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Int J Nanomedicine. 2013;8:1959-73. doi: 10.2147/IJN.S43892. Epub 2013 May 21.

Nanoemulsion loaded with lycobetaine-oleic acid ionic complex: physicochemical characteristics, in vitro, in vivo evaluation, and antitumor activity.

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  • 1Key Laboratory of Drug Targeting, Ministry of Education, Sichuan University, Chengdu, People's Republic of China.

Abstract

BACKGROUND:

Intravenous injection of lycobetaine was found to show significant cytotoxic activity against (inter alia) Lewis lung carcinoma, but its therapeutic use is largely limited due to an extremely short half-life in blood. This study aimed at developing a novel lipid nanocarrier-based formulation for lycobetaine delivery. The formulation is feasible for scale-up production, exhibiting good parenteral acceptability and improved circulation characteristics.

METHODS:

To enhance its lipophilicity, oleic acid was selected to form ionic complexes with lycobetaine (LBT). The nanoemulsion loaded with LBT-oleic acid complex (LBT-OA-nanoemulsion) and PEGylated LBT-OA-nanoemulsion (NE) (LBT-OA-PEG-NE) were prepared by a simple high-pressure homogenization method.

RESULTS:

A high-encapsulation efficiency of around 97.32% ± 2.09% was obtained for LBT-OA-PEG-NE under optimized conditions. Furthermore, the in vivo pharmacokinetics and biodistribution of LBT-OA-NE, LBT-OA-PEG-NE, and free LBT were studied in rats. Free LBT and LBT-OA-PEG-NE displayed AUC0-10h (area under the concentration-time curve from 0 to 10 hours) of 112.99 mg/L*minute and 3452.09 mg/L*minute via intravenous administration (P < 0.005), respectively. Moreover, LBT-OA-PEG-NE showed significantly lower LBT concentration in the heart, liver, and kidney, while achieving higher concentration of LBT in the lung when compared to free LBT at the same time (P < 0.005). The LBT-OA-PEG-NE exhibited higher growth inhibitory effect and longer survival time than free LBT in both heterotopic and lung metastatic tumor models.

CONCLUSION:

These results demonstrated that LBT-OA-PEG-NE is an attractive parenteral formulation for cancer therapy.

KEYWORDS:

antitumor activity; in vivo studies; lycobetaine; nanoemulsion; oleic acid; polyethylene glycol

PMID:
23723698
[PubMed - indexed for MEDLINE]
PMCID:
PMC3666662
Free PMC Article
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