Triolein emulsion enhances temozolomide brain delivery: an experimental study in rats.

To evaluate the enhancement of temozolomide (TMZ) delivery in the rat brain using a triolein emulsion. Rats were divided into the five groups as following: group 1 (negative control), group 2 (treated with triolein emulsion and TMZ 20 mg/kg), and group 3 (TMZ 20 mg/kg treatment without triolein), group 4 (treated with triolein emulsion and TMZ 10 mg/kg), and group 5 (TMZ 10 mg/kg treatment without triolein). Triolein emulsion was infused into the right common carotid artery. One hour later, the TMZ concentration was evaluated quantitatively and qualitatively using high-performance liquid chromatography (HPLC-MS) and desorption electrospray ionization mass spectrometry (DESI-MS) imaging, respectively. The concentration ratios of the ipsilateral to contralateral hemisphere in each group were determined and the statistical analysis was conducted using an unpaired t-test. Quantitatively, the TMZ concentration ratio of the ipsilateral to the control hemisphere was 2.41 and 1.13 in groups 2 and 3, and were 2.49 and 1.14 in groups 4 and 5, respectively. Thus, the TMZ signal intensities of TMZ in group 2 and 4 were statistically high in the ipsilateral hemispheres. Qualitatively, the signal intensity of TMZ was remarkably high in the ipsilateral hemisphere in group 2 and 4. The triolein emulsion efficiently opened the blood-brain barrier and could provide a potential new strategy to enhance the therapeutic effect of TMZ. HPLC-MS and DESI-MS imaging were shown to be suitable for analyses of enhancement of brain TMZ concentrations.

Citation

Won-Bae Seung, Seung Heon Cha, Hak Jin Kim, Seon Hee Choi, Juho Lee, Dongmin Kwak, Kim Hyun Woo, Jin-Wook You, Yong-Woo Kim, Sang Kyoon Kim, Da-Sol Lee. Triolein emulsion enhances temozolomide brain delivery: an experimental study in rats. Drug delivery. 2021 Dec;28(1):2373-2382

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PMID: 34747271

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