Exposure of liposomes containing nanocrystallised ciprofloxacin to digestive media induces solid-state transformation and altered in vitro drug release

Research output: Contribution to journal › Journal article › Research › peer-review

Standard

Exposure of liposomes containing nanocrystallised ciprofloxacin to digestive media induces solid-state transformation and altered in vitro drug release. / Li, Tang; Hawley, Adrian; Rades, Thomas; Boyd, Ben J.

In: Journal of Controlled Release, Vol. 323, 2020, p. 350-360.

Research output: Contribution to journal › Journal article › Research › peer-review

Harvard

Li, T, Hawley, A, Rades, T & Boyd, BJ 2020, 'Exposure of liposomes containing nanocrystallised ciprofloxacin to digestive media induces solid-state transformation and altered in vitro drug release', Journal of Controlled Release, vol. 323, pp. 350-360. https://doi.org/10.1016/j.jconrel.2020.04.034

APA

Li, T., Hawley, A., Rades, T., & Boyd, B. J. (2020). Exposure of liposomes containing nanocrystallised ciprofloxacin to digestive media induces solid-state transformation and altered in vitro drug release. Journal of Controlled Release, 323, 350-360. https://doi.org/10.1016/j.jconrel.2020.04.034

Vancouver

Li T, Hawley A, Rades T, Boyd BJ. Exposure of liposomes containing nanocrystallised ciprofloxacin to digestive media induces solid-state transformation and altered in vitro drug release. Journal of Controlled Release. 2020;323:350-360. https://doi.org/10.1016/j.jconrel.2020.04.034

Author

Li, Tang ; Hawley, Adrian ; Rades, Thomas ; Boyd, Ben J. / Exposure of liposomes containing nanocrystallised ciprofloxacin to digestive media induces solid-state transformation and altered in vitro drug release. In: Journal of Controlled Release. 2020 ; Vol. 323. pp. 350-360.

Bibtex

@article{e4f2258f760a41b7a1349db5cddda708,
title = "Exposure of liposomes containing nanocrystallised ciprofloxacin to digestive media induces solid-state transformation and altered in vitro drug release",
abstract = "A recently reported approach to nanocrystallise encapsulated ciprofloxacin within liposomes has generated increased interest in the solid-state properties of drug nanocrystals within liposomal confinement. To explore the potential application of nanocrystallised drug liposomes in oral delivery, a liposomal ciprofloxacin formulation was used as a model system. An in vitro digestion model coupled to small angle X-ray scattering was used to analyse the solid-state properties of the drug nanocrystals during digestion of the liposomal ciprofloxacin nanocrystal formulations. Results showed a complete polymorphic transformation of the ciprofloxacin hydrate nanocrystals to a new salt form at a threshold sodium taurodeoxycholate to ciprofloxacin molar ratio of 0.6. The in vitro drug release from the nanocrystallised drug containing liposomes showed controlled drug release behaviour under non-digestive conditions, while a 3.5-fold increase in the drug release was seen when they were exposed to the simulated digestive environment. In conclusion, the solid state of the drug inside the liposomes is important in dictating the drug release behaviour from the liposomes. The identification of the solid state transformation during digestion in real time and the bile salt-induced polymorphic transformation of ciprofloxacin from nanocrystallised ciprofloxacin liposome are important to understand how the drug is released in vivo, as well as for future formulation design.",
keywords = "Small angle X-ray scattering, Liposomes, Ciprofloxacin, Nanocrystals, Oral drug delivery, Bile salt, in vitro drug release, X-RAY-SCATTERING, WATER-SOLUBLE DRUG, FLUOROQUINOLONE ANTIMICROBIALS, ORAL ABSORPTION, BILE-SALTS, DOXORUBICIN, DELIVERY, PH, STABILITY, FORMULATIONS",
author = "Tang Li and Adrian Hawley and Thomas Rades and Boyd, {Ben J.}",
year = "2020",
doi = "10.1016/j.jconrel.2020.04.034",
language = "English",
volume = "323",
pages = "350--360",
journal = "Journal of Controlled Release",
issn = "0168-3659",
publisher = "Elsevier",

}

RIS

TY - JOUR

T1 - Exposure of liposomes containing nanocrystallised ciprofloxacin to digestive media induces solid-state transformation and altered in vitro drug release

AU - Li, Tang

AU - Hawley, Adrian

AU - Rades, Thomas

AU - Boyd, Ben J.

PY - 2020

Y1 - 2020

N2 - A recently reported approach to nanocrystallise encapsulated ciprofloxacin within liposomes has generated increased interest in the solid-state properties of drug nanocrystals within liposomal confinement. To explore the potential application of nanocrystallised drug liposomes in oral delivery, a liposomal ciprofloxacin formulation was used as a model system. An in vitro digestion model coupled to small angle X-ray scattering was used to analyse the solid-state properties of the drug nanocrystals during digestion of the liposomal ciprofloxacin nanocrystal formulations. Results showed a complete polymorphic transformation of the ciprofloxacin hydrate nanocrystals to a new salt form at a threshold sodium taurodeoxycholate to ciprofloxacin molar ratio of 0.6. The in vitro drug release from the nanocrystallised drug containing liposomes showed controlled drug release behaviour under non-digestive conditions, while a 3.5-fold increase in the drug release was seen when they were exposed to the simulated digestive environment. In conclusion, the solid state of the drug inside the liposomes is important in dictating the drug release behaviour from the liposomes. The identification of the solid state transformation during digestion in real time and the bile salt-induced polymorphic transformation of ciprofloxacin from nanocrystallised ciprofloxacin liposome are important to understand how the drug is released in vivo, as well as for future formulation design.

AB - A recently reported approach to nanocrystallise encapsulated ciprofloxacin within liposomes has generated increased interest in the solid-state properties of drug nanocrystals within liposomal confinement. To explore the potential application of nanocrystallised drug liposomes in oral delivery, a liposomal ciprofloxacin formulation was used as a model system. An in vitro digestion model coupled to small angle X-ray scattering was used to analyse the solid-state properties of the drug nanocrystals during digestion of the liposomal ciprofloxacin nanocrystal formulations. Results showed a complete polymorphic transformation of the ciprofloxacin hydrate nanocrystals to a new salt form at a threshold sodium taurodeoxycholate to ciprofloxacin molar ratio of 0.6. The in vitro drug release from the nanocrystallised drug containing liposomes showed controlled drug release behaviour under non-digestive conditions, while a 3.5-fold increase in the drug release was seen when they were exposed to the simulated digestive environment. In conclusion, the solid state of the drug inside the liposomes is important in dictating the drug release behaviour from the liposomes. The identification of the solid state transformation during digestion in real time and the bile salt-induced polymorphic transformation of ciprofloxacin from nanocrystallised ciprofloxacin liposome are important to understand how the drug is released in vivo, as well as for future formulation design.

KW - Small angle X-ray scattering

KW - Liposomes

KW - Ciprofloxacin

KW - Nanocrystals

KW - Oral drug delivery

KW - Bile salt

KW - in vitro drug release

KW - X-RAY-SCATTERING

KW - WATER-SOLUBLE DRUG

KW - FLUOROQUINOLONE ANTIMICROBIALS

KW - ORAL ABSORPTION

KW - BILE-SALTS

KW - DOXORUBICIN

KW - DELIVERY

KW - PH

KW - STABILITY

KW - FORMULATIONS

U2 - 10.1016/j.jconrel.2020.04.034

DO - 10.1016/j.jconrel.2020.04.034

M3 - Journal article

C2 - 32335156

VL - 323

SP - 350

EP - 360

JO - Journal of Controlled Release

JF - Journal of Controlled Release

SN - 0168-3659

ER -

ID: 247441336