Hyaluronic acid (HA) coated irinotecan loaded lignin nanoparticles (HDLNPs) were synthesized using ionic interaction method. Optimized nanoparticles were characterized for their active chemotherapeutic targeting potential to CD44 receptors overly-expressed on cancer cells. Blood component interaction studies supported hemocompatible nature of HDLNPs and also demonstrated their sustained plasma residence property. Cell anti-proliferation and mitochondrial depolarization studies on HT-29 cells suggest significantly (p < 0.01) improved chemotherapeutic efficacy of HDLNPs. In vitro cell based studies showed that nanoparticles have retained antioxidant activity of lignin that can prevent cancer relapse. In vivo biodistribution studies in tumor-bearing Balb/c mice confirmed improved drug localization in tumor site for longer duration. Tumor regression and histopathological studies indicated the efficacy ofligand-assisted targeting chemotherapy over the conventional therapy. Hematological and biochemical estimation suggested that irinotecan-associated myelosuppression, liver steatosis and rare kidney failure can be avoided by its encapsulation in HA-coated lignin nanoparticles. HDLNPs were found to be stable over a period of 12 months.

Cell Biology Lab Dabur Research Foundation Ghaziabad UP India

Department of Pharmaceutics School of Pharmaceutical Education and Research Jamia Hamdard New Delhi India

Department of Pharmaceutics School of Pharmaceutical Sciences Delhi Pharmaceutical Sciences and Research University Govt of NCT of Delhi New Delhi India

Department of Production Engineering Warsaw University of Life Sciences Poland

Faculty of Business and Economics Mendel University in Brno Brno Czech Republic

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$a CD44 mediated colon cancer targeting mutlifaceted lignin nanoparticles: Synthesis, in vitro characterization and in vivo efficacy studies / $c L. Siddiqui, N. Hasan, PK. Mishra, N. Gupta, AT. Singh, A. Madaan, M. Jaggi, S. Saad, A. Ekielski, Z. Iqbal, P. Kesharwani, S. Talegaonkar

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$a Hyaluronic acid (HA) coated irinotecan loaded lignin nanoparticles (HDLNPs) were synthesized using ionic interaction method. Optimized nanoparticles were characterized for their active chemotherapeutic targeting potential to CD44 receptors overly-expressed on cancer cells. Blood component interaction studies supported hemocompatible nature of HDLNPs and also demonstrated their sustained plasma residence property. Cell anti-proliferation and mitochondrial depolarization studies on HT-29 cells suggest significantly (p < 0.01) improved chemotherapeutic efficacy of HDLNPs. In vitro cell based studies showed that nanoparticles have retained antioxidant activity of lignin that can prevent cancer relapse. In vivo biodistribution studies in tumor-bearing Balb/c mice confirmed improved drug localization in tumor site for longer duration. Tumor regression and histopathological studies indicated the efficacy ofligand-assisted targeting chemotherapy over the conventional therapy. Hematological and biochemical estimation suggested that irinotecan-associated myelosuppression, liver steatosis and rare kidney failure can be avoided by its encapsulation in HA-coated lignin nanoparticles. HDLNPs were found to be stable over a period of 12 months.

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$a Hasan, Nazeer $u Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India

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$a Mishra, Pawan K $u Faculty of Business and Economics, Mendel University in Brno, Brno, Czech Republic. Electronic address: pawan.mishra@mendelu.cz

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$a Ekielski, Adam $u Department of Production Engineering, Warsaw University of Life Sciences, Poland

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$a Iqbal, Zeenat $u Department of Pharmaceutics, School of Pharmaceutical Education and Research, Jamia Hamdard, New Delhi, India

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$a Talegaonkar, Sushama $u Department of Pharmaceutics, School of Pharmaceutical Sciences, Delhi Pharmaceutical Sciences and Research University, Govt. of NCT of Delhi, New Delhi, India. Electronic address: stalegaonkar@dpsru.edu.in

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