Novel poly(ester amide) derived from tyrosine amino acid for targeted pulmonary drug delivery of fluticasone propionate

Abstract

Nanoaggregates made from amino acid-based polymers have been an important platform for targeted drug delivery systems such as the lungs. Therefore, the aim of the present study is to develop tyrosine-based poly(ester amide)s (Tyr-PEA) for dry powder inhaler (DPI) of a potent drug (fluticasone propionate [FP]) using interfacial polymerization. The molecular and surface profiling characteristics were evaluated using Fourier-transformed infrared spectroscopy, X-ray diffraction, transmission electron microscopy, particle size analysis, nuclear magnetic resonance, differential scanning calorimetry, and scanning electron micrographs. The aerodynamic performance was evaluated using the NGI. The results confirmed the formation of the PEA and FP-loaded Tyr-PEA with an average particle size of, 45.39 ± 6.32 nm. The produced FP/Tyr-PEA showed entrapment efficiency and encapsulation capacity of FP of 92.32% and 0.526% respectively, which enabled the delivery of this potent drug in a reasonable dose. The in-vitro performance of the FP-loaded PEA was compared to a marketed product and results revealed a significant enhancement of the emitted dose (87.29% vs. 59% respectively [t-test, p < 0.05]). FP-loaded Tyr-PEA produced a higher respirable dose when compared to the marketed FP DPI (48.63 μg vs. 34.15 μg). Overall, FP-loaded Tyr-PEA was successfully prepared with optimal performance. Tyr-PEA-based nanoparticles provide a potential platform for targeted drug delivery, particularly potent actives.