Kinetically Stable Bicelles with Dilution Tolerance, Size Tunability, and Thermoresponsiveness for Drug Delivery Applications

Mixtures of a phospholipid (1,2‐dipalmitoyl‐sn‐glycero‐3‐phosphatidylcholine, DPPC) and a sodium‐cholate‐derived surfactant (SC‐C5) at room temperature formed phospholipid bilayer fragments that were edge‐stabilized by SC‐C5: so‐called “bicelles”. Because the bilayer melting point of DPPC (41 °C) is...

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Veröffentlicht in:Chembiochem : a European journal of chemical biology 2018-09, Vol.19 (18), p.1922-1926
Hauptverfasser: Uchida, Noriyuki, Nishizawa Horimoto, Noriko, Yamada, Kuniyo, Hikima, Takaaki, Ishida, Yasuhiro
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container_end_page 1926
container_issue 18
container_start_page 1922
container_title Chembiochem : a European journal of chemical biology
container_volume 19
creator Uchida, Noriyuki
Nishizawa Horimoto, Noriko
Yamada, Kuniyo
Hikima, Takaaki
Ishida, Yasuhiro
description Mixtures of a phospholipid (1,2‐dipalmitoyl‐sn‐glycero‐3‐phosphatidylcholine, DPPC) and a sodium‐cholate‐derived surfactant (SC‐C5) at room temperature formed phospholipid bilayer fragments that were edge‐stabilized by SC‐C5: so‐called “bicelles”. Because the bilayer melting point of DPPC (41 °C) is above room temperature and because SC‐C5 has an exceptionally low critical micelle concentration (
doi_str_mv 10.1002/cbic.201800304
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Because the bilayer melting point of DPPC (41 °C) is above room temperature and because SC‐C5 has an exceptionally low critical micelle concentration (&lt;0.5 mm), the bicelles are kinetically frozen at room temperature. Consequently, they exist even when the mixture is diluted to a concentration of 0.04 wt %. In addition, the lateral size of the bicelles can be fine‐tuned by altering the molar ratio of DPPC to SC‐C5. On heating to ≈37 °C, the bicelles transformed into micelles composed of DPPC and SC‐C5. By taking advantage of the dilution tolerance, size tunability, and thermoresponsiveness, we demonstrated in vitro drug delivery based on use of the bicelles as carriers, which suggests their potential utility in transdermal drug delivery. Frozen membrane disks: Bicelles with structures that are kinetically frozen at room temperature were developed by assembling a phospholipid with a high bilayer melting point and a surfactant with an exceptionally low critical micelle concentration. 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source MEDLINE; Wiley Online Library Journals Frontfile Complete
subjects Antibiotics, Antineoplastic - administration & dosage
Antibiotics, Antineoplastic - pharmacokinetics
bicelles
biomembranes
Cell Line
Delayed-Action Preparations - chemistry
Dilution
Doxorubicin - administration & dosage
Doxorubicin - pharmacokinetics
Drug delivery
Drug Delivery Systems
Drug Liberation
Humans
Kinetics
Lecithin
Lipid Bilayers - chemistry
Melting point
Melting points
Micelles
Phosphatidylcholine
Phosphatidylcholines - chemistry
Phospholipids
Sodium
Surface-Active Agents - chemistry
surfactants
Temperature
Temperature effects
Transdermal medication
title Kinetically Stable Bicelles with Dilution Tolerance, Size Tunability, and Thermoresponsiveness for Drug Delivery Applications
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