Evaluation of the Hemocompatibility and Anticancer Potential of Poly(<i>ε</i>-Caprolactone) and Poly(3-Hydroxybutyrate) Microcarriers with Encapsulated Chrysin

• Main Authors: Eleftherios Halevas (Author), Chrysoula Kokotidou (Author), Elda Zaimai (Author), Alexandra Moschona (Author), Efstratios Lialiaris (Author), Anna Mitraki (Author), Theodore Lialiaris (Author), Anastasia Pantazaki (Author)
• Format: Book
• Published: MDPI AG, 2021-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.
• Notes: 10.3390/pharmaceutics13010109; 1999-4923
• Keywords: chrysin; poly(<i>ε</i>-caprolactone) and poly(3-hydroxybutyrate) biodegradable polymers; drug micro-encapsulation and delivery; human blood compatibility; anticancer activity; Pharmacy and materia medica; RS1-441
• Source: Pharmaceutics, Vol 13, Iss 1, p 109 (2021)

In this work, novel chrysin-loaded poly(<i>ε</i>-caprolactone) and poly(3-hydroxybutyrate) microcarriers were synthesized according to a modified oil-in-water single emulsion/solvent evaporation method, utilizing poly(vinyl alcohol) surfactant as stabilizer and dispersing agent for the emulsification, and were evaluated for their physico-chemical and morphological properties, loading capacity and entrapment efficiency and in vitro release of their load. The findings suggest that the novel micro-formulations possess a spherical and relatively wrinkled structure with sizes ranging between 2.4 and 24.7 µm and a highly negative surface charge with <i>z</i>-potential values between (−18.1)-(−14.1) mV. The entrapment efficiency of chrysin in the poly(<i>ε</i>-caprolactone) and poly(3-hydroxybutyrate) microcarriers was estimated to be 58.10% and 43.63%, whereas the loading capacity was found to be 3.79% and 15.85%, respectively. The average release percentage of chrysin was estimated to be 23.10% and 18.01%, respectively. The novel micromaterials were further biologically evaluated for their hemolytic activity through hemocompatibility studies over a range of hematological parameters and cytoxicity against the epithelial human breast cancer cell line MDA-MB 231. The poly(<i>ε</i>-caprolactone) and poly(3-hydroxybutyrate) microcarriers reached an IC₅₀ value with an encapsulated chrysin content of 149.19 µM and 312.18 µM, respectively, and showed sufficient blood compatibility displaying significantly low (up to 2%) hemolytic percentages at concentrations between 5 and 500 µg·mL⁻¹.