Study of quercetin-loaded liposomes as potential drug carriers: in vitro evaluation of human complement activation

Autor(es)

Landi-Librandi, Ana Paula ^[1] ; Chrysostomo, Tais Nader ^[1] ; Caleiro Seixas Azzolini, Ana Elisa ^[1] ; Marzocchi-Machado, Cleni Mara ^[2] ; de Oliveira, Carlos Alberto ^[3] ; Lucisano-Valim, Yara Maria ^[1]

Afiliação do(s) autor(es)

^[1] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Dept Quim & Fis, BR-14040903 Ribeirao Preto, SP - Brazil

^[2] Univ Sao Paulo, Fac Ciencias Farmaceut Ribeirao Preto, Dept Anal Clin Toxicol & Bromatol, BR-14040903 Ribeirao Preto, SP - Brazil

^[3] Univ Fed Uberlandia, Inst Quim, Ctr Ciencias Exatas & Tecnol, BR-38400100 Uberlandia, MG - Brazil

• Tipo de documento: Artigo Científico
• Fonte: Journal of Liposome Research; v. 22, n. 2, p. 89-99, JUN 2012.
• Citações Web of Science: 18

Resumo

Liposomes have been employed as potential drug carriers. However, after their in vivo administration, they can be destabilized by proteins of complement system, contributing to the clearance of vesicles from blood circulation. Antioxidant flavonoids such as quercetin have been reported to be beneficial to human health, but their low water solubility and bioavailability limit their enteric administration. Therefore, the development of appropriate flavonoid-carriers could be of great importance to drug therapy. The aim of the present study was to evaluate the activation of human complement system proteins by liposomes composed of soya phosphatidylcholine (SPC) and cholesterol (CHOL) or cholesteryl ethyl ether (CHOL-OET) loaded with quercetin or not. The consumption of complement, via classical (CP) and alternative (AP) pathways, by different vesicles was evaluated using a hemolytic assay and quantitative determination of iC3b and natural antibodies deposited on empty liposomal surfaces by ELISA. The main results showed that empty liposomes composed of large amounts of CHOL consumed more complement components than the others for both CP and AP. Furthermore, replacement of CHOL with CHOL-OET reduced complement consumption via both CP and AP. Incorporation of quercetin did not change CP and AP consumption. Deposition of iC3b, IgG and IgM in vesicles composed of SPC: CHOL-OET at a molar ratio of 1.5:1 was lower compared to the others. Taken together, these observations suggest that liposomes composed of SPC: CHOL-OET at a molar ratio of 1.5:1 are the most appropriate among the vesicles studied herein to be used as a drug carrier system in further investigations. (AU)

• Processo FAPESP: 07/00161-3 - Estudo do efeito da composição de lipossomas contendo flavonóides na ativação do sistema complemento e no metabolismo oxidativo de neutrófilos humanos: implicações na estabilidade e aplicação deste sistema de liberação na terapia de doenças inflamatórias
• Beneficiário: Yara Maria Lucisano Valim
• Modalidade de apoio: Auxílio à Pesquisa - Regular
• Processo FAPESP: 06/04398-5 - Estudo in vitro do efeito da ativação do Sistema Complemento na estabilidade de lipossomas de diferentes composições contendo flavonóides: seleção do sistema de liberação mais estável e avaliação da sua aplicabilidade na terapia de doenças inflamatórias.
• Beneficiário: Ana Paula Landi Librandi
• Modalidade de apoio: Bolsas no Brasil - Pós-Doutorado