In vivo pharmacokinetics and biodistribution of novel all-trans retinoic acid derivative-loaded, folate-modified poly (l-amino acid) micelles

Folate is widely used as a target ligand for tumor cells, and poly (l-aspartic acid)-b-poly-(l-phenylalanine) (PAA-PPA) is a biodegradable material with low immunogenicity and toxicity. In this study, to enhance the targeting effect, folate-conjugated PAA-PPA micelles were synthesized. To evaluate the hypothesis, we assessed the pharmacokinetics and biodistribution of a new antitumor drug 4-amino-2-trifluoromethyl-phenyl retinate (ATPR) loaded into the micelles. We also observed in vivo imaging of 1,1′-dioctadecyl-3,3,3′,3′-tetramethylindotricarbocyanine iodide (DiR) loaded micelles to confirm distribution. The results showed that ATPR-loaded, folate-modified PAA-PPA displayed a prolonged circulation half-life and improved the targeting effect.

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