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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

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

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Author(s):
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]
Total Authors: 6
Affiliation:
[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
Total Affiliations: 3
Document type: Journal article
Source: Journal of Liposome Research; v. 22, n. 2, p. 89-99, JUN 2012.
Web of Science Citations: 18
Abstract

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)

FAPESP's process: 07/00161-3 - Study of effect of composition of liposome containing flavonoids on Complement System activation and oxidative metabolism of human neutrophils: implications in the stability and application of this delivery system in the therapy of inflammatory diseases
Grantee:Yara Maria Lucisano Valim
Support Opportunities: Regular Research Grants
FAPESP's process: 06/04398-5 - Study of the effect of Complement System activation in the stability of different compositions of liposomes containning flavonoids: selection of the delivery system more stable and evaluation of its applicability in the therapy of inflammatory diseases.
Grantee:Ana Paula Landi Librandi
Support Opportunities: Scholarships in Brazil - Post-Doctoral