<abstract xml:lang="en" xmlns="http://www.w3.org/1999/xhtml"><p>7-Ethyl-10-hydroxy-camptothecin (SN-38), a metabolite of irinotecan x HCl, is poorly soluble in aqueous solutions and practically insoluble in most physiologically compatible and pharmaceutically acceptable solvents. Formulation of SN-38 in concentrated pharmaceutical delivery systems for parenteral administration is thus very difficult. Due to their biocompatibility and low toxicity, liposomes were considered for the delivery of SN-38. In this study, pegylated liposomes with distearoylphosphatidylcholine, distearoylphosphatidylethanolamine containing SN-38 were prepared and their characteristics, such as particle size, encapsulation efficiency, <italic>in vitro</italic> drug release and biodistribution, were investigated. The particle size of liposomes was in the range of 150--200 nm. The encapsulation efficiency and <italic>in vitro</italic> release rate of pegylated liposomes was higher than those of non-pegylated liposomes. As expected, the distribution of pegylated liposomes in body organs such as liver, kidney, spleen and lung was considerably lower than that of non-pegylated liposomes. Also, their blood concentration was at least 50 % higher than that of non-pegylated liposomes.</p></abstract>

7-Ethyl-10-hydroxy-camptothecin (SN-38), a metabolite of irinotecan x HCl, is poorly soluble in aqueous solutions and practically insoluble in most physiologically compatible and pharmaceutically acceptable solvents. Formulation of SN-38 in concentrated pharmaceutical delivery systems for parenteral administration is thus very difficult. Due to their biocompatibility and low toxicity, liposomes were considered for the delivery of SN-38. In this study, pegylated liposomes with distearoylphosphatidylcholine, distearoylphosphatidylethanolamine containing SN-38 were prepared and their characteristics, such as particle size, encapsulation efficiency, in vitro drug release and biodistribution, were investigated. The particle size of liposomes was in the range of 150--200 nm. The encapsulation efficiency and in vitro release rate of pegylated liposomes was higher than those of non-pegylated liposomes. As expected, the distribution of pegylated liposomes in body organs such as liver, kidney, spleen and lung was considerably lower than that of non-pegylated liposomes. Also, their blood concentration was at least 50 % higher than that of non-pegylated liposomes.

Preparation of pegylated nano-liposomal formulation containing SN-38: <italic>In vitro</italic> characterization and <italic>in vivo</italic> biodistribution in mice

Novel Drug Delivery Systems Laboratory, Faculty of Pharmacy, Tehran University of Medical Sciences, Tehran, PO Box 14155-6451 Islamic Republic of Iran

Medical Nanotechnology Research Centre, Tehran University of Medical Sciences, Tehran, PO Box 14155-6451 Islamic Republic of Iran

Acta Pharmaceutica

Preparation of pegylated nano-liposomal formulation containing SN-38:  characterization and  biodistribution in mice

7-Ethyl-10-hydroxy-camptothecin (SN-38), a metabolite of irinotecan x HCl, is poorly soluble in aqueous solutions and practically insoluble in most...

Preparation of pegylated nano-liposomal formulation containing SN-38: In vitro characterization and in vivo biodistribution in mice

Publicado en línea: 29 jun 2009

Páginas: 133 - 144

DOI: https://doi.org/10.2478/v10007-009-0020-0

Palabras clave
nanočestice, SN-38, pegilirani liposomi, PEG, biodistribucija, isporuka lijeka

This content is open access.