In-vitro cytotoxicity, in-vivo biodistribution and anti-tumour effect of PEGylated liposomal topotecan

In attempt to increase the accumulation of topotecan in tumours and improve its anti‐cancer activity, PEGylated liposome (H‐PEG) containing topotecan was prepared. The in‐vitro cytotoxicity, in‐vivo biodistribution pattern and anti‐tumour effect of H‐PEG were studied systemically. Compared with free...

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Veröffentlicht in:	Journal of pharmacy and pharmacology 2005-10, Vol.57 (10), p.1279-1287
Hauptverfasser:	Hao, Yan-Li, Deng, Ying-Jie, Chen, Yan, Hao, Ai-Jun, Zhang, Yong, Wang, Ke-Zhan
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Antineoplastic Agents - pharmacokinetics Antineoplastic Agents - pharmacology Antineoplastic Agents - therapeutic use Area Under Curve Biological Availability Bone Marrow - chemistry Bone Marrow - drug effects Bone Marrow - metabolism Cell Line, Tumor Cell Survival - drug effects Drug Compounding - methods Drug Stability Female Humans Inhibitory Concentration 50 Liposomes - chemistry Liposomes - pharmacokinetics Liver - drug effects Liver - metabolism Lung - chemistry Lung - drug effects Lung - metabolism Male Mice Mice, Inbred ICR Neoplasms, Experimental - drug therapy Neoplasms, Experimental - metabolism Polyethylene Glycols - chemistry Polyethylene Glycols - pharmacokinetics Spleen - drug effects Spleen - metabolism Tissue Distribution - drug effects Topotecan - chemistry Topotecan - pharmacokinetics Topotecan - pharmacology Xenograft Model Antitumor Assays - methods
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Zusammenfassung:	In attempt to increase the accumulation of topotecan in tumours and improve its anti‐cancer activity, PEGylated liposome (H‐PEG) containing topotecan was prepared. The in‐vitro cytotoxicity, in‐vivo biodistribution pattern and anti‐tumour effect of H‐PEG were studied systemically. Compared with free topotecan or conventional liposome (H‐Lip), H‐PEG improved the cytotoxic effect of topotecan against human ovarian carcinoma A2780 and human colon carcinoma HCT‐8 cells. The IC50 value (concentration leading to 50% cell‐killing) of H‐PEG decreased 5 fold (P
ISSN:	0022-3573 2042-7158
DOI:	10.1211/jpp.57.10.0006