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Influence of Riboflavin Targeting on Tumor Accumulation and Internalization of Peptostar Based Drug Delivery Systems
Influence of Riboflavin Targeting on Tumor Accumulation and Internalization of Peptostar Based Drug Delivery Systems
- Source :
- Bioconjugate Chemistry, 31(12), 2691-2696. AMER CHEMICAL SOC
- Publication Year :
- 2020
-
Abstract
- Riboflavin carrier protein (RCP) and riboflavin transporters (RFVTs) have been reported to be highly overexpressed in various cancer cells. Hence, targeting RCP and RFVTs using riboflavin may enhance tumor accumulation and internalization of drug delivery systems. To test this hypothesis, butyl-based 3-arm peptostar polymers were synthesized consisting of a lysine core (10 units per arm) and a sarcosine shell (100 units per arm). The end groups of the arms and the core were successfully modified with riboflavin and the Cy-5.5 fluorescent dye, respectively. While in phosphate buffered saline the functionalized peptostars showed a bimodal behavior and formed supramolecular structures over time, they were stable in the serum maintaining their hydrodynamic diameter of 12 nm. Moreover, the polymers were biocompatible and the uptake of riboflavin targeted peptostars in A431 and PC3 cells was higher than in nontargeted controls and could be blocked competitively. In vivo, the polymers showed a moderate passive tumor accumulation, which was not significantly different between targeted and nontargeted peptostars. Nonetheless, at the histological level, internalization into tumor cells was strongly enhanced for the riboflavin-targeted peptostars. Based on these results, we conclude that passive accumulation is dominating the accumulation of peptostars, while tumor cell internalization is strongly promoted by riboflavin targeting.
- Subjects :
- Sarcosine
Polymers
media_common.quotation_subject
Riboflavin
Lysine
Biomedical Engineering
Pharmaceutical Science
Bioengineering
chemistry.chemical_compound
In vivo
Riboflavin-carrier protein
Materials Testing
Humans
Internalization
media_common
Pharmacology
Drug Carriers
Chemistry
Organic Chemistry
Membrane Transport Proteins
Biological Transport
Carbocyanines
Cancer cell
Drug delivery
PC-3 Cells
Biophysics
Biotechnology
Subjects
Details
- ISSN :
- 15204812
- Volume :
- 31
- Issue :
- 12
- Database :
- OpenAIRE
- Journal :
- Bioconjugate chemistry
- Accession number :
- edsair.doi.dedup.....427cf303cc41d46601f78f2854b2b603