Delivery of a hydrophilic solute through the skin from novel microemulsion systems

M. Begoña Delgado-Charro, Graciela Iglesias-Vilas, José Blanco-Méndez, M. Arturo López-Quintela, Jean Paul Marty, Richard H. Guy

Research output: Contribution to journalArticle

157 Citations (Scopus)

Abstract

Five microemulsions were prepared with a mean radius of the internal phase droplets varying from 10 to 70 nm. The microemulsions were evaluated for their ability to deliver a model hydrophilic solute (sucrose) across hairless mouse skin in vitro. Maximum sucrose fluxes, following application of the different microemulsions for 9 h, were similar and were about an order of magnitude greater than that from a 20 mM sucrose aqueous solution. The five (unloaded) formulations and three controls (water, propylene glycol and 5% oleic acid in propylene glycol) were applied for 3 h to the ventral forearm of six volunteers. Transepidermal water loss (TEWL) and relative skin blood flow (SBF) were measured immediately after removing the formulations and repeatedly over a further 3 hour period. SBF increased significantly only after application of the oleic acid/propylene glycol positive control; for all other treatments, SBF remained at the pretreatment value. Immediately after removing all the formulations, TEWL was elevated. However, these values quickly recovered to the pretreatment control except in the case of oleic acid/propylene glycol. Overall, this preliminary study indicates that microemulsion formulations can be used to improve the delivery of hydrophilic solutes while eliciting insignificant effects on human skin in vivo.

Original languageEnglish
Pages (from-to)37-42
Number of pages6
JournalEuropean Journal of Pharmaceutics and Biopharmaceutics
Volume43
Issue number1
DOIs
Publication statusPublished - Jan 1997

Fingerprint

Propylene Glycol
Oleic Acid
Skin
Sucrose
Water
Hairless Mouse
Forearm
Volunteers
Therapeutics

Keywords

  • Microemulsions
  • Penetration enhancement
  • Relative skin blood flow
  • Sucrose
  • Transdermal delivery
  • Transepidermal water loss

Cite this

Delivery of a hydrophilic solute through the skin from novel microemulsion systems. / Delgado-Charro, M. Begoña; Iglesias-Vilas, Graciela; Blanco-Méndez, José; López-Quintela, M. Arturo; Marty, Jean Paul; Guy, Richard H.

In: European Journal of Pharmaceutics and Biopharmaceutics, Vol. 43, No. 1, 01.1997, p. 37-42.

Research output: Contribution to journalArticle

Delgado-Charro, M. Begoña ; Iglesias-Vilas, Graciela ; Blanco-Méndez, José ; López-Quintela, M. Arturo ; Marty, Jean Paul ; Guy, Richard H. / Delivery of a hydrophilic solute through the skin from novel microemulsion systems. In: European Journal of Pharmaceutics and Biopharmaceutics. 1997 ; Vol. 43, No. 1. pp. 37-42.
@article{a6f8f2478f864c13b6a2940a6e6b5111,
title = "Delivery of a hydrophilic solute through the skin from novel microemulsion systems",
abstract = "Five microemulsions were prepared with a mean radius of the internal phase droplets varying from 10 to 70 nm. The microemulsions were evaluated for their ability to deliver a model hydrophilic solute (sucrose) across hairless mouse skin in vitro. Maximum sucrose fluxes, following application of the different microemulsions for 9 h, were similar and were about an order of magnitude greater than that from a 20 mM sucrose aqueous solution. The five (unloaded) formulations and three controls (water, propylene glycol and 5{\%} oleic acid in propylene glycol) were applied for 3 h to the ventral forearm of six volunteers. Transepidermal water loss (TEWL) and relative skin blood flow (SBF) were measured immediately after removing the formulations and repeatedly over a further 3 hour period. SBF increased significantly only after application of the oleic acid/propylene glycol positive control; for all other treatments, SBF remained at the pretreatment value. Immediately after removing all the formulations, TEWL was elevated. However, these values quickly recovered to the pretreatment control except in the case of oleic acid/propylene glycol. Overall, this preliminary study indicates that microemulsion formulations can be used to improve the delivery of hydrophilic solutes while eliciting insignificant effects on human skin in vivo.",
keywords = "Microemulsions, Penetration enhancement, Relative skin blood flow, Sucrose, Transdermal delivery, Transepidermal water loss",
author = "Delgado-Charro, {M. Bego{\~n}a} and Graciela Iglesias-Vilas and Jos{\'e} Blanco-M{\'e}ndez and L{\'o}pez-Quintela, {M. Arturo} and Marty, {Jean Paul} and Guy, {Richard H.}",
year = "1997",
month = "1",
doi = "10.1016/S0939-6411(96)00016-1",
language = "English",
volume = "43",
pages = "37--42",
journal = "European Journal of Pharmaceutics and Biopharmaceutics",
issn = "0939-6411",
publisher = "Elsevier",
number = "1",

}

TY - JOUR

T1 - Delivery of a hydrophilic solute through the skin from novel microemulsion systems

AU - Delgado-Charro, M. Begoña

AU - Iglesias-Vilas, Graciela

AU - Blanco-Méndez, José

AU - López-Quintela, M. Arturo

AU - Marty, Jean Paul

AU - Guy, Richard H.

PY - 1997/1

Y1 - 1997/1

N2 - Five microemulsions were prepared with a mean radius of the internal phase droplets varying from 10 to 70 nm. The microemulsions were evaluated for their ability to deliver a model hydrophilic solute (sucrose) across hairless mouse skin in vitro. Maximum sucrose fluxes, following application of the different microemulsions for 9 h, were similar and were about an order of magnitude greater than that from a 20 mM sucrose aqueous solution. The five (unloaded) formulations and three controls (water, propylene glycol and 5% oleic acid in propylene glycol) were applied for 3 h to the ventral forearm of six volunteers. Transepidermal water loss (TEWL) and relative skin blood flow (SBF) were measured immediately after removing the formulations and repeatedly over a further 3 hour period. SBF increased significantly only after application of the oleic acid/propylene glycol positive control; for all other treatments, SBF remained at the pretreatment value. Immediately after removing all the formulations, TEWL was elevated. However, these values quickly recovered to the pretreatment control except in the case of oleic acid/propylene glycol. Overall, this preliminary study indicates that microemulsion formulations can be used to improve the delivery of hydrophilic solutes while eliciting insignificant effects on human skin in vivo.

AB - Five microemulsions were prepared with a mean radius of the internal phase droplets varying from 10 to 70 nm. The microemulsions were evaluated for their ability to deliver a model hydrophilic solute (sucrose) across hairless mouse skin in vitro. Maximum sucrose fluxes, following application of the different microemulsions for 9 h, were similar and were about an order of magnitude greater than that from a 20 mM sucrose aqueous solution. The five (unloaded) formulations and three controls (water, propylene glycol and 5% oleic acid in propylene glycol) were applied for 3 h to the ventral forearm of six volunteers. Transepidermal water loss (TEWL) and relative skin blood flow (SBF) were measured immediately after removing the formulations and repeatedly over a further 3 hour period. SBF increased significantly only after application of the oleic acid/propylene glycol positive control; for all other treatments, SBF remained at the pretreatment value. Immediately after removing all the formulations, TEWL was elevated. However, these values quickly recovered to the pretreatment control except in the case of oleic acid/propylene glycol. Overall, this preliminary study indicates that microemulsion formulations can be used to improve the delivery of hydrophilic solutes while eliciting insignificant effects on human skin in vivo.

KW - Microemulsions

KW - Penetration enhancement

KW - Relative skin blood flow

KW - Sucrose

KW - Transdermal delivery

KW - Transepidermal water loss

UR - http://www.scopus.com/inward/record.url?scp=0031398808&partnerID=8YFLogxK

UR - http://dx.doi.org/10.1016/S0939-6411(96)00016-1

U2 - 10.1016/S0939-6411(96)00016-1

DO - 10.1016/S0939-6411(96)00016-1

M3 - Article

VL - 43

SP - 37

EP - 42

JO - European Journal of Pharmaceutics and Biopharmaceutics

JF - European Journal of Pharmaceutics and Biopharmaceutics

SN - 0939-6411

IS - 1

ER -