title: Development of silymarin self-microemulsifying drug delivery system with enhanced oral bioavailability.
abstract: The objective of this work was to develop a self-microemulsifying drug delivery system (SMEDDS) for improving oral absorption of poorly water-soluble drug, silymarin. The pseudo-ternary phase diagrams were constructed using ethyl linoleate, Cremophor EL, ethyl alcohol, and normal saline to identify the efficient self-microemulsification region. The particle size and its distribution of the resultant microemulsions were determined using dynamic light scattering. The optimal formulation with the best self-microemulsifying and solubilization ability consisted of 10% (w/w) of ethyl linoleate, 30% of Cremophor EL, and 60% of ethyl alcohol. The release of silymarin from SMEDDS was significantly faster than that from the commercial silymarin preparation hard capsule (Legalon). The bioavailability results indicated that the oral absorption of silymarin SMEDDS was enhanced about 2.2-fold compared with the hard capsule in fasted dogs. It could be concluded that SMEDDS would be a promising drug delivery system for poorly water-soluble drugs by the oral route.
authors.affiliation: Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing, China.
authors.forename: Xinru
authors.initials: X
authors.lastname: Li
authors.forename: Quan
authors.initials: Q
authors.lastname: Yuan
authors.forename: Yanqing
authors.initials: Y
authors.lastname: Huang
authors.forename: Yanxia
authors.initials: Y
authors.lastname: Zhou
authors.forename: Yan
authors.initials: Y
authors.lastname: Liu
mesh_terms: D000284:Administration, Oral; D000818:Animals; D000975:Antioxidants / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D004285:Dogs; D004337:Drug Carriers / Q000008:administration & dosage / Q000138:chemical synthesis*; D004339:Drug Compounding / Q000379:methods; D004655:Emulsions / Q000008:administration & dosage / Q000138:chemical synthesis*; D012838:Silymarin / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics*; D012995:Solubility
chemical_list: D000975:Antioxidants; D004337:Drug Carriers; D004655:Emulsions; D012838:Silymarin
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