title: Novel Controlled Release Polymer-Lipid Formulations Processed by Hot Melt Extrusion.
abstract: The aim of the study was to investigate the effect of novel polymer/lipid formulations on the dissolution rates of the water insoluble indomethacin (INM), co-processed by hot melt extrusion (HME). Formulations consisted of the hydrophilic hydroxypropyl methyl cellulose polymer (HPMCAS) and stearoyl macrogol-32 glycerides-Gelucire 50/13 (GLC) were processed with a twin screw extruder to produce solid dispersions. The extrudates characterized by X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC) and hot stage microscopy (HSM) indicated the presence of amorphous INM within the polymer/lipid matrices. In-line monitoring via near-infrared (NIR) spectroscopy revealed significant peak shifts indicating possible interactions and H-bonding formation between the drug and the polymer/lipid carriers. Furthermore, in vitro dissolution studies showed a synergistic effect of the polymer/lipid carrier with 2-h lag time in acidic media followed by enhanced INM dissolution rates at pH > 5.5.
authors.affiliation: School of Sciences, Faculty of Engineering and Science, University of Greenwich, Chatham Maritime, Kent, ME4 4TB, UK.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Maniruzzaman
authors.affiliation: School of Sciences, Faculty of Engineering and Science, University of Greenwich, Chatham Maritime, Kent, ME4 4TB, UK.
authors.forename: Muhammad T
authors.initials: MT
authors.lastname: Islam
authors.affiliation: Thermo Fisher Scientific, Stafford House, Boundary Way, Hemel Hempstead, HP2 7GE, UK.
authors.forename: Sheelagh
authors.initials: S
authors.lastname: Halsey
authors.affiliation: School of Sciences, Faculty of Engineering and Science, University of Greenwich, Chatham Maritime, Kent, ME4 4TB, UK.
authors.forename: Devyani
authors.initials: D
authors.lastname: Amin
authors.affiliation: School of Sciences, Faculty of Engineering and Science, University of Greenwich, Chatham Maritime, Kent, ME4 4TB, UK. d.douroumis@gre.ac.uk.
authors.forename: Dennis
authors.initials: D
authors.lastname: Douroumis
mesh_terms: D002152:Calorimetry, Differential Scanning / Q000379:methods; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D004339:Drug Compounding / Q000379:methods*; D005223:Fats / Q000737:chemistry; D005989:Glycerides / Q000737:chemistry; D006358:Hot Temperature; D006863:Hydrogen-Ion Concentration; D057927:Hydrophobic and Hydrophilic Interactions; D007213:Indomethacin / Q000737:chemistry*; D008055:Lipids / Q000737:chemistry*; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D009821:Oils / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D011108:Polymers / Q000737:chemistry*; D012995:Solubility; D014961:X-Ray Diffraction / Q000379:methods
chemical_list: D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005223:Fats; D005989:Glycerides; D008055:Lipids; D009821:Oils; D011108:Polymers; C071184:Gelucire 50-13; D011092:Polyethylene Glycols; C048331:hydroxypropylmethylcellulose acetate succinate; D008747:Methylcellulose; D007213:Indomethacin
keywords: controlled release; hot melt extrusion; in-line NIR; solid dispersions