Effect of phospholipid composition on characterization of liposomes containing 9-nitrocamptothecin

Autor:	Xiao-Zhu Chu, Qineng Ping, Ming-Mei Song, Jun Chen, Jianxin Guo
Rok vydání:	2006
Předmět:	Male Drug Compounding Phospholipid Pharmaceutical Science Antineoplastic Agents Rats Sprague-Dawley chemistry.chemical_compound Pharmacokinetics Nitrocamptothecin Phosphatidylcholine Drug Discovery Animals Solubility Particle Size Pharmacology Liposome Chromatography Chemistry Cholesterol Organic Chemistry Rats Membrane Injections Intravenous Liposomes Phosphatidylcholines Feasibility Studies Camptothecin Hydrogenation Soybeans
Zdroj:	Drug development and industrial pharmacy. 32(6)
ISSN:	0363-9045
Popis:	9-Nitrocamptothecin (9-NC), a newly developed camptothecin derivative, had poor solubility in any pharmaceutically acceptable solvents. One way of improving the solubility is to formulate the drug into liposomes. However, 9-NC has low affinity to lipid membranes resulting in a very low drug-to-liposome entrapment. We developed a novel liposome-based 9-NC formulation which was composed of soybean phosphatidylcholine (SPC), hydrogenated soybean phosphatidylcholine (HSPC), and cholesterol. Compared with conventional liposomes composed of only SPC and cholesterol, 9-NC/lipid molar ratio increased from 1:72 to 1:18 while incorporation efficiency was still maintained about 80%. In addition, after 9-NC was encapsulated into novel liposomes, pharmacokinetic results revealed an increase in area under the plasma concentration-time curve (AUC) and a decrease in distribution volume of 9-NC following intravenous administration to rats. Increased stability in plasma may account for the improved pharmacokinetic behavior of the novel liposomes. Effect of HSPC/SPC molar ratio on characterization of the novel liposomes was also investigated. Except for drug/lipid molar ratio and encapsulation efficiency, HSPC/SPC molar ratio had only a little effect on other properties of novel liposomes. In conclusion, the study suggests that the novel liposomes can act as promising carriers for hydrophobic substances such as 9-NC.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::99aa20ff90b06336c9b10250c6cc1da6 https://pubmed.ncbi.nlm.nih.gov/16885127 Zobrazit plný text záznamu Plný text ve formátu PDF Plný text ve formátu HTML
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