Stabilising cubosomes with Tween 80 as a step towards targeting lipid nanocarriers to the blood-brain barrier

Hanisah Azhari, Mike Strauss, Sarah Hook, Ben J Boyd, Shakila B. Rizwan

Research output: Contribution to journalArticleResearchpeer-review

Abstract

Coating nanoparticles with the surfactant Tween 80 have been previously shown to enhance drug delivery across the blood-brain barrier (BBB). The aim of this study was to investigate whether Tween 80 could be used to stabilise phytantriol-based cubosomes thereby enabling potential application in delivering macromolecular therapeutics to the brain. Cubosome particles with their large internal and external surface area by virtue of their nanostructure are ideal for delivery of macromolecules. Phase behaviour studies were conducted using a combination of optical microscopy and small-angle X-ray scattering (SAXS) and the addition of Tween 80 to mixtures of phytantriol and water resulted in a rich array of lyotropic mesophases. In particular, a large cubic phase region and a two-phase region of readily dispersed cubosomes is observed. Cubosomes with different concentrations of Tween 80 and phytantriol as the liquid crystal forming lipid were prepared using the solvent precursor method and their physical properties were investigated. A combination of dynamic light scattering, cryogenic electron tomography and SAXS shows formation of well-defined cubosomes with a narrow size distribution and the Im3m cubic structure. Collectively, the results confirm that Tween 80 can effectively stabilize phytantriol cubosomes, opening the possibility for future application in drug delivery across the BBB. Moreover, well-defined, homogenous cubosome formulations prepared using the mild solvent precursor dilution method has significant implications for large-scale production of cubosomes, which currently is a major barrier to the application of cubosomes in the clinic.

Original languageEnglish
Pages (from-to)148-155
Number of pages8
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume104
DOIs
Publication statusPublished - 1 Jul 2016

Keywords

  • Blood-brain barrier
  • Cryogenic electron tomography (cryo-ET)
  • Cubosomes
  • Phytantriol
  • Pluronic F127
  • Tween 80

Cite this

@article{b4edb427470641b38e41675b9bc00751,
title = "Stabilising cubosomes with Tween 80 as a step towards targeting lipid nanocarriers to the blood-brain barrier",
abstract = "Coating nanoparticles with the surfactant Tween 80 have been previously shown to enhance drug delivery across the blood-brain barrier (BBB). The aim of this study was to investigate whether Tween 80 could be used to stabilise phytantriol-based cubosomes thereby enabling potential application in delivering macromolecular therapeutics to the brain. Cubosome particles with their large internal and external surface area by virtue of their nanostructure are ideal for delivery of macromolecules. Phase behaviour studies were conducted using a combination of optical microscopy and small-angle X-ray scattering (SAXS) and the addition of Tween 80 to mixtures of phytantriol and water resulted in a rich array of lyotropic mesophases. In particular, a large cubic phase region and a two-phase region of readily dispersed cubosomes is observed. Cubosomes with different concentrations of Tween 80 and phytantriol as the liquid crystal forming lipid were prepared using the solvent precursor method and their physical properties were investigated. A combination of dynamic light scattering, cryogenic electron tomography and SAXS shows formation of well-defined cubosomes with a narrow size distribution and the Im3m cubic structure. Collectively, the results confirm that Tween 80 can effectively stabilize phytantriol cubosomes, opening the possibility for future application in drug delivery across the BBB. Moreover, well-defined, homogenous cubosome formulations prepared using the mild solvent precursor dilution method has significant implications for large-scale production of cubosomes, which currently is a major barrier to the application of cubosomes in the clinic.",
keywords = "Blood-brain barrier, Cryogenic electron tomography (cryo-ET), Cubosomes, Phytantriol, Pluronic F127, Tween 80",
author = "Hanisah Azhari and Mike Strauss and Sarah Hook and Boyd, {Ben J} and Rizwan, {Shakila B.}",
year = "2016",
month = "7",
day = "1",
doi = "10.1016/j.ejpb.2016.05.001",
language = "English",
volume = "104",
pages = "148--155",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",

}

Stabilising cubosomes with Tween 80 as a step towards targeting lipid nanocarriers to the blood-brain barrier. / Azhari, Hanisah; Strauss, Mike; Hook, Sarah; Boyd, Ben J; Rizwan, Shakila B.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 104, 01.07.2016, p. 148-155.

Research output: Contribution to journalArticleResearchpeer-review

TY - JOUR

T1 - Stabilising cubosomes with Tween 80 as a step towards targeting lipid nanocarriers to the blood-brain barrier

AU - Azhari, Hanisah

AU - Strauss, Mike

AU - Hook, Sarah

AU - Boyd, Ben J

AU - Rizwan, Shakila B.

PY - 2016/7/1

Y1 - 2016/7/1

N2 - Coating nanoparticles with the surfactant Tween 80 have been previously shown to enhance drug delivery across the blood-brain barrier (BBB). The aim of this study was to investigate whether Tween 80 could be used to stabilise phytantriol-based cubosomes thereby enabling potential application in delivering macromolecular therapeutics to the brain. Cubosome particles with their large internal and external surface area by virtue of their nanostructure are ideal for delivery of macromolecules. Phase behaviour studies were conducted using a combination of optical microscopy and small-angle X-ray scattering (SAXS) and the addition of Tween 80 to mixtures of phytantriol and water resulted in a rich array of lyotropic mesophases. In particular, a large cubic phase region and a two-phase region of readily dispersed cubosomes is observed. Cubosomes with different concentrations of Tween 80 and phytantriol as the liquid crystal forming lipid were prepared using the solvent precursor method and their physical properties were investigated. A combination of dynamic light scattering, cryogenic electron tomography and SAXS shows formation of well-defined cubosomes with a narrow size distribution and the Im3m cubic structure. Collectively, the results confirm that Tween 80 can effectively stabilize phytantriol cubosomes, opening the possibility for future application in drug delivery across the BBB. Moreover, well-defined, homogenous cubosome formulations prepared using the mild solvent precursor dilution method has significant implications for large-scale production of cubosomes, which currently is a major barrier to the application of cubosomes in the clinic.

AB - Coating nanoparticles with the surfactant Tween 80 have been previously shown to enhance drug delivery across the blood-brain barrier (BBB). The aim of this study was to investigate whether Tween 80 could be used to stabilise phytantriol-based cubosomes thereby enabling potential application in delivering macromolecular therapeutics to the brain. Cubosome particles with their large internal and external surface area by virtue of their nanostructure are ideal for delivery of macromolecules. Phase behaviour studies were conducted using a combination of optical microscopy and small-angle X-ray scattering (SAXS) and the addition of Tween 80 to mixtures of phytantriol and water resulted in a rich array of lyotropic mesophases. In particular, a large cubic phase region and a two-phase region of readily dispersed cubosomes is observed. Cubosomes with different concentrations of Tween 80 and phytantriol as the liquid crystal forming lipid were prepared using the solvent precursor method and their physical properties were investigated. A combination of dynamic light scattering, cryogenic electron tomography and SAXS shows formation of well-defined cubosomes with a narrow size distribution and the Im3m cubic structure. Collectively, the results confirm that Tween 80 can effectively stabilize phytantriol cubosomes, opening the possibility for future application in drug delivery across the BBB. Moreover, well-defined, homogenous cubosome formulations prepared using the mild solvent precursor dilution method has significant implications for large-scale production of cubosomes, which currently is a major barrier to the application of cubosomes in the clinic.

KW - Blood-brain barrier

KW - Cryogenic electron tomography (cryo-ET)

KW - Cubosomes

KW - Phytantriol

KW - Pluronic F127

KW - Tween 80

UR - http://www.scopus.com/inward/record.url?scp=84967104243&partnerID=8YFLogxK

U2 - 10.1016/j.ejpb.2016.05.001

DO - 10.1016/j.ejpb.2016.05.001

M3 - Article

VL - 104

SP - 148

EP - 155

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

ER -