Targeting cancer cells with biotin-dendrimer conjugates.
Star-burst dendrimers represent a superior carrier platform for targeted drug delivery. Partially acetylated generation 5 (G5) polyamidoamine (PAMAM) dendrimer was conjugated with the targeting moiety (biotin) and the imaging moiety (fluoresceinisothiocyanate, FITC), and the resulting dendrimer-biotin conjugate was characterized by (1)H NMR, UV-vis spectrum. As revealed by flow cytometry and confocal microscopy, the bifunctional conjugate (dendrimer-biotin-FITC) exhibited much higher cellular uptake into HeLa cells than the conjugate without biotin. The uptake was energy-dependent, dose-dependent, and could be effectively blocked by dendrimer-conjugated biotin. Our results indicated that the biocompatible biotin-dendrimer conjugate might be a promising nano-platform for cancer therapy and cancer diagnosis.
Yang
Wenjun
W
Hefei National Laboratory for Physical Sciences at Microscale and School of Life Sciences, University of Science and Technology of China, Hefei, Anhui 230027, China.
Cheng
Yiyun
Y
Xu
Tongwen
T
Wang
Xueyuan
X
Wen
Long-Ping
LP
D000970:Antineoplastic Agents / Q000008:administration & dosage; D001672:Biocompatible Materials / Q000138:chemical synthesis / Q000493:pharmacokinetics; D001710:Biotin; D050091:Dendrimers / Q000737:chemistry* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems / Q000379:methods*; D016650:Fluorescein-5-isothiocyanate; D006367:HeLa Cells; D006801:Humans; D009369:Neoplasms / Q000175:diagnosis / Q000628:therapy; D011073:Polyamines / Q000737:chemistry / Q000493:pharmacokinetics
D000970:Antineoplastic Agents; D001672:Biocompatible Materials; D050091:Dendrimers; C104700:PAMAM Starburst; D011073:Polyamines; D001710:Biotin; D016650:Fluorescein-5-isothiocyanate