A New Liposomal Formulation of Hydrogenated Anacardic Acid to Improve Activities Against Cancer Stem Cells

• Published in: Natural product communications 2022-06, Vol.17 (6)
• Main Authors: Vien, Le Tri, Nga, Nguyen Thi, Hue, Phung Thi Kim, Kha, Tran Hoang Bao, Hoang, Nguyen Hong, Hue, Pham Thi, Thien, Pham Ngoc, Huang, Chi-Ying F, Van Kiem, Phan, Thao, Do Thi
• Format: Article
• Language: English
• ISSN: 1934-578X; 1555-9475
• DOI: 10.1177/1934578X221105696

Anacardic acid (AA) is a natural active ingredient that accounts for 65% of the liquid extract from the shell of the cashew nut. Due to the stronger cytotoxic activity of hydrogenated AA (HAA) against NTERA-2 cancer stem cells (CSCs) than AA itself, HAA was co-conjugated with CD133 monoclonal antibody (mAb^CD133) into nanoliposomal particles (AMC). This nanoliposomal complex is expected to improved HAA activities against CSCs based on the targeting capacity of mAb^CD133 toward CD133, a typical CSCs’ surface marker. AMC was manufactured with a mean size of 100.9 nm, a zeta potential of −40.7 mV, and a PDI of 0.283. We report a 100% encapsulation efficiency of HAA into liposomes and a 90.7% conjugation efficiency with mAb^CD133. The penetration of AMC into NTERA-2 CSCs after 2 h was 83.7%. The AMC complex inhibited NTERA-2 growth with an IC50 (inhibition concentration at 50%) value of 75.83  ±  6.70 µM, showing the targeting ability and lower toxicity (IC50 > 100 µM) on healthy cells. The AMC nanoparticles also demonstrated significant potential apoptotic induction by activating caspase 3 activity by up to 2.57 and 2.06 folds compared to that of the negative control at 20 and 4 µM, respectively. This induction was significant improvement in comparison with that of unconjugated HAA (P