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.
Hefei National Laboratory for Physical Sciences at Microscale and School of Life Sciences, University of Science and Technology of China, Hefei, Anhui 230027, China.
Wenjun
W
Yang
Yiyun
Y
Cheng
Tongwen
T
Xu
Xueyuan
X
Wang
Long-Ping
LP
Wen
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