Liposomes as vehicles for water insoluble platinum-based potential drug: 2-(4-(Tetrahydro-2H-pyran-2-yloxy)-undecyl)-propane-1,3-diamminedichloroplatinum(II)

Formulation of liposome delivery system loaded with water insoluble 2-(4-(tetrahydro-2H-pyran-2-yloxy)-undecyl)-propane-1,3-diamminedichloroplatinum(II), LipoTHP–C11 was carried out. The particle size distributions were determined by dynamic light scattering and asymmetrical flow field-flow fraction...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2012-08, Vol.54, p.567-572
Main Authors: Kaluđerović, Goran N., Dietrich, Andrea, Kommera, Harish, Kuntsche, Judith, Mäder, Karsten, Mueller, Thomas, Paschke, Reinhard
Format: Article
Language:English
Subjects:
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - chemistry
Antineoplastic Agents - pharmacology
Antitumoral activity
Biological and medical sciences
Cell Line, Tumor
Cisplatin
Humans
Inhibitory Concentration 50
Liposomes
Medical sciences
Miscellaneous
Organoplatinum Compounds - administration & dosage
Organoplatinum Compounds - chemistry
Organoplatinum Compounds - pharmacology
Pharmacology. Drug treatments
Platinum(II) complexes
Selectivity
Solubility
Water - chemistry
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Summary:Formulation of liposome delivery system loaded with water insoluble 2-(4-(tetrahydro-2H-pyran-2-yloxy)-undecyl)-propane-1,3-diamminedichloroplatinum(II), LipoTHP–C11 was carried out. The particle size distributions were determined by dynamic light scattering and asymmetrical flow field-flow fractionation indicating size of around 120 nm. Stability study showed that LipoTHP–C11 was stable at 4 °C for more than two months. To test suitability of chosen formulation, LipoTHP–C11 was investigated against several tumor cell lines: H12.1, 1411HP, 518A2, A549, HT-29, MCF-7 and SW1736. Furthermore, toxicity against normal fibroblasts was examined. LipoTHP–C11 may be used as an attractive candidate for further assessment in vivo as antitumor agent. Liposomes containing THP–C11 has been formulated and tested on seven different tumor cell lines as well as on normal fibroblasts. [Display omitted] ► Liposomal formulation of water insoluble platinum(II) based drug, LipoTHP–C11. ► LipoTHP–C11 effective than cisplatin on cisplatin resistant TGCT 1411HP cells. ► LipoTHP–C11 effective than cisplatin on anaplastic thyroid carcinoma SW1736 cells. ► LipoTHP–C11 attractive candidate for further assessment in vivo as antitumor agent
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2012.06.004