Development of nanoemulsions and solid lipid nanoparticles containing retinoic acid for treatment of solid tumors
Guilherme Carneiro Department of Pharmaceutics, Faculty of Pharmacy
Federal University of Minas Gerais
Brazil
Abstract:
All-trans retinoic acid (RA), a lipophilic vitamin A derivative, has been investigated in the chemoprevention and treatment of cancer. Due to the highly variable bioavailability of oral RA, development of alternative parenteral dosage forms is required. Despite nanoemulsions (NE) and solid lipid nanoparticles (SLN) can favorably alter the chemical stability and biological activities of RA, encapsulation efficiency (EE) in both systems is usually low, unless a high surfactant/lipid ratio is used. The principal aim of this study was to develop NE and SLN as carriers of RA using stearylamine (SA) to increase the EE. Both systems were prepared by hot homogenization method using an emulsification-ultrasound. The mean particle diameter, EE and zeta potential were carried out. The EE in NE with 0, 0,1 and 0,2% of SA was 62 ± 4,5; 98 ± 3,5 and 99 ± 3,5% respectively. In SLN with 0 and 0,2% of SA, the EE was 66 ± 1 and 101 ± 7%, respectively. Size ranged from 70 to 121 nm for NE and from 144 to 167 nm for SLN. Thus, formation of ion pairing between RA and SA increased the EE and possibly controlled release of RA from these systems can be promoted.
