4.7 Article

Perillaldehyde 1,2-epoxide Loaded SLN-Tailored mAb: Production, Physicochemical Characterization and In Vitro Cytotoxicity Profile in MCF-7 Cell Lines

Journal

PHARMACEUTICS
Volume 12, Issue 2, Pages -

Publisher

MDPI
DOI: 10.3390/pharmaceutics12020161

Keywords

perillaldehyde 1; 2-epoxide; Compritol ATO 888; cationic SLN; streptavidin adsorption; MCF-7 cells

Funding

  1. CNPq (Conselho Nacional de Desenvolvimento Cientifico e Tecnologico)
  2. CAPES (Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior)
  3. FAPITEC/SE (Fundacao de Apoio a Pesquisa e Inovacao Tecnologica do Estado de Sergipe)
  4. Portuguese Science and Technology Foundation [M-ERA-NET-0004/2015-PAIRED, UIDB/04469/2020]
  5. Ministry of Science and Education (FCT/MEC) through national funds
  6. FEDER

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We have developed a new cationic solid lipid nanoparticle (SLN) formulation, composed of Compritol ATO 888, poloxamer 188 and cetyltrimethylammonium bromide (CTAB), to load perillaldehyde 1,2-epoxide, and surface-tailored with a monoclonal antibody for site-specific targeting of human epithelial growth receptor 2 (HER2). Perillaldehyde 1,2-epoxide-loaded cationic SLN (cPa-SLN), with a mean particle size (z-Ave) of 275.31 +/- 4.78 nm and polydispersity index (PI) of 0.303 +/- 0.081, were produced by high shear homogenization. An encapsulation efficiency of cPa-SLN above 80% was achieved. The release of perillaldehyde 1,2-epoxide from cationic SLN followed the Korsemeyer-Peppas kinetic model, which is typically seen in nanoparticle formulations. The lipid peroxidation of cPa-SLN was assessed by the capacity to produce thiobarbituric acid-reactive substances, while the antioxidant activity was determined by the capacity to scavenge the stable radical DPPH. The surface functionalization of cPa-SLN with the antibody was done via streptavidin-biotin interaction, monitoring z-Ave, PI and ZP of the obtained assembly (cPa-SLN-S-Ab), as well as its stability in phosphate buffer. The effect of plain cationic SLN (c-SLN, monoterpene free), cPa-SLN and cPa-SLN-S-Ab onto the MCF-7 cell lines was evaluated in a concentration range from 0.01 to 0.1 mg/mL, confirming that streptavidin adsorption onto cPa-SLN-S-Ab improved the cell viability in comparison to the cationic cPa-SLN.

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