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

• Published in: Pharmaceutics Vol. 13; no. 1; p. 109
• Main Authors: Halevas, Eleftherios, Kokotidou, Chrysoula, Zaimai, Elda, Moschona, Alexandra, Lialiaris, Efstratios, Mitraki, Anna, Lialiaris, Theodore, Pantazaki, Anastasia
• Format: Journal Article
• Language: English
• Published: Switzerland MDPI AG 16-01-2021; MDPI
• Subjects: Acids; anticancer activity; Bioavailability; Biocompatibility; Biodegradable materials; Biodegradation; Biopolymers; Breast cancer; Chromatography; chrysin; Drug delivery systems; drug micro-encapsulation and delivery; human blood compatibility; Molecular weight; Particle size; Pharmaceutical industry; poly(ε-caprolactone) and poly(3-hydroxybutyrate) biodegradable polymers; Polymers; Scanning electron microscopy; Tissue engineering; United Kingdom > UK; United States > US; anticancer activity; drug micro-encapsulation and delivery; chrysin; human blood compatibility; poly(ε-caprolactone) and poly(3-hydroxybutyrate) biodegradable polymers
• ISSN: 1999-4923; 1999-4923
• DOI: 10.3390/pharmaceutics13010109

In this work, novel chrysin-loaded poly(
-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
-potential values between (-18.1)-(-14.1) mV. The entrapment efficiency of chrysin in the poly(
-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(
-caprolactone) and poly(3-hydroxybutyrate) microcarriers reached an IC
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
.