Banca de QUALIFICAÇÃO: DANIELLE LIMA BEZERRA DE MENEZES

Uma banca de QUALIFICAÇÃO de MESTRADO foi cadastrada pelo programa.
STUDENT : DANIELLE LIMA BEZERRA DE MENEZES
DATE: 29/01/2020
TIME: 09:00
LOCAL: SALA 2 DO PPGCF
TITLE:

6CN LOADED HPMC MICROPARTICLES: PHYSICOCHEMICAL AND in vitro EVALUATION OF ANTIPROLIFERATIVE ACTIVITY

KEY WORDS:

microparticles, 2-aminothiophene, spray-drying.

PAGES: 54
BIG AREA: Ciências da Saúde
AREA: Farmácia
SUMMARY:

Cancer is a complex and heterogeneous diseases characterizad by disordered and uncontrolled cells proliferation capable of invading tissues. Conventional cancer chemotherapy still uses non specific drugs that can cause healthy tissue demage. Therefore, the search for new drug that are able to combine safety and efficacy remain as a challenge for the pharmaceutical industry. The 2-amine-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (6CN) has antiproliferative activity in human cancer cell lines. However, 6CN has physicochemical problems as low aqueous solubility and toxicity that limit its potential clinical utility. Polymeric microparticles (PM) are drug delivery systems that presented vantages as protection against external agents, modulated release to specific site of action, greater stability and bioavailability. Thus, this work aimed to develop HPMC loaded microparticles with 6CN in order to improve its physicochemical properties. Solubility assay of 6CN has been performed. Briefly, 20 mg of 6CN was added to 10 mL of dis distilled water. The suspensions formed were shaken at 25 ± 0.5 °C and 37 ± 0.5 °C for 72 hours, and then filtered through a 0.22 μm membrane filter to obtain a clear solution. The 6CN concentrations were determined using spectrophotometry in the UV region (294 nm). PM are produced by the spray-drying method with different active-polymer ratios (1:1, 1:2 and 1:3 w/w) under the conditions: inlet temperature 120°C, outlet temperature 80 °C, bower 6.5 and 0.1 MBa air atomization. The systems are studied by Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), thermogravimetric analysis (TG), x-ray diffraction (DRX) and scanning electron microscopy (SEM). In vitro MTT assays investigated the antiproliferative effect of the 6CN and MP3. The quantitative solubility in water at 25 °C was calculated as 0.023 mg/mL and the solubility in water at 37 °C was calculated as 0.040 mg/mL, wich classifies this drug as poorly soluble or insoluble in water. FTIR showed the interactions between the components of the formulation. Thermal analysis showed that the MP are thermally stable. X-ray analysis showed that MP masked the crystalline nature of 6CN. And SEM showed that the spray-drying method was efficient for producing well defined spherical microparticles with a smooth surface. The MTT assay indicated that 6CN demonstrated cytostatic and antiproliferative effects at 250 μg/mL after 72h of expusure and the MP3 enhancing its the cytostatic effect, increasing the antiproliferative activity. Thus, 6CN-loaded HPMC microparticles may be considered promising candidates for anticancer drugs.

BANKING MEMBERS:
Externa ao Programa - 1679481 - ANA PAULA BARRETO GOMES
Externo à Instituição - EDUARDO PEREIRA DE AZEVEDO - UnP
Presidente - 1893445 - EUZEBIO GUIMARAES BARBOSA