Desenvolvimento tecnológico e caracterização de micropartículas poliméricas contendo piperina obtidas por spray-drying

Abstract

Piperine (PIP) is an alkaloid found in fruits and roots of the pepper, in the Piper nigrum (Linnaeus) and Piper longum (Linnaeus) species that has been widely used because of its pharmacological activity, with anti-inflammatory, analgesic, anti-depressant and cytoprotective effects, antileukemic, antioxidant and its ability to increase the bioavailability of drugs. Another important activity of the PIP is its thermogenic and fat reducing effect, however, its high pungency does not allow the population to use it in higher doses. In order to improve the drug bioavailability and its antiobesity activity with possible reduction of side effects, microparticles were developed from the Eudragit® RS30D and S100 polymers by the spray drying method.The formulations were prepared in ethanol:water (50:50, v/v).Microparticles were obtained with yield (39.55% - 57.23%) and humidity (2.97% - 6.25%) suitable. The drug’s quantification was realized by ultra performance liquid chromatography analytical method developed and validated. The method demonstrated to be specific, linear (r = 0.9999), precise, accurate and robust in a range of 0.5 to 50.0 µg.mL-1 , with analysis and retention time of 2.0 and 1.5 minutes, respectively. The microparticles presented a rounded shape, with homogeneous characteristics, size between 1,37µm - 7,27 µm, with drug content between 66.36% and 90.15%. No chemical interactions was observed in the Fourier transformed infrared spectrum for microparticles. The thermal analysis and X ray diffraction indicated that the incorporation of PIP into the microparticles contributed to the amorphization of the drug. Thus we can conclude that piperine-containing polymeric microparticles were successfully obtained for the modified release of the drug, suggesting their use in the treatment of obesity with possible reduction of side effects.