Desenvolvimento, caracterização físico-química e avaliação da eficiência de encapsulação de nanocápsulas poliméricas contendo hidroxitirosol

Abstract

Hydroxytyrosol (HT) is a naturally occurring phenolic phytochemical in extra virgin olive oil, and in the leaves of olive trees. It has antioxidant, anti-inflammatory and cancer-preventing potential. The objective of this work was to develop and evaluate polymeric nanoparticles containing HT, using the poly (ԑ-caprolactone) polymer - PCL - by the interfacial deposition method of the preformed polymer, varying the drug concentration in 2 mg / mL (NC-2 ) and 5 mg / mL (NC-5), in addition to the negative control (NC-0). Validation of the analytical method by UHPLC-PDA, characterization of systems containing HT (morphological, spectroscopic, and thermal methods) and evaluation of physical-chemical stability. The results of the validation of the analytical method as recommended by the National Health Surveillance Agency and The International Conference on Harmonization, obtained satisfactory results, with the ability to quantify the HT incorporated in the nanocapsules with efficiency encapsulation above 99.52%. No drug was observed in the surface morphological evaluation. Pure HT, polymers, physical mixture and polymeric nanocapsules were examined by X-ray diffraction, Fourier transform infrared (FTIR) and the viability of nanoencapsulation of HT was proven. In the study of physical-chemical stability, the formulations were monitored during 120 days of storage, in triplicate, monthly checking the pH, particle size, size distribution and zeta potential. In particle size, there was a significant difference for NC-2. The Polydispersity index (PDI) changed to NC-0 and NC-5 after 90 days and to NC-2 over 30 days, but the values remained acceptable below 0.3, satisfactory for pharmaceutical use. In the zeta potential, there was a change in all formulations after 60 days and accentuated in NC-0 and NC-2, in 90 days. The pH changes over 60 days in all samples, except for NC-2, which was after 90 days. During the study, all formulations remained with the same milky appearance, indicating good physical-chemical stability. The polymeric nanocapsules of HT are shown as a new effective pharmaceutical form, to guarantee the full potential of the drug, favorable to the treatment of several diseases.