Conventional and PEGylated Liposomes as Vehicles of Copaifera sabulicola

Ian M R Blanco; Raquel de Melo Barbosa; Julita M P Borges; Silvio A B Vieira de Melo; Ramon Dos Santos El-Bachá; César Viseras; Patricia Severino; Elena Sanchez-Lopez; Eliana B Souto; Elaine Cabral-Albuquerque

doi:10.3390/pharmaceutics15020671

Conventional and PEGylated Liposomes as Vehicles of Copaifera sabulicola

Pharmaceutics. 2023 Feb 16;15(2):671. doi: 10.3390/pharmaceutics15020671.

Affiliations

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.

Keywords: Copaifera spp.; antitumor activity; astrocytes; copaiba oil; liposomes.

Grants and funding

This study was financed by the Coordenação de Aperfeiçoamento de Pessoal de Nível Superior—Brasil (CAPES)—Finance Code 001. This work was financed by national funds from FCT—Fundação para a Ciência e a Tecnologia, I.P., in the scope of the project UIDP/04378/2020 and UIDB/04378/2020 of the Research Unit on Applied Molecular Biosciences—UCIBIO and the project LA/P/0140/2020 of the Associate Laboratory Institute for Health and Bioeconomy—i4HB.