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28 February 2007 Enhancing PDT drug delivery by enzymatic cleavage of porphyrin phosphates
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A new anionic porphyrin-phosphate conjugate has been made as the substrate of phosphatase to evaluate its cellular-uptake and potential targeting on cancer cells, taking advantage of the over-expression of phosphatases associated with the development of cancers. The phosphate groups increase the hydrophilicity of porphyrin dityrosine phosphate and facilitate its formulation in aqueous solvent. Upon hydrolysis by phosphatase after cellular uptaking, the more hydrophobic porphyrin-dityrosine promises to give better cellular retention. Indeed, the phosphate conjugate displayed a much better PDT effect than that of the parent porphyrin at the same concentration (10 &mgr;M) and light dosage on HeLa cells, indicating the enzyme-cleavage reaction occurred in HeLa cells plays a role. Photosenzitizers utilizing enzyme-cleavage might be a promising approach for photodynamic therapy.
© (2007) COPYRIGHT Society of Photo-Optical Instrumentation Engineers (SPIE). Downloading of the abstract is permitted for personal use only.
Bing Xu, Gaolin Liang, Ling Wang, Zhimou Yang, Kalok Chan, and Chi K. Chang "Enhancing PDT drug delivery by enzymatic cleavage of porphyrin phosphates", Proc. SPIE 6427, Optical Methods for Tumor Treatment and Detection: Mechanisms and Techniques in Photodynamic Therapy XVI, 64271A (28 February 2007);

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