• Preparation and Characterization of AS1411 Aptamer-Targeted Solid Lipid Nanoparticles Containing Lawson for Enhanced Anticancer Efficacy
  • Sara Qeshlaqi,1 Armita Seddighi,2 Maryam Hashemi,3 Shiva GolMohamadzadeh,4 Zahra Salmasi,5,*
    1. Department of Pharmaceutical Nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
    2. Pharmacy Department,, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
    3. Department of Pharmaceutical Biotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
    4. Pharmacy Department,, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran
    5. Department of Pharmaceutical Nanotechnology, School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran


  • Introduction: Lawsone (LWS), a naphthoquinone-type dye with anticancer properties, faces challenges in aqueous solubility, affecting its medicinal benefits. Solid lipid nanoparticles (SLNs), known to enhance bioavailability of poorly soluble drugs, conjugated with aptamers provide a targeted and effective approach in cancer therapy, minimizing toxicity to healthy tissues. This study aimed to develop chitosan-coated LWS-loaded SLN conjugated with aptamer AS1411 (LWS-SLN-Chit-Apt) for cytotoxicity evaluation against mouse colon adenocarcinoma cells (C26).
  • Methods: First, the LWS-SLN were prepared using high-shear homogenization and ultrasound methods. Various tests including dynamic light scattering (DLS), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and fourier-transform infrared spectroscopy (FTIR) were conducted to determine the nanoparticle (NP) properties. The LWS-SLNs were then coated with chitosan and bound with AS1411 aptamer, confirmed by DLS and gel electrophoresis. Cytotoxicity was assessed using the MTT assay on mouse colon cancer (C26) and Chinese hamster ovary (CHO) cell lines, and cellular uptake was measured.
  • Results: The LWS-SLN and LWS-SLN-Chit-Apt showed a size of 160 ± 14.8 and 350 ± 22.5 nm, respectively with encapsulation efficiency of 70% ± 4.3, and continuous drug release over 120 hours. Higher cellular uptake and cytotoxicity were observed in C26 cells, as nucleolin-positive cells, with AS1411 aptamer-targeted NPs compared to non-targeted NPs, while no significant difference was noted in CHO cells.
  • Conclusion: Our findings suggest that the LWS-SLN-Chit-Apt formulation is a promising drug delivery system for enhancing the bioavailability of LWS and improving its therapeutic effects against cancer cells. This stable and non-invasive formulation shows promise as a candidate for in vivo and clinical studies.
  • Keywords: Targeted Drug Delivery, AS1411 Aptamer, Lawson, Solid Lipid Nanoparticle, Colon Cancer.