Conventional and PEGylated Liposomes as Vehicles of Copaifera sabulicola

Author:

Blanco Ian M. R.1,Barbosa Raquel de Melo2ORCID,Borges Julita M. P.3ORCID,de Melo Silvio A. B. Vieira1ORCID,El-Bachá Ramon dos Santos4ORCID,Viseras César2ORCID,Severino Patricia5ORCID,Sanchez-Lopez Elena678ORCID,Souto Eliana B.910ORCID,Cabral-Albuquerque Elaine1

Affiliation:

1. Industrial Engineering Program, Polytechnic School, Federal University of Bahia, Salvador 40210-630, Bahia, Brazil

2. Department of Pharmacy and Pharmaceutical Technology, School of Pharmacy, University of Granada, Campus of Cartuja s/n, 18071 Granada, Spain

3. Department of Science and Technology, State University of Southwestern Bahia, Salvador 45083-900, Bahia, Brazil

4. Laboratory of Neurochemistry and Cell Biology, Department of Biochemistry and Biophysics, Institute of Health Sciences, UFBA, Salvador 40170-110, Bahia, Brazil

5. Biotechnological Postgraduate Program, Tiradentes University, Aracaju 49010-390, Sergipe, Brazil

6. Department of Pharmacy, Pharmaceutical Technology and Physical Chemistry, Faculty of Pharmacy and Food Sciences, University of Barcelona, 08007 Barcelona, Spain

7. Institute of Nanoscience and Nanotechnology (IN2UB), University of Barcelona, 08007 Barcelona, Spain

8. Unit of Synthesis and Biomedical Applications of Peptides, IQAC-CSIC, 08034 Barcelona, Spain

9. UCIBIO—Applied Molecular Biosciences Unit, MEDTECH, Laboratory of Pharmaceutical Technology, Department of Drug Sciences, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal

10. Associate Laboratory i4HB, Institute for Health and Bioeconomy, Faculty of Pharmacy, University of Porto, 4050-313 Porto, Portugal

Abstract

Traditional medicine uses resin oils extracted from plants of the genus Copaifera for several purposes. Resin oils are being studied to understand and profile their pharmacological properties. The aim of this work was to prepare and to characterize conventional and pegylated liposomes incorporating resin oils or the hexanic extract obtained from Copaifera sabulicola (copaiba) leaves. The cytotoxic effect of these products was also investigated. Conventional and stealth liposomes with copaiba extract showed similar average diameters (around 126 nm), encapsulation efficiencies greater than 75% and were stable for 90 days. A cytotoxicity test was performed on murine glioma cells and the developed liposomes presented antiproliferative action against these cancer cells at the average concentration of 30 μg/mL. Phytochemicals encapsulated in PEGylated liposomes induced greater reduction in the viability of tumor cells. In addition, bioassay-s measured the cytotoxicity of copaiba resin oil (Copaifera sabulicola) in liposomes (conventional and PEGylated), which was also checked against pheochromocytoma PC12 cells. Its safety was verified in normal rat astrocytes. The results indicate that liposomes encapsulating copaiba oil showed cytotoxic activity against the studied tumor strains in a dose-dependent fashion, demonstrating their potential applications as a chemotherapeutic bioactive formulation.

Funder

Coordenação de Aperfeiçoamento de Pessoal de Nível Superior—Brasil

national funds from FCT—Fundação para a Ciência e a Tecnologia, I.P.

Research Unit on Applied Molecular Biosciences—UCIBIO

Associate Laboratory Institute for Health and Bioeconomy—i4HB

Publisher

MDPI AG

Subject

Pharmaceutical Science

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