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

Authors Zhao H, Lu H, Gong T, Zhang Z

Received 11 February 2013

Accepted for publication 18 March 2013

Published 21 May 2013 Volume 2013:8(1) Pages 1959—1973


Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 2

Hui Zhao, Hua Lu, Tao Gong, Zhirong Zhang

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

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: lycobetaine, oleic acid, polyethylene glycol, nanoemulsion, in vivo studies, antitumor activity

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