A biodegradable copolyester, poly(Butylene succinate-co-e-caprolactone), as a high efficiency matrix former for controlled release of drugs
A biodegradable copolyester, poly(butylene succinate-co-e-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 system...
| Autores: | , , , , |
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| Tipo de recurso: | artículo |
| Fecha de publicación: | 2021 |
| País: | España |
| Institución: | Universitat Politècnica de Catalunya (UPC) |
| Repositorio: | UPCommons. Portal del coneixement obert de la UPC |
| Idioma: | inglés |
| OAI Identifier: | oai:upcommons.upc.edu:2117/358265 |
| Acceso en línea: | https://hdl.handle.net/2117/358265 https://dx.doi.org/10.3390/pharmaceutics13071057 |
| Access Level: | acceso abierto |
| Palabra clave: | drugs -- Controlled release Biomedical materials Copolymers Poly(butylene succinate-co-e-caprolactone) Biodegradable polymer Ultrasound-assisted compression Hot melt extrusion Controlled release Nanostructured matrices Medicaments -- Alliberament retardat Materials biomèdics Copolímers Àrees temàtiques de la UPC::Enginyeria química |
| Sumario: | A biodegradable copolyester, poly(butylene succinate-co-e-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% v/v of PBS_CL, controlled release forms were obtained using USAC whereas in HME over 34% v/v of excipient is necessary. Amounts over 23% v/v 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% v/v 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. |
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