Faculty and Student Publications

Document Type

Article

Publication Date

1-1-2021

Abstract

The objective of this study was to assess the potential of Lutrol® F grades as polymeric surfactants for dissolution enhancement of Kollidon®VA64-drug matrices produced by hot-melt extrusion (HME). The poorly soluble model drug felodipine (FEL) with a medium melting point was selected for this study. Two different grades of Lutrol® F (also called Kolliphor® P grades) were added into the HME systems to investigate their influence on the drug-incorporated matrices. Two grades of Lutrols i.e., Lutrol® F 68 (Kolliphor®P 188) and Lutrol® F 127 (Kolliphor®P 407) were studied as polymeric solubilizers. FEL was mixed with Kollidon®VA64, with or without Lutrol®F (alone or in combination) at predetermined amounts which resulted in 8 different formulations. Each blend was melt-extruded at the same extrusion conditions. Differential scanning calorimetry (DSC) and powder X-ray diffraction (PXRD) analyses were performed to evaluate their physicochemical properties. DSC and PXRD studies suggested the formation of amorphous solid dispersion for all extruded formulations. Dissolution studies revealed that the extrudates with Lutrol® F grades exhibited faster and higher release compared to formulations without Lutrol® F grades. Formulations with high drug loading, which did not include Lutrol® F grades, demonstrated low drug release profiles when compared with the same formulations containing Lutrol® F grades. Fourier transform infrared (FTIR) studies suggested that a stronger hydrogen bond has occurred between the (-NH) of FEL and (C=O) of the pyrrolidone group in Kollidon® VA 64. Overall, these studies suggested the potential of Lutrols in enhancing the dissolution rate of poorly soluble model drug FEL.

Relational Format

journal article

DOI

10.32383/APPDR/138256

Accessibility Status

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