We report the use of multifunctional dendrimer-modified multi-walled carbon nanotubes (MWCNTs) for targeted and pH-responsive delivery of doxorubicin (DOX) into cancer cells . In this study, amine-terminated generation five poly(amidoamine) (PAMAM) dendrimers modified with fluorescein isothiocyanate (FI) and folic acid (FA) were covalently linked to acid-treated MWCNTs, followed by acetylation of the remaining dendrimer terminal amines to neutralize the positive surface potential. The formed multifunctional MWCNTs (MWCNTs-G5-FI-FA-Ac) were characterized via different techniques. Then, the MWCNTs-G5-FI-FA-Ac was used to load DOX for targeted and pH-responsive delivery to cancer cells overexpressing high-affinity folic acid receptors (FAR). We showed that the MWCNTs-G5-FI-FA-Ac enabled a high drug payload and encapsulation efficiency both up to 98% and the formed DOX/MWCNT-G5-FI-FA-Ac complexes displayed a pH-responsive release property with fast DOX release under acidic environment. Importantly, the DOX/MWCNT-G5-FI-FA-Ac complexes displayed a therapeutic efficacy similar to that of free DOX, and were able to target to cancer cells overexpressing high-affinity FAR and effectively inhibit the growth of the cancer cells. The synthesized multifunctional dendrimer-modified MWCNTs may be used as a targeted and pH-responsive delivery system for targeting therapy of different types of cancer.

Targeted and pH-responsive delivery of doxorubicin to cancer cells using mutifunctional dendrimer-modified multi-walled carbon nanotubes

245th National Meeting (2013)

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