Folate-PEG-CKK2-DTPA, A Potential Carrier for Lymph-Metastasized Tumor Targeting
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A novel conjugate, Folate-PEG-CKK2-DTPA, was designed and prepared as a carrier for lymphatic metastasized tumor imaging diagnosis and targeting therapy.
Folate-PEG-CKK2-DTPA was synthesized and characterized by analysis High Performance Liquid Chromatography, Size Exclusive Chromatography and 1H-NMR. 99mTc-labeled conjugation was prepared, and in vivo quantitative biodistribution and SPECT imaging were studied after subcutaneously injected into the rats and rabbits, respectively. Cell uptake study was carried in a KB cell line using fluorescent methods. In vivo and ex vivo fluorescent imaging study was carried in tumor-bearing nude mouse to evaluate its targeting ability.
Folate-PEG-CKK2-DTPA was synthesized with high purity. Both in vivo biodistribution study and SPECT imaging study show the rapid direction and high distribution of the conjugation to the lymph nodes. The uptake of fluorescence-labeled Folate-PEG-CKK2-DTPA in human oral epidermis carcinoma cells was observed. In vivo and ex vivo fluorescent imaging study indicated it could accumulate in tumor region after vein tail injection in nude mouse.
All these findings suggested Folate-PEG-CKK2-DTPA as a novel and dependable carrier for tumor diagnosis and therapy, especially for lymph-metastasized tumors.
KEY WORDSfluorescent imaging folate-PEG-CKK2-DTPA lymph targeting radio active tracing tumor targeting
Bull Calf Serum
1-Ethyl-3-(3-dimethyllaminopropyl) carbodiimide hydrochloride
Fetal bovine serum
high-performance liquid chromatography
human oral epidermoid carcinoma
maleimide-polyethyl glycol-succinimidyl ester
Region of Interest
Single-Photon-Emission Computed Tomography
- 1H NMR
1H nuclear magnetic resonance
- 15.Oussoren C, Eling WMC, Crommelin DJA, Storm G, Zuidema J. The influence of the route of administration and liposome composition on the potential of liposomes to protect tissue against local toxicity of two antitumor drugs. Biochim Biophys Acta, Biomembranes. 1998;1369:159–72.CrossRefPubMedGoogle Scholar
- 21.Fisher RE, Siegel BA, Edell SL, Oyesiku NM, Morgenstern DE, Messmann RA, et al. Exploratory study of 99mTc-EC20 imaging for identifying patients with folate receptor-positive solid tumors. J Nucl Med. jnumed.107.049478 (2008).Google Scholar
- 26.Kaiser RLCE, Bossinger CD, Cook PI. Color test for detection of free terminal amino groups in the solid-phase synthesis of peptides. 1970;34:595–598.Google Scholar
- 37.Birn H, Nielsen S, Christensen EI. Internalization and apical-to-basolateral transport of folate in rat kidney proximal tubule. Am J Physiol Renal Physiol. 1997;272:F70–8.Google Scholar