NASCIMENTO, I. V. S R.; http://lattes.cnpq.br/2199374953830609; NASCIMENTO, Imarally Vitor de Souza Ribeiro.
Résumé:
Controlled drug delivery systems offer many advantages when compared to
other conventional dosage methods with biodegradable polysaccharides
gaining enough acceptance in the development of these systems. Chitosan is
an example of a biodegradable polysaccharide, whose rate of release can be
modulated from the ionic crosslinking with sodium tripolyphosphate (TPP).
Piperine is one of the major constituent of black pepper, having many
pharmacological actions that can cause the death of cancer cells and when
combined with chitosan has better bioavailability and faster action. Therefore,
this study aimed to develop and comparatively evaluate polymer membranes of
chitosan and crosslinked chitosan by TPP to be used in a controlled release
system of piperine, in order to obtain an alternative route for the administration
of this drug system. Piperine was added under constant stirring to the solution
of chitosan and membranes were obtained by the solvent evaporation method.
The developed membranes were characterized by the techniques of Infrared
Spectroscopy in the Region Fourier Transform (FTIR), X-ray Diffraction (XRD),
Optical Microscopy (OM), scanning electron microscopy (SEM), Energy
Dispersive Spectroscopy X-Ray (EDS), Thermogravimetric Analysis (TGA),
Scanning Calorimetry Analysis of Difference (DSC), Efficiency Charge (EC) by
liquid Chromatography Ultra Efficiency (HPLC), Assessment of Cell Viability of
Macrophages (MTT). It was observed by FTIR analysis, bands characteristic of
chitosan, the crosslinking agent and piperine, as well as bands characterizing
an interaction between chitosan and piperine. The XRD technique showed
change in semi-crystalline nature of chitosan in the presence of piperine and
tripolyphosphate. It was possible to see, through the techniques of OM and
SEM, changes in the morphology of the membrane containing piperine
compared to pure chitosan, with the presence of fibrillar particles. TG analysis
showed that, when piperine was added to the chitosan it provided a smaller
weight loss of the system, showing the interaction between chitosan and
piperine. DSC analysis showed that addition of piperine into chitosan provided
greater stability to the system. The charging efficiency test showed that the drug
can be entrapped by 57% in the uncrosslinked membranes and crosslinking
influenced the extraction of drug. The developed membranes showed cytotoxic
potential for human breast cancer cells MCF 7. Under the developed conditions
in this research, MQPR system was shown as a reference for drug delivery
testing and new biological tests. Given the above, the developed system is
presented as promising for obtaining a system for controlled release of drugs.