Novel self-nanoemulsifying drug-delivery system enhances antileukemic properties of all-trans retinoic acid.
Gabriel Silva Marques BorgesMicael de Oliveira FerencsCristina de Mello Gomide LouresMostafa Al Abdel-SalamFernanda Cristina Gontijo EvangelistaCamila Campos SalesPedro Henrique Reis da SilvaRenata Barbosa de OliveiraÂngelo MalachiasMaria Irene YoshidaElaine Maria de Souza-FagundesAdriano de Paula SabinoChristian FernandesLucas Antônio Miranda FerreiraPublished in: Nanomedicine (London, England) (2020)
Aim: All-trans retinoic acid (ATRA) shows erratic oral bioavailability when administered orally against leukemia, which can be solved through its incorporation in self-nanoemulsifying drug-delivery systems (SEDDS). The SEDDS developed contained a hydrophobic ion pair between benzathine (BZT) and ATRA and was enriched with tocotrienols by the input of a palm oil tocotrienol rich fraction (TRF) in its composition. Results: SEDDS-TRF-ATRA-BZT allowed the formation of emulsions with nanometric size that retained ATRA within their core after dispersion. Pharmacokinetic parameters after oral administration of SEDDS-TRF-ATRA-BZT in mice were improved compared with what was seen for an ATRA solution. Moreover, SEDDS-TRF-ATRA-BZT had improved activity against HL-60 cells compared with SEDDS without TRF. Conclusion: SEDDS-TRF-ATRA-BZT is a promising therapeutic choice over ATRA conventional medicine.