Novel gastroretentive floating pulsatile drug delivery system produced via hot-melt extrusion and fused deposition modeling 3D printing

© 2020 by the authors. Licensee MDPI, Basel, Switzerland. This study was performed to develop novel core-shell gastroretentive floating pulsatile drug delivery systems using a hot-melt extrusion-paired fused deposition modeling (FDM) 3D printing and direct compression method. Hydroxypropyl cellulose (HPC) and ethyl cellulose (EC)-based filaments were fabricated using hot-melt extrusion technology and were utilized as feedstock material for printing shells in FDM 3D printing. The directly compressed theophylline tablet was used as the core. The tablet shell to form pulsatile floating dosage forms with different geometries (shell thickness: 0.8, 1.2, 1.6, and 2.0 mm; wall thickness: 0, 0.8, and 1.6 mm; and % infill density: 50, 75, and 100) were designed, printed, and evaluated. All core-shell tablets floated without any lag time and exhibited good floating behavior throughout the dissolution study. The lag time for the pulsatile release of the drug was 30 min to 6 h. The proportion of ethyl cellulose in the filament composition had a significant (p \u3c 0.05) effect on the lag time. The formulation (2 mm shell thickness, 1.6 mm wall thickness, 100% infill density, 0.5% EC) with the desired lag time of 6 h was selected as an optimized formulation. Thus, FDM 3D printing is a potential technique for the development of complex customized drug delivery systems for personalized pharmacotherapy

R19. Investigation of Taste Masking Efficiency of Caffeine Citrate by Lipids Utilizing Hot Melt Extrusion Technology

Corresponding author (Pharmaceutics and Drug delivery): Priyanka Srinivasan, [email protected]://egrove.olemiss.edu/pharm_annual_posters/1018/thumbnail.jp

R20. Development of sustained release gastroretentive floating tablets using HME coupled 3D printing: A QbD approach

Corresponding author (Pharmaceutics and Drug delivery): Nagireddy Dumpa, [email protected]://egrove.olemiss.edu/pharm_annual_posters/1019/thumbnail.jp

Formulation and development of orodispersible sustained release tablet of domperidone

Commercially available domperidone orodispersible tablets (ODT) are intended for immediate release of the drug, but none of them have been formulated for sustained action. The aim of the present research work was to develop and evaluate orodispersible sustained release tablet (ODT-SR) of domperidone, which has the convenience of ODT and benefits of controlled release product combined in one. The technology comprised of developing sustained release microspheres (MS) of domperidone, followed by direct compression of MS along with suitable excipients to yield ODT-SR which rapidly disperses within 30 seconds and yet the dispersed MS maintain their integrity to have a sustained drug release. The particle size of the MS was optimized to be less than 200 μm to avoid the grittiness in the mouth. The DSC thermograms of MS showed the absence of drug-polymer interaction within the microparticles, while SEM confirmed their spherical shape and porous nature. Angle of repose, compressibility and Hausner's ratio of the blend for compression showed good flowability and high percent compressibility. The optimized ODT-SR showed disintegration time of 21 seconds and matrix controlled drug release for 9 h. In-vivo pharmacokinetic studies in Wistar rats showed that the ODT-SR had a prolonged MRT of 11.16 h as compared 3.86 h of conventional tablet. The developed technology is easily scalable and holds potential for commercial exploitation

R17. Solid Crystal Suspensions of Carbamazepine using Hot-melt Extrusion: A Solubility Enhancement Approach

Corresponding author (Pharmaceutics and Drug delivery): Sagar Narala, [email protected]://egrove.olemiss.edu/pharm_annual_posters/1016/thumbnail.jp

Hot melt extrusion processing parameters optimization

© 2020 by the authors. Licensee MDPI, Basel, Switzerland. The aim of this study was to demonstrate the impact of processing parameters of the hot-melt extrusion (HME) on the pharmaceutical formulation properties. Carbamazepine (CBZ) was selected as a model water-insoluble drug. It was incorporated into Soluplus®, which was used as the polymeric carrier, to produce a solid dispersion model system. The following HME-independent parameters were investigated at different levels: extrusion temperature, screw speed and screw configuration. Design of experiment (DOE) concept was applied to find the most significant factor with minimum numbers of experimental runs. A full two-level factorial design was applied to assess the main effects, parameter interactions and total error. The extrudates’ CBZ content and the in vitro dissolution rate were selected as response variables. Material properties, including melting point, glass transition, and thermal stability, and polymorphs changes were used to set the processing range. In addition, the extruder torque and pressure were used to find the simplest DOE model. Each change of the parameter showed a unique pattern of dissolution profile, indicating that processing parameters have an influence on formulation properties. A simple, novel and two-level factorial design was able to evaluate each parameter effect and find the optimized formulation. Screw configuration and extrusion temperature were the most affecting parameters in this study

R13. Formulation development of loratadine immediate-release tablets using hot-melt extrusion coupled with 3d-printing technology

Corresponding author (Pharmaceutics and Drug delivery): Sundus Hussain Omari, [email protected]://egrove.olemiss.edu/pharm_annual_posters/1012/thumbnail.jp

R15. Development and characterization of hot-melt extruded ocular inserts of moxifloxacin for bacterial keratitis

Corresponding author (Pharmaceutics and Drug delivery): Ruchi Thakkar, [email protected]://egrove.olemiss.edu/pharm_annual_posters/1014/thumbnail.jp

Employing Hot-Melt Extrusion Technology to Enhance the Solubility of Cannabidiol (CBD)

Corresponding author (Pharmaceutics and Drug Delivery): Iman Taha, [email protected]://egrove.olemiss.edu/pharm_annual_posters_2022/1020/thumbnail.jp

Vacuum compression molding as a screening tool to investigate carrier suitability for hot-melt extrusion formulations

© 2020 by the authors. Licensee MDPI, Basel, Switzerland. Hot-melt extrusion (HME) is the most preferred and effective method for manufacturing amorphous solid dispersions at production scale, but it consumes large amounts of samples when used for formulation development. Herein, we show a novel approach to screen the polymers by overcoming the disadvantage of conventional HME screening by using a minimum quantity of active pharmaceutical ingredient (API). Vacuum Compression Molding (VCM) is a fusion-based method to form solid specimens starting from powders. This study aimed to investigate the processability of VCM for the creation of amorphous formulations and to compare its results with HME-processed formulations. Mixtures of indomethacin (IND) with drug carriers (Parteck® MXP, Soluplus®, Kollidon® VA 64, Eudragit® EPO) were processed using VCM and extrusion technology. Thermal characterization was performed using differential scanning calorimetry, and the solid-state was analyzed via X-ray powder diffraction. Dissolution studies in the simulated gastric fluid were performed to evaluate the drug release. Both technologies showed similar results proving the effectiveness of VCM as a screening tool for HME-based formulations