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Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
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Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins

Published on: August 31, 2019

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Effect of solubilizing agents on mupirocin loading into and release from PEGylated nanoliposomes

Ahuva Cern1, Einat Nativ-Roth2, Amiram Goldblum3

  • 1Laboratory of Membrane and Liposome Research, Department of Biochemistry, IMRIC, The Hebrew University - Hadassah Medical School, Jerusalem, Israel; Molecular Modeling and Drug Design Laboratory, The Institute for Drug Research, The Hebrew University of Jerusalem, Jerusalem, Israel.

Journal of Pharmaceutical Sciences
|June 6, 2014
PubMed

Insights

Mupirocin antibiotic loading into nanoliposomes was enhanced using solubilizing agents like propylene glycol and hydroxypropyl-β-cyclodextrin (HPCD). This formulation may enable parenteral delivery by protecting mupirocin from degradation.

Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems
  • Nanotechnology

Background:

  • Mupirocin is an antibiotic limited to topical use due to rapid in vivo hydrolysis.
  • Nanoliposomal formulation offers potential for parenteral administration and targeted delivery.
  • Solubilizing agents can improve drug loading in liposomes.

Purpose of the Study:

  • To investigate the effect of solubilizing agents on remote mupirocin loading into PEGylated nanoliposomes.
  • To evaluate the impact of these agents on drug stability and release characteristics.

Main Methods:

  • Quantitative structure-property relationship (QSPR) modeling identified mupirocin as suitable for liposomal loading.
  • Nanoliposomes were formulated with PEGylation.
  • Solubilizing agents (propylene glycol, polyethylene glycol 400, hydroxypropyl-β-cyclodextrin) were added to the drug loading solution.
  • Drug loading efficiency and in vitro release were assessed.

Main Results:

  • Propylene glycol increased mupirocin loading into nanoliposomes.
  • Polyethylene glycol 400 had no significant effect on loading.
  • Hydroxypropyl-β-cyclodextrin (HPCD) demonstrated a concentration-dependent effect, enhancing loading at optimal concentrations but inhibiting it at higher levels.
  • Incorporating HPCD during liposome formation increased drug loading and significantly reduced serum-mediated drug release.

Conclusions:

  • Solubilizing agents, particularly propylene glycol and optimized HPCD concentrations, can enhance mupirocin remote loading into nanoliposomes.
  • HPCD inclusion improves drug loading and stability, suggesting potential for developing parenteral mupirocin formulations.
  • PEGylated nanoliposomes with HPCD show promise for protecting mupirocin from degradation and controlling its release.
Keywords:
computer-aided drug designexcipientsformulationliposomesnanoparticlessolubility

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