Biopharmaceutics studies applied to goyazensolide: a drug candidate from Lychnophora species

Abstract

Abstract Objectives To predict the substance’s behaviour in vivo and determine the viability of the bioactive substance to become a drug, this work aimed to evaluate the biopharmaceutics characteristics of goyazensolide. Methods Differential scanning calorimetry (DSC) and thermogravimetry (TG) were applied for the characterization of goyazensolide. The biopharmaceutics characteristics were evaluated using in-silico and in-vitro (shake-flask and Parallel Artificial Membrane Permeability Assay) methods. Key findings DSC curve showed a single endothermic peak. According to the TG curve, goyazensolide has thermal stability close to 221.0°C and 210.0°C, under a nitrogen and oxygen atmosphere, respectively. In-silico data indicated that goyazensolide has high solubility and low permeability. The high solubility was confirmed by equilibrium solubility studies determined by the shake-flask method. The dose/solubility ratio values were 175.16 ml (pH 1.2), 194.99 ml (pH 4.5) and 222.07 ml (pH 6.8). The effective permeability of 0.03 × 10−6 cm/s was obtained for goyazensolide. This value is lower than furosemide (1.03 × 10−6 cm/s), confirming the low permeability of goyazensolide. Conclusions Biopharmaceutics characteristics of goyazensolide are similar to drugs available on the market and attest to the feasibility of starting the process of developing a formulation containing this substance.