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Int J Pharm. 2013 Sep 15;454(1):472-7. doi: 10.1016/j.ijpharm.2013.06.032. Epub 2013 Jun 24.

Development of intravenous lipid emulsion of vinorelbine based on drug-phospholipid complex technique.

Author information

1
State Key Laboratory of Drug Delivery Technology and Pharmacokinetics, Tianjin Institute of Pharmaceutical Research, No. 308, Anshan Road, Tianjin 300193, People's Republic of China.

Abstract

In order to reduce the severe venous toxicity, we developed an intravenous lipid emulsion of vinorelbine and investigated its preclinical stability, toxicity and antitumor efficacy. Vinorelbine-phospholipid complex was prepared to enhance the lipophilicity of vinorelbine thus facilitating the encapsulation into lipid emulsion. After complexation more than 70% of vinorelbine was encapsulated into the oil phase. Meanwhile, the lipid emulsion showed good stability without drug leakage. Local irritation after injection of the lipid emulsion was investigated in rabbits and compared with Navelbine(®) (the commercial product). The antitumor therapeutic efficacies were evaluated in tumor-bearing mouse models inoculated with A549 human lung cancer cells and BCAP-37 human breast cancer cells and compared as well. Results showed that the lipid emulsion significantly reduced the injection irritation compared with that of Navelbine(®), while maintained the antitumor activity in A549 and BCAP-37 cells xenograft tumor mouse models. Taken together, lipid emulsion loaded with vinorelbine-phospholipid complex is a promising vinorelbine intravenous injection with reduced venous irritation.

KEYWORDS:

Antitumor activity; Drug–phospholipid complex; Injection irritation; Vinorelbine

PMID:
23806812
DOI:
10.1016/j.ijpharm.2013.06.032
[Indexed for MEDLINE]

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