Novel Hot Melt Extruded Matrices of Hydroxypropyl Cellulose and Amorphous Felodipine–Plasticized Hydroxypropyl Methylcellulose as Controlled Release Systems

Hydroxypropyl methylcellulose (HPMC) is a hydrophilic retarding-release polymer with the limited application in hot melt extrusion (HME) due to its high glass transition temperature (T_g181–191°C) and melt viscosity.

The aim of this study is to develop hot melt extruded matrices using hydroxypropyl cellulose (HPC) and felodipine (FLDP) with HPMC for controlled release and explore the relations of their specialty, processability, and structure with the product properties. Results showed that FLDP/HPC_EF/HPMC can be extruded at 160°C with torques not more than 0.5 N·m. The extruded matrices of FLDP/HPC_EF/HPMC_K15M (10:45:45 and 30:35:35) achieved the controlled release for 24 h. Rheological behaviors demonstrated that HPC_EF and FLDP were miscible with HPMC_K15M, attaining maximum 30% FLDP soluble in the molten mixtures.

HPC_EF and FLDP decreased the complex viscosity and plasticized HPMC_K15Mto improve the extrusion processing. DSC and FT-IR indicated that the molten soluble FLDP was amorphous in the extruded matrices by hydrogen bonding with HPC_EF/HPMC_K15M. SEM/energy-dispersive X-ray microanalysis illustrated that the microstructure of extrudates was surface dense and interior loose, and FLDP was homogenously dispersed.

Three-point bending test revealed that the plasticizers of HPC_EF and FLDP contributed differently to the mechanical properties. HPC_EF decreased the flexural modulus of HPMC_K15M while that of HPC_EF/HPMC_K15M was increased by FLDP. Besides controlled release, low moisture absorption and enhanced stability were also the correlated achievements. Therefore, HPC_EF-combined poorly water-soluble drugs to plasticize HPMC_K15M provide an alternative novel potential approach to realize the controlled-release delivery via HME. More on hotmelt extruded matrices