Preparation of Biodegradable and Elastic Poly(ε-caprolactone-co-lactide) Copolymers and Evaluation as a Localized and Sustained Drug Delivery Carrier

Abstract

To develop a biodegradable polymer possessing elasticity and flexibility, we synthesized MPEG-b-(PCL-co-PLA) copolymers (PCxLyA), which display specific rates of flexibility and elasticity. We synthesize the PCxLyA copolymers by ring-opening polymerization of ε-caprolactone and l-lactide. PCxLyA copolymers of various compositions were synthesized with 500,000 molecular weight. The PCxLyA copolymers mechanical properties were dependent on the mole ratio of the ε-caprolactone and l-lactide components. Cyclic tensile tests were carried out to investigate the resistance to creep of PCxLyA specimens after up to 20 deformation cycles to 50% elongation. After in vivo implantation, the PCxLyA implants exhibited biocompatibility, and gradually biodegraded over an eight-week experimental period. Immunohistochemical characterization showed that the PCxLyA implants provoked in vivo inflammation, which gradually decreased over time. The copolymer was used as a drug carrier for locally implantable drugs, the hydrophobic drug dexamethasone (Dex), and the water-soluble drug dexamethasone 21-phosphate disodium salt (Dex(p)). We monitored drug-loaded PCxLyA films for in vitro and in vivo drug release over 40 days and observed real-time sustained release of near-infrared (NIR) fluorescence over an extended period from hydrophobic IR-780- and hydrophilic IR-783-loaded PCxLyA implanted in live animals. Finally, we confirmed that PCxLyA films are usable as biodegradable, elastic drug carriers.

Designing Molecular Building Blocks for Functional Polymersomes

“…By copolymerization of PCL with PLA the T g can be controlled and integration of PLA in the PCL polymer network also increased the elasticity, which is an important parameter for drug loading capacity in polymersomes. [26]…”

Effect of Ethylene Oxide and Gamma (γ-) Sterilization on the Properties of a PLCL Polymer Material in Balloon Implants

“…Flexibility in inflated balloons to withhold extreme muscular pressures relies on the physical properties of PLCL materials. 5,6 The composition of the PLCL consists of a soft matrix of a poly-ε-caprolactone (PCL) chain that provides a stable environment for the cellular matrix surrounding the balloons. 7−9 This helps to create a smooth balloon surface that reduces friction between the joints, providing improved shoulder movements and guaranteed pain reduction.…”

Effect of Drug Carrier Melting Points on Drug Release of Dexamethasone-Loaded Microspheres

“…Some Dex was remained inside the microspheres. The remained Dex within the microspheres after in vitro and in vivo release for 18 or 28 days were probably due to the incomplete biodegradation of microspheres, because we already reported 30-40% biodegradation of PLC with similar concentration even at 8 weeks [19,25]. Thus, we conjecture that the remained Dex can be completely release through biodegradation by in vitro and in vivo biological media after longer release period.…”