Homogeneous nanoparticles to enhance the efficiency of a hydrophobic drug, antihyperlipidemic probucol, characterized by solid-state NMR.
A low absorption in the gastrointestinal tract of hydrophobic pharmaceutical compounds in use today considerably limits their bioavailability, and therefore they are taken in large doses in order to reach the therapeutic plasma concentration, which inevitably results in undesired side effects. In this study, we demonstrate a new nanoparticle approach to overcome this problem, and our experimental results show that this approach has a high efficiency of drug loading and is easily adaptable to industrial scale. Characterization of nanoparticles containing a cholesterol-lowering hydrophobic drug, probucol, using a variety of biophysical techniques revealed higher homogeneity of these particles compared to those prepared using other approaches. Intermolecular interactions of these nanoparticles are probed at high resolution by magic angle spinning solid-state NMR experiments.
Io
Takeshi
T
College of Pharmacy, Nihon University, Chiba 274-8555, Japan.
Fukami
Toshiro
T
Yamamoto
Kazutoshi
K
Suzuki
Toyofumi
T
Xu
Jiadi
J
Tomono
Kazuo
K
Ramamoorthy
Ayyalusamy
A
D018938:Caco-2 Cells; D002463:Cell Membrane Permeability; D016503:Drug Delivery Systems; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D000960:Hypolipidemic Agents / Q000008:administration & dosage* / Q000493:pharmacokinetics; D009682:Magnetic Resonance Spectroscopy; D008855:Microscopy, Electron, Scanning; D008958:Models, Molecular; D053758:Nanoparticles / Q000737:chemistry / Q000648:ultrastructure; D010316:Particle Size; D011109:Polymethacrylic Acids; D011341:Probucol / Q000008:administration & dosage* / Q000493:pharmacokinetics; D012967:Sodium Dodecyl Sulfate
D000960:Hypolipidemic Agents; D011109:Polymethacrylic Acids; C038300:methylmethacrylate-methacrylic acid copolymer; D012967:Sodium Dodecyl Sulfate; D011341:Probucol