Ligand-based targeted therapy: a novel strategy for hepatocellular carcinoma

Targeted delivery of microRNA‐199a‐3p using self‐assembled dipeptide nanoparticles efficiently reduces hepatocellular carcinoma in mice

“…On the other hand, carbohydrate based small molecules like galactose, galactosamine, lactobionic acid have been reported to possess high affinity for ASGPR and can easily be conjugated. Therefore, we chose LA which binds to ASGPR leading to internalization of the NPs through receptor mediated endocytosis as the ligand of choice for tumor targeting . Also, LA contains a free carboxylic group which could be exploited for conjugation with the amino terminus of short peptides.…”

“…Therefore, we chose LA which binds to ASGPR leading to internalization of the NPs through receptor mediated endocytosis as the ligand of choice for tumor targeting. (33) Also, LA contains a free carboxylic group which could be exploited for conjugation with the amino terminus of short peptides. Conjugation of LA with RDF NPs was carried out easily by EDC-NHS chemistry, did not alter the morphology of NPs but as expected led to an increase in the size from 20nm to 40nm.…”

Development of Asialoglycoprotein Receptor-Targeted Nanoparticles for Selective Delivery of Gemcitabine to Hepatocellular Carcinoma

“…Various targeting approaches have been explored to improve the pharmacotherapy of cytotoxic agents by delivering them to the tumor cells [4]. Among these, the active targeting of anticancer drugs by developing carrier systems with specific ligands has attained much attention [5]. Typically, these nano-sized ligand-bound systems will potentially transport the drug to the tumor site and bind effectively to the overexpressed target receptors in cancer cells.…”

“…On the other hand, polymeric nanocarriers have also demonstrated certain progress in targeting cancer cells in absence of ligands due to their higher permeability to the tumor vasculature, along with an enhanced permeability and retention effect [9,10]. Nevertheless, the pharmacological and therapeutic responses are improved when these carriers are combined with ligands [5,11].…”

Transferrin and folic acid co-modified bufalin-loaded nanoliposomes: preparation, characterization, and application in anti-cancer activity

“…17 Targeted nanoparticulate drug delivery systems, especially biodegradable nanoparticles, provide an opportunity to meet these existing challenges, with improved pharmacokinetics, benefits to drug accumulation in tumor tissue, and reduced side-effects. 18 Folate receptor (FR) combined with folic acid (FA) has high affinity and mediates its intracellular transport through receptor-mediated endocytosis. 19 There are three isoforms of FR (FRα, FRβ, and FRγ), and type α is the main subtype of FA transport.…”