A Biodegradable Copolyester, Poly(butylene succinate-<i>co</i>-ε-caprolactone), as a High Efficiency Matrix Former for Controlled Release of Drugs

oleh: Eduardo Galdón, Mónica Millán-Jiménez, Gloria Mora-Castaño, Antxon Martínez de Ilarduya, Isidoro Caraballo

Format: Article
Diterbitkan: MDPI AG 2021-07-01

Deskripsi

A biodegradable copolyester, poly(butylene succinate-<i>co</i>-ε-caprolactone) (PBS_CL), was used for first time as an excipient for pharmaceutical dosage forms using direct compression and hot processing techniques (ultrasound-assisted compression (USAC) and hot melt extrusion (HME)). Robust binary systems were achieved with hot processing techniques, allowing a controlled release of the drug. With only 12% <i>v</i>/<i>v</i> of PBS_CL, controlled release forms were obtained using USAC whereas in HME over 34% <i>v</i>/<i>v</i> of excipient is necessary. Amounts over 23% <i>v</i>/<i>v</i> allowed a long-extended release for more than 72 h following diffusional kinetic. Thanks to the high melting point of theophylline and the physicochemical properties of PBS_CL selected and synthesized, the structure of the excipient inside the USAC tablets and HME filaments corresponds to a continuum medium. A percolation threshold around 23% <i>v</i>/<i>v</i> was estimated, which agrees with a continuum percolation model. The polymer shows a high excipient efficiency value using HME and USAC. A nanostructured matrix with wall thicknesses lower than 0.1 µm was obtained. This leads to a very effective coating of the drug particles by the excipient, providing a slow and reproducible release. The present study therefore supports the use of PBS_CL, for the preparation of controlled release dosage forms using hot processing techniques.