RESUMO
Despite advances in neuroscience cancer research during the past decades, the survival of cancer patients has only marginally improved and the cure remains unlikely. The blood-brain barrier (BBB) is a major obstacle protecting the entry of therapeutic agents to central nervous system, especially for primary central nervous system lymphoma (PCNSL). Thus, the use of small nanoparticle as a drug carrier may be new strategies to overcome this problem. In this study, we fabricated liposome consisting of superparamagnetic iron oxide nanoparticles (SPIONs) functionalized with anti-CD20 (Rituximab; RTX). The designed nanoparticles have a theranostic property which is not only to improve drug delivery, but also to offer diagnostic and monitoring capabilities. TEM images revealed the spherical shape of liposome with the approximately average diameters about 140-190nm with slightly negatively charge surfaces. Superparamagnetic property of SPIONs-loaded liposomes was confirmed by VSM. Liposome colloidal could be prolonged at 4°C and 25°C storages. RTX conjugated liposome induced cell internalization and apoptosis effect in B-lymphoma cells. Drug targeting and therapeutic effect was investigated in BBB model. The result confirmed that liposome nanocarrier is required as a drug carrier for effectively RTX across the BBB.
Assuntos
Neoplasias do Sistema Nervoso Central/tratamento farmacológico , Compostos Férricos/química , Linfoma/tratamento farmacológico , Nanopartículas de Magnetita/química , Rituximab/administração & dosagem , Ensaios Antitumorais Modelo de Xenoenxerto , Animais , Antineoplásicos Imunológicos/administração & dosagem , Antineoplásicos Imunológicos/química , Antineoplásicos Imunológicos/farmacocinética , Barreira Hematoencefálica/metabolismo , Linhagem Celular Tumoral , Neoplasias do Sistema Nervoso Central/metabolismo , Neoplasias do Sistema Nervoso Central/patologia , Portadores de Fármacos/química , Humanos , Lipossomos/química , Lipossomos/ultraestrutura , Linfoma/metabolismo , Linfoma/patologia , Fenômenos Magnéticos , Nanopartículas de Magnetita/ultraestrutura , Camundongos Nus , Rituximab/química , Rituximab/farmacocinética , Nanomedicina Teranóstica/métodosRESUMO
The complexation between two isomers of citral in lemongrass oil and varying types of cyclodextrins (CDs), α-CD, ß-CD, and HP-ß-CD, were studied by molecular modeling and physicochemical characterization. The results obtained revealed that the most favorable complex formation governing between citrals in lemongrass oil and CDs were found at a 1:2 mole ratio for all CDs. Complex formation between E-citral and CD was more favorable than between Z-citral and CD. The thermal stability of the inclusion complex was observed compared to the citral in the lemongrass oil. The release time course of citral from the inclusion complex was the diffusion control, and it correlated well with Avrami's equation. The release rate constants of the E- and Z-citral inclusion complexes at 50 °C, 50% RH were observed at 1.32×10(-2) h(-1) and 1.43×10(-2) h(-1) respectively.