lastname: Cui
authors.forename: Wen-Jing
authors.initials: WJ
authors.lastname: Zhang
mesh_terms: D000818:Animals; D019540:Area Under Curve; D001572:Benzofurans / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002482:Cellulose / Q000737:chemistry; D005079:Excipients / Q000737:chemistry*; D005487:Foam Cells / Q000378:metabolism*; D007785:Lactose / Q000737:chemistry; D008297:Male; D046529:Microscopy, Electron, Transmission; D010316:Particle Size; D010539:Permeability; D010743:Phospholipids / Q000737:chemistry*; D011205:Povidone / Q000737:chemistry; D011817:Rabbits; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013997:Time Factors; D053630:Depsides
chemical_list: D001572:Benzofurans; D002482:Cellulose; D005079:Excipients; D007785:Lactose; D010743:Phospholipids; D011205:Povidone; C076944:salvianolic acid B; D053630:Depsides; C109691:microcrystalline cellulose