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Novel Self-Nanoemulsifying Drug-Delivery System Enhances Antileukemic Properties of All- Trans Retinoic Acid

2020; Future Medicine; Volume: 15; Issue: 15 Linguagem: Inglês

10.2217/nnm-2020-0061

1748-6963

Gabriel Silva Marques Borges, Micael de Oliveira Ferencs, Cristina de Mello Gomide Loures, M. A. Abdelsalam, Fernanda Cristina Gontijo Evangelista, Camila Campos Sales, Pedro Henrique Reis da Silva, Renata Barbosa de Oliveira, Ângelo Malachias, María Irene Yoshida, Elaine M. Souza–Fagundes, Adriano de Paula Sabino, Christian Fernandes, Lucas Antônio Miranda Ferreira,

Nanoparticle-Based Drug Delivery

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.