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

Abstract

A biodegradable copolyester, poly(butylene succinate-co-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% 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.

Poly(butylene succinate-co-ε-caprolactone) Copolyesters: Enzymatic Synthesis in Bulk and Thermal Properties

“…In an effort to improve those drawbacks, an enzymatic polymerization of PBSCL copolyesters using CALB catalyst from commercial monomers (CL, BD, and DMS) is proposed, which makes the reaction much simpler because the step of the formation of cycles is avoided. The use of this catalyst avoids the presence of metallic and organometallic compounds in the final polymer, which is an added benefit if the polymers are to be used for biomedical applications such as scaffolds, excipients for drug delivery systems [34], or sutures. A preliminary study of the kinetics of the reaction and a full characterization of the structure and thermal properties of the eco-friendly synthesized polymers are addressed.…”

Recent insight into the biomedical applications of polybutylene succinate and polybutylene succinate-based materials

“…In drug delivery systems, polymers are used to control the release of drugs into the body by either oral administration and/or implant [26]. A drug delivery system is used to sustain the release of drugs and avoid or minimize the daily taking of drugs as well as reduce the side effects [1]. Drug release depends on many factors to obtain the desired results.…”

“…Drug release depends on many factors to obtain the desired results. These factors include preparation method, distribution of drugs into the matrix, concentration of drug, and the interaction between drugs and polymer matrix [1,26]. For instance, the direct compression process has been used to develop a drug delivery system to control the release of drugs.…”

“…For instance, the direct compression process has been used to develop a drug delivery system to control the release of drugs. This is due to the low cost and industrial scalability of the process [1]. It was reported in the study of Llorens et al [26] that poor interaction between drug and polymer matrix resulted in drug migration.…”

“…In recent years, advances in material science have led to the discovery and development of novel biodegradable and biocompatible materials for biomedical applications as a substitute for non-biodegradable synthetic polymers [1]. Synthetic polymers contribute to waste disposal problems because they are resistant to microbial degradation [2].…”