title: Efficacy of temoporfin-loaded invasomes in the photodynamic therapy in human epidermoid and colorectal tumour cell lines.
abstract: In the case of cutaneous malignant or non-malignant diseases, topical photodynamic therapy (PDT) with a temoporfin (mTHPC)-containing formulation would be advantageous. Unfortunately, mTHPC is a highly hydrophobic drug with low percutaneous absorption and novel mTHPC-loaded invasomes for enhanced skin delivery were developed. The purpose of this study was to investigate photodynamic efficacy of mTHPC-loaded invasomes in vitro in two cell lines, i.e. the human colorectal tumour cell line HT29 and the epidermoid tumour cell line A431. Invasomes are vesicles containing besides phospholipids a mixture of terpenes or only one terpene and ethanol. Dark toxicity, phototoxicity and intracellular localization of mTHPC were studied. Laser scanning microscopy indicated perinuclear localization of mTHPC. Results revealed that mTHPC-invasomes and mTHPC-ethanolic solution used at a 2μM mTHPC-concentration and photoirradiation at 20J/cm(2) were able to reduce survival of HT29 cells and especially of A431 cells, being more sensitive to PDT. In contrast to HT29 cells, where there was not a significant difference between cytotoxicity of mTHPC-ethanolic solution and mTHPC-invasomes, in A431 cells mTHPC-invasomes were more cytotoxic. Survival of about 16% of A431 cells treated with mTHPC-invasomes is very promising, since it demonstrates invasomes' potential to be used in topical PDT of cutaneous malignant diseases.
authors.affiliation: Department of Pharmaceutical Technology, Friedrich Schiller University Jena, Lessingstrasse 8, 07743 Jena, Germany. ninadragicevic@hotmail.com
authors.forename: Nina
authors.initials: N
authors.lastname: Dragicevic-Curic
authors.forename: Susanna
authors.initials: S
authors.lastname: Gräfe
authors.forename: Burkhard
authors.initials: B
authors.lastname: Gitter
authors.forename: Alfred
authors.initials: A
authors.lastname: Fahr
mesh_terms: D045744:Cell Line, Tumor; D015179:Colorectal Neoplasms / Q000188:drug therapy*; D000431:Ethanol / Q000737:chemistry; D006801:Humans; D008027:Light; D008081:Liposomes / Q000737:chemistry*; D008652:Mesoporphyrins / Q000008:administration & dosage* / Q000633:toxicity; D018613:Microscopy, Confocal; D010778:Photochemotherapy; D017319:Photosensitizing Agents / Q000008:administration & dosage* / Q000633:toxicity; D012878:Skin Neoplasms / Q000188:drug therapy*
chemical_list: D008081:Liposomes; D008652:Mesoporphyrins; D017319:Photosensitizing Agents; D000431:Ethanol; C072269:temoporfin