Desenvolvimento tecnológico de micro e nanoformulações contendo dilapiol do óleo essencial de Piper aduncum da Amazônia

Abstract

Several resources of the Amazonian flora are known for their aromatic, pharmacological and cosmetic potential. The Amazonian Piperaceae botanical family stands out due to biological activities and the production of aromatic essential oils, such as the Piper aduncum species rich in dillapiole which is active for several pharmacological activities such as antibacterial, antifungal and anti-inflammatory. Essential oils, because they are lipophilic and hydrophobic, have limitations such as high volatility, low stability, bioavailability and solubility that triggers less use of these inputs for the pharmaceutical and cosmetic industry. The phenylpropanoid dillapiole of the essential oil of P. aduncum, which has great pharmaceutical potential, in which complexations were made with cyclodextrins (CDs), microemulsions, nanoemulsions and nanostructured lipid carriers that are convenient technological alternatives to solve these limitations, and may provide more soluble derivatives, stable, greater bioavailability and retention time of active substances. This work aims to analyze different methodologies for incorporating dillapiole from the essential oil of P. aduncum from the Amazon into pharmaceutical technologies such as nanoformulations, microemulsions and inclusion complex with cyclodextrins, in order to obtain viable innovative products for pharmaceutical and cosmetic use. The oils were obtained by the hydrodistillation technique and by steam dragging in an electric extractor. Then, the main constituents were fractionated and isolated by chromatographic techniques and analyzed by spectrometric techniques. The inclusion complexes were made with β-cyclodextrin and Hydroxypropyl-β-cyclodextrin by physical mixing, malaxagem and slurry methods. The microemulsions were made by the pseudoternary phase diagram, the nanoemulsion and the nanostructured lipid carrier were carried out using the high pressure homogenization technique and also thickened them in hydrogels. Physical-chemical analyzes were performed in all formulations. In the nanos, the release of substances and topical permeation and the toxicity profile were evaluated. The antibacterial and antibiotic modulating activities were performed on the microemulsion and inclusion complexes. The microemulsions were 167 nm in size with 10% dillapiole. The antimicrobial and modulating activity with the complexes and microemulsion showed modulation of the antibiotics ampicillin and vancomycin for the bacteria Staphylococcus aureus and Enterococcus faecalis. The release and topical permeation of the nanos and hydrogels that presented nanometric sizes in the range of 118 and 134 nm, presented controlled release profiles in comparison with the pure substance and the low toxicity levels. The micro and nanotechnologies in bioactive essential oils from the Amazon allow greater pharmacological and cosmetic exploration of these natural sources, increasing their economic potential, greater knowledge of Amazonian biodiversity and the elaboration of a new highly efficient pharmacological bioproduct.