Poly (N-isopropylacrylamide)–PLA and PLA blend nanoparticles for temperature-controllable drug release and intracellular uptake

We designed a temperature-responsive and biodegradable novel drug-delivery carrier. A block copolymer, poly (N-isopropylacrylamide-dl-lactide) (PNIPAAm–PLA), was synthesized by the ring-opening polymerization of dl-lactide, and used as a carrier for a drug-delivery system. In this study, temperature-responsive nanoparticles (NPs) encapsulating betamethasone disodium 21-phosphate (BP) were prepared from a blend of PLA homopolymer and block copolymers by an oil-in-water solvent-diffusion method in the presence of zinc ion (PLA/PNIPAAm–PLA (NPs)). The resulting NP size was around 140 nm. The drug release from temperature-responsive NP could be controllable by changing the temperature. Moreover, a murine macrophage-like cell line, RAW 264.7 cells, was used to measure and image the cell uptake of fluorescent PLA/PNIPAAm–PLA NPs at 30 °C and 37 °C on the boundary of LCST (34 °C). Below the LCST, cellular uptake was not observed, but contrary to cellular uptake it was clearly observed above the LCST. Moreover, we found this effect to be useful for controlling the stealthiness by changing the temperature. Present temperature-responsive NPs have successfully exhibited thermo-responsive drug release and intracellular uptake while possessing a biodegradable character.

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► A temperature-responsive and biodegradable novel drug-delivery carrier was designed.
► Temperature-responsive nanoparticles (NPs) were prepared utilizing poly (N-isopropylacrylamide-dl-lactide) (PNIPAAm–PLA).
► NPs have successfully exhibited thermo-responsive drug release and intracellular uptake.
► PLA/PNIPAAm–PLA NP can be controlling the stealthiness by changing the temperature.
► NPs could allow controllable drug release and cellular uptake by changing the temperature.