Chondrocyte affinity peptide modified PAMAM conjugate as a nanoplatform for targeting and retention in cartilage
Qing Hu1,2, Qing Chen3, Xiuyun Yan1
1Department of Pharmaceutics, College of Pharmaceutical Sciences, Soochow University, Suzhou 215123, PR China.
Aim:
To develop a nanocarrier for targeted delivery of agents to the cartilage.
Materials & Methods:
Chondrocyte affinity peptide modified PEGylated polyamidoamine conjugates (CAP-PEG-PAMAM) were prepared and rhodamine B isothiocyanate (RB) fluorophore was linked on them for comparative biological tracing and profiling.
Results:
CAP4-PP-RB exhibited much more efficient cellular uptake in vitro than that of PEG-PAMAM-RB. Both the conjugates were likely internalized by chondrocytes via clathrin and caveolin co-mediated endocytosis, and delivered to lysosomes. In vivo imaging demonstrated the fluorescein-labeled nanocarrier was capable to persist in the joint cavity of rats for a prolonged time. Furthermore, the CAP4-PEG-PAMAM showed a good biocompatibility and enhanced penetration effects in vivo.
Conclusion:
CAP-PEG-PAMAM could be an effective nanocarrier for intra-articular delivery of agents to cartilage.
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