gamma-Butyrolactone Copolymerization with the Well-Documented Polymer Drug Carrier Poly(ethylene oxide)-block-poly(epsilon-caprolactone) to Fine-Tune Its Biorelevant Properties
Abstrakt
Polymeric drug carriers exhibit excellent properties that advance drug delivery systems. In particular, carriers based on poly(ethylene oxide)-block-poly(epsilon-caprolactone) are very useful in pharmacokinetics.
In addition to their proven biocompatibility, there are several requirements for the efficacy of the polymeric drug carriers after internalization, e.g., nanoparticle behavior, cellular uptake, the rate of degradation, and cellular localization. The introduction of γ-butyrolactone units into the hydrophobic block enables the tuning of the abovementioned properties over a wide range.
In this study, a relatively high content of γ-butyrolactone units with a reasonable yield of approximate to 60% is achieved by anionic ring-opening copolymerization using 1,5,7-triazabicyclo[4.4.0]dec-5-ene as a very efficient catalyst in the nonpolar environment of toluene with an incorporated γ-butyrolactone content of approximate to 30%. The content of γ-butyrolactone units can be easily modulated according to the feed ratio of the monomers.
This method enables control over the rate of degradation so that when the content of γ-butyrolactone increases, the rate of degradation increases. These findings broaden the application possibilities of polyester-polyether-based nanoparticles for biomedical applications, such as drug delivery systems.