Lipid vesicular gels for topical administration of antioxidants
Fornasier, Marco LU
; Dessì, Francesca
LU
; Pireddu, Rosa
; Sinico, Chiara
; Carretti, Emiliano
and Murgia, Sergio
(2022)
In Colloids and Surfaces B: Biointerfaces
213.
- Abstract
The application of a formulation on the skin represents an effective way to deliver bio-active molecules for therapeutical purposes. Moreover, the outermost skin layer, the stratum corneum, can be overcome by employing chemical permeation enhancers and edge activators as components. Several lipids can be considered as permeation enhancers, such as the ubiquitous monoolein, one of the most used building blocks for the preparation of lipid liquid crystalline nanoparticles which are applied as drug carriers for nanomedicine applications. Recent papers highlighted how bile salts can affect the phase behavior of monoolein to obtain drug carriers suitable for topical administration, given their role as edge activators into the formulation.... (More)
The application of a formulation on the skin represents an effective way to deliver bio-active molecules for therapeutical purposes. Moreover, the outermost skin layer, the stratum corneum, can be overcome by employing chemical permeation enhancers and edge activators as components. Several lipids can be considered as permeation enhancers, such as the ubiquitous monoolein, one of the most used building blocks for the preparation of lipid liquid crystalline nanoparticles which are applied as drug carriers for nanomedicine applications. Recent papers highlighted how bile salts can affect the phase behavior of monoolein to obtain drug carriers suitable for topical administration, given their role as edge activators into the formulation. Herein, the encapsulation of natural antioxidants (caffeic acid and ferulic acid) into lipid vesicular gels (LVGs) made by monoolein and sodium taurocholate (TC) in water was studied to produce formulations suitable for topical application. TC induces a bicontinuous cubic to multilamellar phase transition for monoolein in water at the given concentrations, and by increasing its content into the formulations, unilamellar LVGs are formed. The encapsulation of the two antioxidants did not affect significantly the structure of the gels. The oscillating rheological studies showed that ferulic acid has a structuring effect on the lipid matrix, in comparison with the empty dispersion and the one containing caffeic acid. These gels were then tested in vitro on new-born pig skin to evaluate their efficacy as drug carriers for topical administration, showing that caffeic acid is mostly retained in the gel whereas ferulic acid is released at a higher degree. The data herein reported provide some further information on the effect of bile salts on the lipid self-assembly to evaluate useful compositions for topical administration of natural antioxidants.
(Less)
- author
- Fornasier, Marco
LU
; Dessì, Francesca
LU
; Pireddu, Rosa
; Sinico, Chiara
; Carretti, Emiliano
and Murgia, Sergio
- organization
- publishing date
- 2022-05-01
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Bile salts, Lamellarity, Monoolein, Skin, Sodium taurocholate
- in
- Colloids and Surfaces B: Biointerfaces
- volume
- 213
- article number
- 112388
- publisher
- Elsevier
- external identifiers
-
- scopus:85124666131
- pmid:35183999
- ISSN
- 0927-7765
- DOI
- 10.1016/j.colsurfb.2022.112388
- language
- English
- LU publication?
- yes
- id
- 5c3d03c1-3285-45ce-9ee3-ba6fdc5ca18b
- date added to LUP
- 2022-05-18 15:11:59
- date last changed
- 2024-06-27 13:53:20
@article{5c3d03c1-3285-45ce-9ee3-ba6fdc5ca18b,
abstract = {{<p>The application of a formulation on the skin represents an effective way to deliver bio-active molecules for therapeutical purposes. Moreover, the outermost skin layer, the stratum corneum, can be overcome by employing chemical permeation enhancers and edge activators as components. Several lipids can be considered as permeation enhancers, such as the ubiquitous monoolein, one of the most used building blocks for the preparation of lipid liquid crystalline nanoparticles which are applied as drug carriers for nanomedicine applications. Recent papers highlighted how bile salts can affect the phase behavior of monoolein to obtain drug carriers suitable for topical administration, given their role as edge activators into the formulation. Herein, the encapsulation of natural antioxidants (caffeic acid and ferulic acid) into lipid vesicular gels (LVGs) made by monoolein and sodium taurocholate (TC) in water was studied to produce formulations suitable for topical application. TC induces a bicontinuous cubic to multilamellar phase transition for monoolein in water at the given concentrations, and by increasing its content into the formulations, unilamellar LVGs are formed. The encapsulation of the two antioxidants did not affect significantly the structure of the gels. The oscillating rheological studies showed that ferulic acid has a structuring effect on the lipid matrix, in comparison with the empty dispersion and the one containing caffeic acid. These gels were then tested in vitro on new-born pig skin to evaluate their efficacy as drug carriers for topical administration, showing that caffeic acid is mostly retained in the gel whereas ferulic acid is released at a higher degree. The data herein reported provide some further information on the effect of bile salts on the lipid self-assembly to evaluate useful compositions for topical administration of natural antioxidants.</p>}},
author = {{Fornasier, Marco and Dessì, Francesca and Pireddu, Rosa and Sinico, Chiara and Carretti, Emiliano and Murgia, Sergio}},
issn = {{0927-7765}},
keywords = {{Bile salts; Lamellarity; Monoolein; Skin; Sodium taurocholate}},
language = {{eng}},
month = {{05}},
publisher = {{Elsevier}},
series = {{Colloids and Surfaces B: Biointerfaces}},
title = {{Lipid vesicular gels for topical administration of antioxidants}},
url = {{http://dx.doi.org/10.1016/j.colsurfb.2022.112388}},
doi = {{10.1016/j.colsurfb.2022.112388}},
volume = {{213}},
year = {{2022}},
}