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Emulsion-templated synthesis and in vitro characterizations of niosomes for improved therapeutic potential of hydrophobic anti-cancer drug: tamoxifen

  • Hamid Saeed Shah
  • Fazala Khalid
  • Sajid Bashir
  • Muhammed Hasham Bin Asad
  • Kashif-Ur-Rehman Khan
  • Faisal UsmanEmail author
  • Ibrahim JavedEmail author
Research Paper
  • 49 Downloads

Abstract

Hydrophobic nature of anti-cancer drugs not only imparts different pharmacokinetic barriers in drug delivery, but also associates with off-target toxicity and low-dose exposure of drug at the tumor site which is subsequently responsible for the development of multi-drug resistance. This study describes a water-in-oil emulsion templated reverse-phase evaporation strategy, using Span 120 as non-ionic surfactant, for the synthesis of tamoxifen-loaded niosomes. The dicetyl phosphate and Span 120 were used to engineer niosomes for sustained drug release over 12 h and improved surface morphology. The spherical niosomes were 260–300 nm in size with − 34.6 mV zeta potential. The scanning electron microscopy revealed a rough texture on the surface of niosomes. Niosomes released the drug in first-order and sustained release pattern up to 12 h. Cholesterol was embedded in the outer hydrophobic surface of niosomes, via inclusion in oil phase, to enhance the interaction with lipid bilayer of the cells. Niosomes were able to improve the cellular uptake of tamoxifen and introduced apoptosis (29%) as major mechanism of cell death as compared to necrosis (17%). DSC and XRD studies revealed the crystalline nature of the drug inside niosomes while FTIR displayed chemical stability of the drug after entrapment. After encapsulation inside niosomes, the anti-cancer activity of tamoxifen was improved up to five times with IC50 reduced from 1 μM to 0.2 μM against MCF-7 cells. Cytotoxicity and sulforhodamine B assay revealed the apoptotic cell death. The unloaded niosomes alone showed no toxicity to the cells and presented a biocompatible nanoscale delivery platform for hydrophobic anti-cancer drugs.

Graphical abstract

Keywords

Niosome Tamoxifen Controlled release Breast cancer Emulsion Span 120 Cholesterol Nanomedicine 

Notes

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

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Copyright information

© Springer Nature B.V. 2019

Authors and Affiliations

  1. 1.Institute of Pharmaceutical SciencesUniversity of Veterinary and Animal SciencesLahorePakistan
  2. 2.College of PharmacyUniversity of SargodhaSargodhaPakistan
  3. 3.Department of Pharmaceutical SciencesCOMSATS Institute of Information TechnologyAbbottabadPakistan
  4. 4.Laboratory INSERM UMR 1097Aix-Marseille UniversityMarseilleFrance
  5. 5.Department of Pharmaceutical Chemistry, Faculty of Pharmaceutical SciencesPrince of Songkla UniversityHat YaiThailand
  6. 6.Department of Pharmaceutics, Faculty of PharmacyBahauddin Zakariya UniversityMultanPakistan
  7. 7.Drug Delivery System Excellence Center, Department of Pharmaceutical Technology, Faculty of Pharmaceutical SciencesPrince of Songkla UniversityHat YaiThailand
  8. 8.Drug Delivery, Disposition and Dynamics, Monash Institute of Pharmaceutical SciencesMonash UniversityParkvilleAustralia

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