Abstract
Liposomal formulations have important therapeutic applications in anti-cancer treatments but current formulations suffer from serious side effects, high dosage requirements and prolonged treatment. In this study, PEGylated azide-functionalized liposomes containing drug nanocrystals were investigated with the aim of increasing the drug payload and achieving functionalization for targeted delivery. Liposomes were characterized using cryogenic transmission electron microscopy (cryo-TEM), dynamic light scattering (DLS), small and ultra-small angle neutron scattering (SANS/USANS) and small and wide angle X-ray scattering (SAXS/WAXS). Cryo-TEM experiments revealed the dimensions of the nanocrystal-loaded liposomes and the change of shape from spherical to elongated after the formation of nanocrystals. Results from SANS/USANS experiments confirmed the asymmetric particle shape. SAXS/WAXS experiments confirmed that the crystalline drug only occurred in freeze-thawed samples and correlated with a new unidentified polymorphic form of ciprofloxacin. Using a small molecule dye, dibenzocyclooctyne (DBCO)-cy5, specific conjugation between DBCO groups and surface azide groups on the liposomes was confirmed; this indicates the promise of this system for tumour-targeted delivery.
| Original language | English |
|---|---|
| Article number | 110362 |
| Number of pages | 10 |
| Journal | Colloids and Surfaces B: Biointerfaces |
| Volume | 182 |
| DOIs | |
| Publication status | Published - 1 Oct 2019 |
Keywords
- Click chemistry
- Drug nanocrystals
- Liposomes
- PEGylation
- Scattering
- Targeted delivery
Cite this
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PEGylation and surface functionalization of liposomes containing drug nanocrystals for cell-targeted delivery. / Xiao, Yunxin; Liu, Qingtao; Clulow, Andrew J.; Li, Tang; Manohar, Madhura; Gilbert, Elliot P.; de Campo, Liliana; Hawley, Adrian; Boyd, B. J.
In: Colloids and Surfaces B: Biointerfaces, Vol. 182, 110362, 01.10.2019.Research output: Contribution to journal › Article › Research › peer-review
TY - JOUR
T1 - PEGylation and surface functionalization of liposomes containing drug nanocrystals for cell-targeted delivery
AU - Xiao, Yunxin
AU - Liu, Qingtao
AU - Clulow, Andrew J.
AU - Li, Tang
AU - Manohar, Madhura
AU - Gilbert, Elliot P.
AU - de Campo, Liliana
AU - Hawley, Adrian
AU - Boyd, B. J.
PY - 2019/10/1
Y1 - 2019/10/1
N2 - Liposomal formulations have important therapeutic applications in anti-cancer treatments but current formulations suffer from serious side effects, high dosage requirements and prolonged treatment. In this study, PEGylated azide-functionalized liposomes containing drug nanocrystals were investigated with the aim of increasing the drug payload and achieving functionalization for targeted delivery. Liposomes were characterized using cryogenic transmission electron microscopy (cryo-TEM), dynamic light scattering (DLS), small and ultra-small angle neutron scattering (SANS/USANS) and small and wide angle X-ray scattering (SAXS/WAXS). Cryo-TEM experiments revealed the dimensions of the nanocrystal-loaded liposomes and the change of shape from spherical to elongated after the formation of nanocrystals. Results from SANS/USANS experiments confirmed the asymmetric particle shape. SAXS/WAXS experiments confirmed that the crystalline drug only occurred in freeze-thawed samples and correlated with a new unidentified polymorphic form of ciprofloxacin. Using a small molecule dye, dibenzocyclooctyne (DBCO)-cy5, specific conjugation between DBCO groups and surface azide groups on the liposomes was confirmed; this indicates the promise of this system for tumour-targeted delivery.
AB - Liposomal formulations have important therapeutic applications in anti-cancer treatments but current formulations suffer from serious side effects, high dosage requirements and prolonged treatment. In this study, PEGylated azide-functionalized liposomes containing drug nanocrystals were investigated with the aim of increasing the drug payload and achieving functionalization for targeted delivery. Liposomes were characterized using cryogenic transmission electron microscopy (cryo-TEM), dynamic light scattering (DLS), small and ultra-small angle neutron scattering (SANS/USANS) and small and wide angle X-ray scattering (SAXS/WAXS). Cryo-TEM experiments revealed the dimensions of the nanocrystal-loaded liposomes and the change of shape from spherical to elongated after the formation of nanocrystals. Results from SANS/USANS experiments confirmed the asymmetric particle shape. SAXS/WAXS experiments confirmed that the crystalline drug only occurred in freeze-thawed samples and correlated with a new unidentified polymorphic form of ciprofloxacin. Using a small molecule dye, dibenzocyclooctyne (DBCO)-cy5, specific conjugation between DBCO groups and surface azide groups on the liposomes was confirmed; this indicates the promise of this system for tumour-targeted delivery.
KW - Click chemistry
KW - Drug nanocrystals
KW - Liposomes
KW - PEGylation
KW - Scattering
KW - Targeted delivery
UR - http://www.scopus.com/inward/record.url?scp=85069735959&partnerID=8YFLogxK
U2 - 10.1016/j.colsurfb.2019.110362
DO - 10.1016/j.colsurfb.2019.110362
M3 - Article
VL - 182
JO - Colloids and Surfaces B: Biointerfaces
JF - Colloids and Surfaces B: Biointerfaces
SN - 0927-7765
M1 - 110362
ER -