Abstract
SEDDS: NANOCARRIER SYSTEM FOR A NEW CARDIAC DYSFUNCTION DRUG

Beatriz Zanchetta, Marco Vinícius Chaud and Maria Helena Andrade Santana*

ABSTRACT

The aim of this research was to screen and select components for formulation development of a self-emulsifying drug delivery systems of LASSBio-294 (3,4-methylenedioxybenzoyl-2- thienylhy-drazone) for oral administration. The screened components were long and medium chain oils, surfactants with Hydrophile– Lipophile Balance between 4 to 17 and an alkane diol and glycil esther or glycol ether as cosurfactants. The selection was driven by the ability of selected surfactants to emulsifying the selected oils as well as by the properties of the emulsions such as mean diameter of the droplets, polydispersity index, zeta potential and turbidity. LASSBio-294 solubility was evaluated quantitatively in oils, surfactants and cosurfactants and by compatibility using DSC. Mean diameter, polydispersity index and zeta potential were evaluated by dynamic light scattering method, as well as turbidity. Labrafac PG, Labrasol, and Transcutol HP were selected as the best promising components for SEDDS development of LASSBio294. Although LASSBio-294 is more soluble in the surfactants than in the screened oils, the components were rapidly dispersed into fine droplets with mean diameter 176.83 nm, polydispersity index 0.216, turbidity 91.97 NTU, and zeta potential - 38.43 mV. The screening and selection of components allowed obtaining a nanosized emulsion with low polydispersity and electrostatic stability. This formulation in the SEEDS form is promising with carrier of LASSBio-294.

Keywords: Drug Delivery Systems, Emulsion, Lipids, Nanoparticles, Oral Drug Delivery, Poorly watersoluble drug, Self-emulsifying, Surfactant, Bioavailability, Biomimetics


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