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

  • Hans F. Fritz
  • Andrea C. Ortiz
  • Sitaram P. Velaga
  • Javier O. Morales
Original Article
  • 20 Downloads

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.

Keywords

Lipid-core micelles Low-energy method Poorly water soluble drugs Hot-melt emulsification Nanocarriers 

Notes

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Supplementary material

13346_2018_521_MOESM1_ESM.docx (44 kb)
ESM 1 (DOCX 44 kb)

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Copyright information

© Controlled Release Society 2018

Authors and Affiliations

  • Hans F. Fritz
    • 1
    • 2
  • Andrea C. Ortiz
    • 1
    • 2
  • Sitaram P. Velaga
    • 3
  • Javier O. Morales
    • 1
    • 2
    • 3
  1. 1.Department of Pharmaceutical Science and Technology, School of Chemical and Pharmaceutical SciencesUniversity of ChileSantiagoChile
  2. 2.Advanced Center for Chronic Diseases (ACCDiS)SantiagoChile
  3. 3.Pharmaceutical and Biomaterial Research Group, Department of Health SciencesLuleå University of TechnologyLuleåSweden

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