title: Effects of spray-drying and choice of solid carriers on concentrations of Labrasol® and Transcutol® in solid self-microemulsifying drug delivery systems (SMEDDS).
abstract: Solid self-microemulsifying drug delivery systems (SMEDDS) have been  used increasingly for improving the bioavailability of hydrophobic drugs. Labrasol® and Transcutol® are used widely as surfactant and solubilizer in the formulation of solid SMEDDS. We investigated the effects of spray-drying and the use of different solid carriers on concentrations of Labrasol® and Transcutol® in solid SMEDDS with scutellarin as the formulated drug. Liquid and gas chromatography tandem mass spectrometry (LC-MS and GC-MS) methods were developed for measuring low concentrations of Labrasol® and Transcutol®. In the preparation of solid SMEDDS, lactose, hydroxypropylmethyl cellulose (HPMC) and microcrystalline cellulose (MCC) were used as solid carriers. Judging from the retention ratios of Labrasol® and Transcutol®, the droplet size of solid SMEDDS increased after spray-drying of liquid SMEDDS, and concentrations of these excipients decreased after the solidifying procedure. In such reduction, Lactose and HPMC were found to preserve Labrasol® and Transcutol® better than MCC during spray-drying, and the resultant droplet sizes were smaller than that of MCC. Labrasol® and Transcutol® showed good thermal stability at 60 °C degree for 10 days. It can be concluded that spray-drying could increase the droplet size of solid SMEDDS and decreased the concentration of Labrasol® and Transcutol® therein, while water-soluble solid carriers could preserve Labrasol® and Transcutol® better than insoluble carriers in the solid SMEDDS.
authors.affiliation: State Key Laboratory for Quality Research in Chinese Medicine, Macau Institute for Applied Research in Medicine and Health, Macau University of Science and Technology, Taipa, Macau.
authors.forename: Liang
authors.initials: L
authors.lastname: Li
authors.forename: Tao
authors.initials: T
authors.lastname: Yi
authors.forename: Christopher Wai-Kei
authors.initials: CW
authors.lastname: Lam
mesh_terms: D047310:Apigenin / Q000737:chemistry*; D002482:Cellulose / Q000737:chemistry; D002626:Chemistry, Pharmaceutical; D003890:Desiccation; D004337:Drug Carriers / Q000737:chemistry*; D004339:Drug Compounding / Q000379:methods; D004355:Drug Stability; D045703:Emulsifying Agents / Q000737:chemistry*; D004655:Emulsions / Q000737:chemistry; D005026:Ethylene Glycols / Q000737:chemistry*; D005079:Excipients / Q000737:chemistry; D008401:Gas Chromatography-Mass Spectrometry / Q000592:standards; D005965:Glucuronates / Q000737:chemistry*; D005989:Glycerides; D065347:Hypromellose Derivatives; D007785:Lactose / Q000737:chemistry; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D009930:Organic Chemicals / Q000737:chemistry; D010316:Particle Size; D012015:Reference Standards; D012995:Solubility; D021241:Spectrometry, Mass, Electrospray Ionization / Q000592:standards
chemical_list: D004337:Drug Carriers; D045703:Emulsifying Agents; D004655:Emulsions; D005026:Ethylene Glycols; D005079:Excipients; D005965:Glucuronates; D005989:Glycerides; D009930:Organic Chemicals; C440220:Labrasol; C484876:scutellarin; D065347:Hypromellose Derivatives; D047310:Apigenin; D002482:Cellulose; D008747:Methylcellulose; C010111:carbitol; D007785:Lactose; C109691:microcrystalline cellulose