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Preparation of a novel lipid-core micelle using a low-energy emulsification method

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Abstract

High-energy methods for the manufacturing of nanomedicines are widely used; however, interest in low-energy methods is increasing due to their simplicity, better control over the process, and energy-saving characteristics during upscaling. Here, we developed a novel lipid-core micelle (LCM) as a nanocarrier to encapsulate a poorly water-soluble drug, nifedipine (NFD), by hot-melt emulsification, a low-energy method. LCMs are self-assembling colloidal particles composed of a hydrophobic core and a hydrophilic shell. Hybrid materials, such as Gelucire 44/14, are thus excellent candidates for their preparation. We characterized the obtained nanocarriers for their colloidal properties, drug loading and encapsulation efficiency, liquid state, stability, and drug release. The low-energy method hot-melt emulsification was successfully adapted for the manufacturing of small and narrowly dispersed LCMs. The obtained LCMs had a small average size of ~ 11 nm and a narrow polydispersity index (PDI) of 0.228. These nanocarriers were able to increase the amount of NFD dispersible in water more than 700-fold. Due to their sustained drug release profile and the PEGylation of Gelucire 44/14, these nanocarriers represent an excellent starting point for the development of drug delivery systems designed for long circulation times and passive targeting.

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Funding

The authors acknowledge the funding support from FONDECYT 1181689, FONDAP 15130011, and STINT IB2015-6087.

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Authors and Affiliations

  1. Department of Pharmaceutical Science and Technology, School of Chemical and Pharmaceutical Sciences, University of Chile, Santos Dumont 964, 4to piso, Of. 09, Independencia, 8380494, Santiago, Chile

    Hans F. Fritz, Andrea C. Ortiz & Javier O. Morales

  2. Advanced Center for Chronic Diseases (ACCDiS), 8380494, Santiago, Chile

    Hans F. Fritz, Andrea C. Ortiz & Javier O. Morales

  3. Pharmaceutical and Biomaterial Research Group, Department of Health Sciences, Luleå University of Technology, 97187, Luleå, Sweden

    Sitaram P. Velaga & Javier O. Morales

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  1. Hans F. Fritz
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  2. Andrea C. Ortiz
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  4. Javier O. Morales
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Correspondence to Javier O. Morales.

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Fritz, H.F., Ortiz, A.C., Velaga, S.P. et al. Preparation of a novel lipid-core micelle using a low-energy emulsification method. Drug Deliv. and Transl. Res. 8, 1807–1814 (2018). https://doi.org/10.1007/s13346-018-0521-9

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