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Self-assembling properties of ionisable amphiphilic drugs in aqueous solution

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Self-assembling properties of ionisable amphiphilic drugs in aqueous solution. / Efthymiou, Christina; Bergström, L. Magnus; Pedersen, Jannik Nedergaard; Pedersen, Jan Skov; Hansson, Per.

In: Journal of Colloid and Interface Science, Vol. 600, 10.2021, p. 701-710.

Research output: Contribution to journal/Conference contribution in journal/Contribution to newspaperJournal articleResearchpeer-review

Harvard

Efthymiou, C, Bergström, LM, Pedersen, JN, Pedersen, JS & Hansson, P 2021, 'Self-assembling properties of ionisable amphiphilic drugs in aqueous solution', Journal of Colloid and Interface Science, vol. 600, pp. 701-710. https://doi.org/10.1016/j.jcis.2021.05.049

APA

Efthymiou, C., Bergström, L. M., Pedersen, J. N., Pedersen, J. S., & Hansson, P. (2021). Self-assembling properties of ionisable amphiphilic drugs in aqueous solution. Journal of Colloid and Interface Science, 600, 701-710. https://doi.org/10.1016/j.jcis.2021.05.049

CBE

Efthymiou C, Bergström LM, Pedersen JN, Pedersen JS, Hansson P. 2021. Self-assembling properties of ionisable amphiphilic drugs in aqueous solution. Journal of Colloid and Interface Science. 600:701-710. https://doi.org/10.1016/j.jcis.2021.05.049

MLA

Efthymiou, Christina et al. "Self-assembling properties of ionisable amphiphilic drugs in aqueous solution". Journal of Colloid and Interface Science. 2021, 600. 701-710. https://doi.org/10.1016/j.jcis.2021.05.049

Vancouver

Efthymiou C, Bergström LM, Pedersen JN, Pedersen JS, Hansson P. Self-assembling properties of ionisable amphiphilic drugs in aqueous solution. Journal of Colloid and Interface Science. 2021 Oct;600:701-710. https://doi.org/10.1016/j.jcis.2021.05.049

Author

Efthymiou, Christina ; Bergström, L. Magnus ; Pedersen, Jannik Nedergaard ; Pedersen, Jan Skov ; Hansson, Per. / Self-assembling properties of ionisable amphiphilic drugs in aqueous solution. In: Journal of Colloid and Interface Science. 2021 ; Vol. 600. pp. 701-710.

Bibtex

@article{b90c7ad058724c6fbd0cedaa65701b9a,
title = "Self-assembling properties of ionisable amphiphilic drugs in aqueous solution",
abstract = "Hypothesis: Common amphiphilic drug molecules often have a more rigid nonpolar part than conventional surfactants. The rigidity is expected to influence the self-assembling properties and possibly give rise to aggregation patterns different from that of regular surfactants. Experiments: We have investigated self-assembling properties of the hydrochloride salts of adiphenine (ADP), pavatrine (PVT), and amitriptyline (AMT) at concentrations up to 50 wt% using small-angle x-ray scattering, dynamic light scattering, cryo-transmission electron microscopy, and surface tension measurements. Findings: All drugs form small micelles of oblate spheroidal shape at concentrations above the critical micelle concentrations (CMC). The micelles grow weakly in size up to about 20 wt%, where the aggregation number reaches a maximum followed by a slight decrease in size at higher drug concentrations. We observe a correlation between the decrease in micelle size at high concentrations and an increasing charge of the micelles, as the degree of ionization increases with increasing drug concentration and decreasing pH. In contrast to what has previously been reported, the aggregation behavior of all studied drugs resembles the closed association behavior of conventional surfactants with a short aliphatic chain as hydrophobic tail group i.e. the micelles are always small in size and lack a second CMC. CMC values were determined with surface tension measurements, including also lidocaine hydrochloride (LDC) and chlorpromazine hydrochloride (CHL).",
keywords = "Amphiphilic drugs, Cryo-TEM, Dynamic light scattering (DLS), Micelles, Self-assembly, Small-angle x-ray scattering (SAXS)",
author = "Christina Efthymiou and Bergstr{\"o}m, {L. Magnus} and Pedersen, {Jannik Nedergaard} and Pedersen, {Jan Skov} and Per Hansson",
note = "Publisher Copyright: {\textcopyright} 2021 Elsevier Inc.",
year = "2021",
month = oct,
doi = "10.1016/j.jcis.2021.05.049",
language = "English",
volume = "600",
pages = "701--710",
journal = "Journal of Colloid and Interface Science",
issn = "0021-9797",
publisher = "Academic Press",

}

RIS

TY - JOUR

T1 - Self-assembling properties of ionisable amphiphilic drugs in aqueous solution

AU - Efthymiou, Christina

AU - Bergström, L. Magnus

AU - Pedersen, Jannik Nedergaard

AU - Pedersen, Jan Skov

AU - Hansson, Per

N1 - Publisher Copyright: © 2021 Elsevier Inc.

PY - 2021/10

Y1 - 2021/10

N2 - Hypothesis: Common amphiphilic drug molecules often have a more rigid nonpolar part than conventional surfactants. The rigidity is expected to influence the self-assembling properties and possibly give rise to aggregation patterns different from that of regular surfactants. Experiments: We have investigated self-assembling properties of the hydrochloride salts of adiphenine (ADP), pavatrine (PVT), and amitriptyline (AMT) at concentrations up to 50 wt% using small-angle x-ray scattering, dynamic light scattering, cryo-transmission electron microscopy, and surface tension measurements. Findings: All drugs form small micelles of oblate spheroidal shape at concentrations above the critical micelle concentrations (CMC). The micelles grow weakly in size up to about 20 wt%, where the aggregation number reaches a maximum followed by a slight decrease in size at higher drug concentrations. We observe a correlation between the decrease in micelle size at high concentrations and an increasing charge of the micelles, as the degree of ionization increases with increasing drug concentration and decreasing pH. In contrast to what has previously been reported, the aggregation behavior of all studied drugs resembles the closed association behavior of conventional surfactants with a short aliphatic chain as hydrophobic tail group i.e. the micelles are always small in size and lack a second CMC. CMC values were determined with surface tension measurements, including also lidocaine hydrochloride (LDC) and chlorpromazine hydrochloride (CHL).

AB - Hypothesis: Common amphiphilic drug molecules often have a more rigid nonpolar part than conventional surfactants. The rigidity is expected to influence the self-assembling properties and possibly give rise to aggregation patterns different from that of regular surfactants. Experiments: We have investigated self-assembling properties of the hydrochloride salts of adiphenine (ADP), pavatrine (PVT), and amitriptyline (AMT) at concentrations up to 50 wt% using small-angle x-ray scattering, dynamic light scattering, cryo-transmission electron microscopy, and surface tension measurements. Findings: All drugs form small micelles of oblate spheroidal shape at concentrations above the critical micelle concentrations (CMC). The micelles grow weakly in size up to about 20 wt%, where the aggregation number reaches a maximum followed by a slight decrease in size at higher drug concentrations. We observe a correlation between the decrease in micelle size at high concentrations and an increasing charge of the micelles, as the degree of ionization increases with increasing drug concentration and decreasing pH. In contrast to what has previously been reported, the aggregation behavior of all studied drugs resembles the closed association behavior of conventional surfactants with a short aliphatic chain as hydrophobic tail group i.e. the micelles are always small in size and lack a second CMC. CMC values were determined with surface tension measurements, including also lidocaine hydrochloride (LDC) and chlorpromazine hydrochloride (CHL).

KW - Amphiphilic drugs

KW - Cryo-TEM

KW - Dynamic light scattering (DLS)

KW - Micelles

KW - Self-assembly

KW - Small-angle x-ray scattering (SAXS)

UR - http://www.scopus.com/inward/record.url?scp=85106549775&partnerID=8YFLogxK

U2 - 10.1016/j.jcis.2021.05.049

DO - 10.1016/j.jcis.2021.05.049

M3 - Journal article

C2 - 34049025

AN - SCOPUS:85106549775

VL - 600

SP - 701

EP - 710

JO - Journal of Colloid and Interface Science

JF - Journal of Colloid and Interface Science

SN - 0021-9797

ER -