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

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

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

Biphasic gastroretentive drug delivery system of acyclovir: formulation and in vitro evaluation

A biphasic gastroretentive drug delivery system of acyclovir consisted of loading dose tablet and floating multiple matrix tablets was prepared by direct compression process. The delivery system was designed by hydroxy propyl methyl cellulose as retardant polymer with an effervescent component to get the desired buoyant and sustained release characteristics. All formulations compile within the limits. The FTIR studies did not show any evidence of an interaction between acyclovir and polymers. Dissolution studies revealed biphasic drug release pattern, with loading dose released within 30 min and floating multiple matrix tablets provided zero order sustained release profile for 12 h. It is concluded that floating multiple matrix tablets designed were particularly suitable as gastro retentive drug delivery system with anomalous non-fickian diffusion mechanism. The stability studies showed no significant change in dissolution profiles (f2 value > 50).Colegio de Farmacéuticos de la Provincia de Buenos Aire

Priprava i evaluacija dvofazičnih plutajućih tableta fenoverina

A biphasic gastroretentive drug delivery system of fenoverine was developed to maintain constant plasma concentration. The delivery system consisted of a loading-dose tablet and a floating multiple matrix tablet prepared by the direct compression process. The drug release from biphasic GRDDS in 0.1 mol L1 HCl and SGF (enzyme free) was sustained over 12 h with buoyant properties. Stability studies showed no significant change in dissolution profiles (f2 value > 50). Based on the release kinetics, it can be concluded that the floating multiple matrix tablet containing HPMC was a particularly suitable gastroretentive drug delivery system with a zero-order release profile.U radu je opisan razvoj bifazičnog sustava za isporuku fenoverina s produljenim zadržavanjem u želucu radi održavanja konstantne koncentracije lijeka u plazmi. Sustav je dobiven metodom izravne kompresije, a sastoji se od tablete za inicijalno doziranje i matriksne tablete za plutanje. Oslobađanje lijeka iz bifazičnog GRDDS u 0,1 mol L1 HCl i SGF (bez enzima) bilo je produljeno više od 12 h, a sustav je pokazao plutajuća svojstva. Ispitivanja stabilnosti pokazala su da nema značajne promjene u profilu oslobađanja (f2 > 50). Na temelju kinetike oslobađanja može se zaključiti da su plutajuće višeslojne matriksne tablete s HPMC posebno pogodan sustav za isporuku fenoverina u želucu s kinetikom oslobađanja nultog reda

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

Coupling FDM 3D Printing with Hot-Melt Extrusion to Produce Hypertensive Dual Therapy Fixed Dose Combination Tablet

Presenter: Abdullah Alzahranihttps://egrove.olemiss.edu/pharm_annual_posters_2021/1002/thumbnail.jp

Venlafaxine hydrochloride transdermal patches: effect of hydrophilic and hydrophobic matrix on in vitro characteristics

Transdermal drug delivery systems of venlafaxine hydrochloride were prepared by using combination of hydrophilic (HPMC E15) and hydrophobic (ERS100 and ERL 100) polymers in 1:5, 2:4, 3:3, 4:2, 5:1 ratios by solvent casting technique with 15 % v/w propylene glycol as plasticizer. The drug permeation studies revealed that drug permeation increased proportionally with increasing HPMC ratio where ERS 100 as hydrophobic polymer but in case of ERL 100 as hydrophobic polymer proportional increase was not obtained this may be due to increased diffusion path length. The drug permeation kinetics followed zero order profile with diffusion mechanism. The average steady state flux obtained with HPMC: ERL 100 (3:3) was 193.2 μg/cm2 /h and the same was increased to 257 μg/cm2 /h with the incorporation of 5 % v/w of dimethyl sulfoxide as permeation enhancer that was 3 fold of target flux (86 μg/cm2 /h). The FTIR studies showed drug-polymer compatibility.Colegio de Farmacéuticos de la Provincia de Buenos Aire

In vitro transcutaneous permeation of acyclovir sodium from HPMC gels: role of chemical permeation enhancers

The main objective of the present study is to improve the permeation of acyclovir sodium (ACV) across stratum corneum (SC) from HPMC gel formulations. We have also investigated the role of chemical permeation enhancers like dimethyl sulfoxide, ethanol, limonene and sodium taurodeoxycholate on the transcutaneous permeation of ACV from HPMC gels. The optimized formulations were characterized and subjected to in vitro permeation study using excised rat abdominal skin. The histological examination of the skin was studied to understand the mechanisms involved in the permeation of ACV across skin. The cumulative amount of ACV permeated and the increase in permeation parameters (Jss, Kp and ER) were significantly higher for gel formulations compared to marketed formulation. A 2 to 4 fold increase in enhancement ratio clearly indicates the potential of formulating ACV into a gel.Colegio de Farmacéuticos de la Provincia de Buenos Aire

Formulation and pharmacodynamic evaluation of meloxicam liquisolid compacts

The purpose of this study was to improve the meloxicam dissolution rate through its formulation into liquisolid compacts and then to evaluate the in vitro and in vivo performance of the prepared liquisolid compacts. Dissolution efficiency, mean dissolution time and relative dissolution rate of liquisolid compacts were calculated and compared to marketed formulation. The degree of interaction between the ME and excipients was studied by differential scanning calorimetry and X-ray diffraction were used and results revealed that, there was a loss of meloxicam crystallanity upon liquisolid formulation and almost molecularly dispersed state, which contributed to the enhanced drug dissolution properties. The optimized liquisolid compact showed higher dissolution rates and dissolution efficiency compared to commercial product. The analgesic and anti inflammatory response of optimized liquisolid compact in Swiss albino mice and Wistar rats was found to be superior compared to the marketed formulation.Colegio de Farmacéuticos de la Provincia de Buenos Aire