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Preparation of the Rutin-SBA-16 Drug Delivery System

Journal of Biomaterials and Nanobiotechnology 2020年第1期11卷 1-13页

作者： Juliana Camila Fischer Karnopp teofilo fernando mazon cardoso Daniel Araujo Goncalves Aline Regina Hellman Carollo Gustavo Rocha de Castro Adriana Pereira Duarte Marco Antonio Utrera Martines Institute of Chemistry Federal University of Mato Grosso do SulCidade UniversitariaCampo GrandeMSBrazil Faculty of Pharmaceutical Sciences Food and NutritionFederal University of Mato Grosso do SulCidade UniversitariaCampo GrandeMSBrazil Department of Chemistry Minas Gerais State UniversityItuiutabaMGBrazil Institute of Biosciences Sao Paulo State UniversityBotucatuSPBrazil

This study sets out a scheme for a controlled release delivery system using SBA-16 as a carrier matrix and Rutin as a drug (Rutin-SBA-16). Physicochemical characterizations were performed to confirm the structure of the SBA-16 for post-synthesis by scanning electron microscopy (SEM), Transmission Electron Microscopy (TEM) and X-ray Diffraction (XRD). The presence of Rutin-SBA-16 was confirmed by Fourier-transform infrared spectroscopy (FTIR) and Nitrogen adsorption-desorption isotherms at 77 K. The dissolution kinetics was evaluated by the Zero Order, First Order and Higuchi models, and Rutin quantification was carried out by High Performance Liquid Chromatography (HPLC). The best impregnation time, which was 8 hours, adsorbing 284 μg Rutin per mg of silica, and the maximum degree of dissolution occurred in a period of 20 - 25 h. The release kinetics of the Rutin was called Higuchi, and showed high linearity, with a correlation coefficient (R2) of 0.999 compared with 0.905 and 0.980 of the zero order and first order models respectively. The study shows the benefits of Rutin-SBA-16 as a drug delivery system.

关键词： Rutin Controlled Release Systems Kinetic Study Mesoporous Silica Flavonoid

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Ursolic Acid Derivatives Induced Apoptosis and Reduces the NF-κB in Human Lung Adenocarcinoma Cells

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Journal of Cancer Therapy 2019年第10期10卷 863-876页

作者： Elaine Carlos Scherrer Ydia Mariele Valadares Caio Cesar Souza Alves Gabriella Freitas Ferreira Marcela Pereira Leao Jessica Aline Soares fernando Sa Silva Alessandra Paula Carli Oswaldo cardoso Jr. Fabiana Simao Machado Sandra Bertelli Ribeiro Castro Life Sciences Institute Federal University of Juiz de ForaGovernador ValadaresMGBrazil Faculty of Medicine Federal University of the Valleys of Jequitinhonha and MucuriTeofilo OtoniMGBrazil Department of Biochemistry and Immunology Federal University of Minas GeraisBelo HorizonteMGBrazil

Lung cancer is the major cause of death in the neoplastic diseases. In spite of the advances in the chemotherapy, the lung cancer treatments are still complex and costly, being necessary the seeking of new drugs. In this context, the ursolic acid (UA) becomes the target of studies that investigate its antitumor potential and, thus, structural modifications can enhance its biological activities. Eight UA semisynthetic derivative compounds (UAD1-8) were synthesized and evaluated their cytotoxic activity against human alveolar adenocarcinoma cells (A549). UAD1, UAD3, UAD5, UAD6 and UAD8 were able to reduce the viability of the A549 cells. Only UAD1 and UAD6 reduced the viability at 24 h, and only UAD3 didn’t reduce the NF-κB expression. The compound UAD1 showed the greater apoptosis induction. Moreover, the compound UAD1 showed better results than UA in all assays. The present study shows, for the first time, the action of these compounds in the apoptotic effect, in the expression of NF-κB and in the A549 cell line. The ursolic acid derivatives showed substantial results in the apoptosis, cytotoxicity and NF-κB inhibition of A549 cells, and further studies are necessary for the development of possible new therapeutic drugs.

关键词： Ursolic Acid Apoptosis NF-κB A549 Cells Tumoral

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