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Receptor-mediated Uptake of Folic Acid-functionalized Dextran Nanoparticles for Applications in Photodynamic Therapy.


ABSTRACT: In photodynamic therapy (PDT), photosensitizers and light are used to cause photochemically induced cell death. The selectivity and the effectiveness of the phototoxicity in cancer can be increased by a specific uptake of the photosensitizer into tumor cells. A promising target for this goal is the folic acid receptor ? (FR?), which is overexpressed on the surface of many tumor cells and mediates an endocytotic uptake. Here, we describe a polysaccharide-based nanoparticle system suitable for targeted uptake and its photochemical and photobiological characterization. The photosensitizer 5, 10, 15, 20-tetraphenyl-21H, 23H-porphyrine (TPP) was encapsulated in spermine- and acetal-modified dextran (SpAcDex) nanoparticles and conjugated with folic acid (FA) on the surface [SpAcDex(TPP)-FA]. The particles are successfully taken up by human HeLa-KB cells, and a light-induced cytotoxicity is observable. An excess of free folate as the competitor for the FR?-mediated uptake inhibits the phototoxicity. In conclusion, folate-modified SpAcDex particles are a promising drug delivery system for a tumor cell targeted photodynamic therapy.

SUBMITTER: Butzbach K 

PROVIDER: S-EPMC6572481 | biostudies-literature | 2019 May

REPOSITORIES: biostudies-literature

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Receptor-mediated Uptake of Folic Acid-functionalized Dextran Nanoparticles for Applications in Photodynamic Therapy.

Butzbach Kathrin K   Konhäuser Matthias M   Fach Matthias M   Bamberger Denise N DN   Breitenbach Benjamin B   Epe Bernd B   Wich Peter R PR  

Polymers 20190516 5


In photodynamic therapy (PDT), photosensitizers and light are used to cause photochemically induced cell death. The selectivity and the effectiveness of the phototoxicity in cancer can be increased by a specific uptake of the photosensitizer into tumor cells. A promising target for this goal is the folic acid receptor α (FRα), which is overexpressed on the surface of many tumor cells and mediates an endocytotic uptake. Here, we describe a polysaccharide-based nanoparticle system suitable for tar  ...[more]

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