Self-Assembled Polymeric Micelles for Targeted Dual-Drug Delivery to Neuroendocrine Tumors
Tugce Karatas, MSc – R&D Specialist, RS Research Inc.; Gulsah Nomak, MD – Medical Director, RS Research Inc.; Amitav Sanyal, PhD – Professor, Department of Chemistry, Bogazici University; Rana Sanyal, PhD – Professor, Department of Chemistry, Bogazici University
PhD Candidate Bogazici University İstanbul, Istanbul, Turkey
Introduction: Neuroendocrine tumors (NETs) pose significant challenges due to their heterogeneous nature and limited therapeutic options. NETs overexpress somatostatin and integrin αvβ3 receptors (1), yet conventional treatment with somatostatin analogues largely provide palliative benefit (2). Herein, we developed peptide-targeted polymeric micelles for combination therapy of NETs. Amphiphilic block copolymers that bear covalently bound 5-FU self-assemble into micelles that physically encapsulate a hydrophobic drug, while decoration of micelle corona with KE108, a novel SSTR targeting peptide, or cRGDfK enables receptor-mediated uptake to enhance selectivity and therapeutic efficacy.
Learning Objectives:
Understand the synthesis of amphiphilic 5-FU conjugated block copolymers for micelle formation and drug loading.
Recognize how peptide functionalization of the micelle corona enables receptor-mediated uptake in NETs.
Evaluate how using chemical conjugation along with physical drug loading enhances in vitro therapeutic efficacy.
