An investigation of the thermodynamic miscibility between VeTPGS and polymers.
Within the past decade, more than half of the drug candidates generated are poorly water soluble and therefore overcoming the low aqueous solubility of drug candidates becomes critical for product development. Vitamin E TPGS (VeTPGS), a non-ionic surfactant, has been used in both liquid and solid dosage forms to solubilize compounds and improve their bioavailability. To prepare solid dosage forms using VeTPGS, VeTPGS is often mixed with other excipients, mostly polymers. However, there is still a lack of understanding of miscibility between VeTPGS and polymers from a thermodynamic point of view. In this paper, the miscibility of VeTPGS with polymers has been studied in the light of the Flory-Huggins (F-H) theory with an objective to understand the effect of dispersion forces (solubility parameter) and nondispersive interactions on the miscibility between VeTPGS and polymers. A series of polymers with similar solubility parameters and structure similarity were selected. Binary blends of polymers and VeTPGS were prepared using a vapor evaporation technique followed by XRPD, DSC, and SEM characterization. Results suggest that the miscibility between VeTPGS and PMMA is very likely due to a specific interaction between the hydrophobic portion of VeTPGS (Vitamin E) and PMMA.
Li
Jinjiang
J
Department of Pharmaceutics, Boehringer Ingelheim Pharmaceuticals Inc., Ridgefield, CT 06887, USA. jinjiang@bms.com
Chiappetta
Doris
D
D002152:Calorimetry, Differential Scanning; D011092:Polyethylene Glycols / Q000737:chemistry; D019904:Polymethyl Methacrylate / Q000737:chemistry*; D012995:Solubility; D013816:Thermodynamics; D014810:Vitamin E / Q000031:analogs & derivatives* / Q000737:chemistry; D014961:X-Ray Diffraction
D014810:Vitamin E; D011092:Polyethylene Glycols; D019904:Polymethyl Methacrylate; C014225:tocophersolan