FDM 3D-Printed Sustained-Release Gastric-Floating Verapamil Hydrochloride Formulations with Cylinder, Capsule and Hemisphere Shapes, and Low Infill Percentage.

Haonan Qian,Guangrong Yan,Di Chen,Rui Li,Xiangyu Xu,Tianyuan Fan

doi:10.3390/pharmaceutics14020281

Haonan Qian, Guangrong Yan + Show 4 more

Open Access

https://doi.org/10.3390/pharmaceutics14020281

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Journal: Pharmaceutics	Publication Date: Jan 25, 2022
Citations: 16	License type: CC BY 4.0

Affiliation: Beihang University, Peking University

Abstract

The aim of this work was to design and fabricate fused deposition modeling (FDM) 3D-printed sustained-release gastric-floating formulations with different shapes (cylinder, capsule and hemisphere) and infill percentages (0% and 15%), and to investigate the influence of shape and infill percentage on the properties of the printed formulations. Drug-loaded filaments containing HPMC, Soluplus® and verapamil hydrochloride were prepared via hot-melt extrusion (HME) and then used to print the following gastric-floating formulations: cylinder-15, capsule-0, capsule-15, hemisphere-0 and hemisphere-15. The morphology of the filaments and the printed formulations were observed by scanning electron microscopy (SEM). The physical state of the drugs in the filaments and the printed formulations were characterized by X-ray diffraction (XRD), thermogravimetric analysis (TGA) and differential scanning calorimetry (DSC). The printed formulations were evaluated in vitro, including the weight variation, hardness, floating time, drug content and drug release. The results showed that the drug-loaded filament prepared was successful in printing the gastric floating formulations. Verapamil hydrochloride was proved thermally stable during HME and FDM, and in an amorphous state in the filament and the printed formulations. The shape and infill percentage of the printed formulations effected the hardness, floating time and in vitro drug release.

Highlights

The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, School Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China
Conclusions close to each other in order to ensure a similar rate for water penetrating into the formuThe drug-loaded hot-melt extrusion (HME) filament composed of HPMC, Soluplus®, PEG 400 and veralations
All the components were thermally stable throughout the whole preparation process and the verapamil hydrochloride was dispersed in an amorphous state, or molecularly

Summary

Introduction

The State Key Laboratory of Natural and Biomimetic Drugs, School of Pharmaceutical Sciences, School Beijing Key Laboratory of Molecular Pharmaceutics and New Drug Delivery Systems, School of Pharmaceutical Sciences, Peking University, Beijing 100191, China. The bioavailability of conventional oral dosage forms may be influenced by short gastro-retentive time or unpredictable gastric emptying times, especially for drugs which are absorbed in the upper part of the digestive system, or more soluble in acidic environments [2]. To solve this problem, a series of gastroretentive systems, including mucoadhesion systems, expandable systems and floating systems, were developed to prolong gastric residence time of drugs to obtain better drug absorption and bioavailability [3,4]. The gastro-floating systems are sometimes published maps and institutional affiliations

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