Silymarin in liposomes and ethosomes: pharmacokinetics and tissue distribution in free-moving rats by high-performance liquid chromatography-tandem mass spectrometry.
The aim of this study was to prepare silymarin formulations (silymarin entrapped in liposomes and ethosomes, formulations referred to as LSM and ESM, respectively) to improve oral bioavailability of silymarin and evaluate its tissue distribution by liquid chromatography with tandem mass spectrometry (LC-MS/MS) in free-moving rats. Silibinin is the major active constituent of silymarin, which is the main component to be analyzed. A rapid, sensitive, and repeatable LC-MS/MS method was developed and validated in terms of precision, accuracy, and extraction recovery. Furthermore, the established method was applied to study the pharmacokinetics and tissue distribution of silymarin in rats. The size, ζ potential, and drug release of the formulations were characterized. These results showed that the LSM and ESM encapsulated formulations of silymarin may provide more efficient tissue distribution and increased oral bioavailability, thus improving its therapeutic bioactive properties in the body.
Institute of Traditional Medicine, National Yang-Ming University , Taipei 112, Taiwan.
Li-Wen
LW
Chang
Mei-Ling
ML
Hou
Tung-Hu
TH
Tsai
D000818:Animals; D002626:Chemistry, Pharmaceutical; D002851:Chromatography, High Pressure Liquid / Q000379:methods*; D004365:Drugs, Chinese Herbal / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D008081:Liposomes / Q000737:chemistry; D008297:Male; D020944:Silybum marianum / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012838:Silymarin / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D053719:Tandem Mass Spectrometry / Q000379:methods*; D014018:Tissue Distribution
D004365:Drugs, Chinese Herbal; D008081:Liposomes; D012838:Silymarin
encapsulated formulation; ethosome; liposome; pharmacokinetics; silymarin; tandem mass spectrometry