Novel self-nanoemulsifying drug-delivery system enhances antileukemic properties of all- trans retinoic acid

Nanomedicine (Lond). 2020 Jun;15(15):1471-1486. doi: 10.2217/nnm-2020-0061. Epub 2020 Jun 17.

Abstract

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.

Keywords: acute promyelocytic leukemia; all-trans retinoic acid; hydrophobic ion pair; self-nanoemulsifying drug-delivery system; tocotrienols.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Administration, Oral
  • Animals
  • Biological Availability
  • Drug Delivery Systems*
  • Emulsions
  • Mice
  • Tretinoin*

Substances

  • Emulsions
  • Tretinoin