Conclusion
Taken together, these findings suggest that TB-ATRA-loaded NLC represents a promising alternative to intravenous administration of ATRA in cancer treatment.
Methods
The influence of in situ formation of an ion pairing between ATRA and a lipophilic amine (benethamine) on the characteristics of NLC (size, zeta potential, encapsulation efficiency) was evaluated. TB, a butyric acid donor, was used as a component of the lipid matrix. In vitro activity on cell viability and distribution of cell cycle phases were evaluated for MCF-7, MDA-MB-231, HL-60 and Jurkat cell lines.
Results
The presence of the amine significantly increased the encapsulation efficiency of ATRA in NLC. Inhibition of cell viability by TB-ATRA-loaded NLC was more pronounced than the free drug. Analysis of the distribution of cell cycle phases also showed increased activity for TB-ATRA-loaded NLC, with the clear effect of cell cycle arrest in G0/G1 phase transition. The presence of TB played an important role in the activity of the formulation.