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Updated: May 10, 2026
Preparation and Characterization of Individual and Multi-drug Loaded Physically Entrapped Polymeric Micelles
Published on: August 28, 2015
Nanoemulsion loaded with lycobetaine-oleic acid ionic complex: physicochemical characteristics, in vitro, in vivo
1Key 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.
