Banca de DEFESA: DANIELLE LIMA BEZERRA DE MENEZES

Uma banca de DEFESA de MESTRADO foi cadastrada pelo programa.
STUDENT : DANIELLE LIMA BEZERRA DE MENEZES
DATE: 25/02/2021
TIME: 09:00
LOCAL: Videoconferência
TITLE:

Development of 6CN-loaded HPMC microparticles via spray-drying and in vitro cytotoxicity for drug delivery to cancer cells

KEY WORDS:

polymeric microparticles, 2-aminothiophene derivative, kinetics release, alamarBlue assay.

PAGES: 76
BIG AREA: Ciências da Saúde
AREA: Farmácia
SUMMARY:

2-amino-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carbonitrile (6CN) is a thiophene derivative with antiproliferative activity against cancer cell lines. However, presents low aqueous solubility which interferes its clinical use. This work aims to evaluate the influence of microencapsulation technique to developed a new system capable of modulate its release and improve the biological activity. 6CN-loaded hydroxypropyl methylcellulose (HPMC) microspheres employing the spray-drying method were developed with different drug-polymer ratios. These systems were characterized for drug content (%), infrared, scanning electron microscopy (SEM), X-ray diffraction (XRD), granulometric and differential scanning calorimetry (DSC) analysis. Plus, release kinetics and cytotoxicity activity in vitro by alamarBlue assay in human kidney embryo cells (HEK-293) and colon carcinoma cells (CT-26). The systems showed a drug content (%) between 70-80%, although losses during the developing process. Infrared results evidenced interactions between the components of the formulation. The granulometric analysis showed microparticles with an average size between 31-47 μm and SEM analysis showed particles with a well-defined and smooth spherical surface morphology. XRD and DSC analysis confirmed the 6CN crystalline nature. In contrast, in the systems it showed an amorphous state. The kinetics study with the dialysis method showed that after 10 hours almost 100% of 6CN was released in both medium (pH 1.2 and pH 7.4). The systems MP2 and MP3 were capable of promote a controlled release for 56 hours fitted the mono and biexponential model. The results of alamarBlue assay showed that 6CN, at concentrations between 5-50 μg/mL, demonstrated a protective activity in up to 48 hours. In CT-26 cells, no significant cytotoxic effect was observed. However, cells treated with MP3 at concentrations of 25 and 50 μg/mL, cell viability was reduced by 40 and 50%, respectively. Therefore, the data ensures that a microparticulate system obtained by spray-drying from HPMC was developed, capable of modifying the release of 6CN and interfering in the cell growth of CT-26 cells with potential for application in long-term treatments.

BANKING MEMBERS:
Presidente - 1789788 - ADLEY ANTONINI NEVES DE LIMA
Externo à Instituição - FABIO ROCHA FORMIGA - FIOCRUZ
Externo ao Programa - 2195251 - HUGO ALEXANDRE DE OLIVEIRA ROCHA