Therapeutic surfactant-stripped frozen micelles

Yumiao Zhang, Wentao Song, Jumin Geng, Upendra Chitgupi, Hande Unsal, Jasmin Federizon, Javid Rzayev, Dinesh K. Sukumaran, Paschalis Alexandridis and Jonathan F. Lovell ()
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Yumiao Zhang: University at Buffalo, State University of New York
Wentao Song: University at Buffalo, State University of New York
Jumin Geng: University at Buffalo, State University of New York
Upendra Chitgupi: University at Buffalo, State University of New York
Hande Unsal: State University of New York
Jasmin Federizon: State University of New York
Javid Rzayev: State University of New York
Dinesh K. Sukumaran: State University of New York
Paschalis Alexandridis: University at Buffalo, State University of New York
Jonathan F. Lovell: University at Buffalo, State University of New York

Nature Communications, 2016, vol. 7, issue 1, 1-9

Abstract: Abstract Injectable hydrophobic drugs are typically dissolved in surfactants and non-aqueous solvents which can induce negative side-effects. Alternatives like ‘top-down’ fine milling of excipient-free injectable drug suspensions are not yet clinically viable and ‘bottom-up’ self-assembled delivery systems usually substitute one solubilizing excipient for another, bringing new issues to consider. Here, we show that Pluronic (Poloxamer) block copolymers are amenable to low-temperature processing to strip away all free and loosely bound surfactant, leaving behind concentrated, kinetically frozen drug micelles containing minimal solubilizing excipient. This approach was validated for phylloquinone, cyclosporine, testosterone undecanoate, cabazitaxel and seven other bioactive molecules, achieving sizes between 45 and 160 nm and drug to solubilizer molar ratios 2–3 orders of magnitude higher than current formulations. Hypertonic saline or co-loaded cargo was found to prevent aggregation in some cases. Use of surfactant-stripped micelles avoided potential risks associated with other injectable formulations. Mechanistic insights are elucidated and therapeutic dose responses are demonstrated.

Date: 2016
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DOI: 10.1038/ncomms11649

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