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Published on: November 9, 2016
Biopharmaceutics studies applied to goyazensolide: a drug candidate from Lychnophora species
Iara Dévula Tiso Tana1, Dênia Antunes Saúde-Guimarães1, Tamires Guedes Caldeira1
1Programa de Pós-graduação em Ciências Farmacêuticas, Escola de Farmácia, Universidade Federal de Ouro Preto, Campus Universitário Morro do Cruzeiro, Ouro Preto, Minas Gerais, Brazil.
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.
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