Oil-Frozen W1/O/W2 Double Emulsions for Dermal Biomacromolecular Delivery Containing Ethanol as Chemical Penetration Enhancer

Oil-frozen water-in-oil-in-water (W1/O/W2) double emulsions (DE) containing ethanol up to 40% (w/v) in the external aqueous W2 phase exhibited external coalescence upon thawing of the oil phase, releasing up to 85% of the encapsulated protein of the internal aqueous phase. These emulsions were studi...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 2011-04, Vol.100 (4), p.1398-1406
Main Authors: Jaimes-Lizcano, Yuly A., Lawson, Louise B., Papadopoulos, Kyriakos D.
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Animals
Biological and medical sciences
Cattle
emulsion
Emulsions - chemistry
Ethanol - chemistry
Fluorescein-5-isothiocyanate - administration & dosage
Fluorescein-5-isothiocyanate - analogs & derivatives
Fluorescein-5-isothiocyanate - pharmacokinetics
formulation
Freezing
General pharmacology
macromolecular drug delivery
Medical sciences
Oils - chemistry
permeation enhancers
Pharmaceutical technology. Pharmaceutical industry
Pharmaceutical Vehicles - chemistry
Pharmacology. Drug treatments
Serum Albumin, Bovine - administration & dosage
Serum Albumin, Bovine - pharmacokinetics
Skin - metabolism
Skin Absorption
Swine
transdermal drug delivery
Water - chemistry
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Summary:Oil-frozen water-in-oil-in-water (W1/O/W2) double emulsions (DE) containing ethanol up to 40% (w/v) in the external aqueous W2 phase exhibited external coalescence upon thawing of the oil phase, releasing up to 85% of the encapsulated protein of the internal aqueous phase. These emulsions were studied in vitro as potential dermal macromolecular delivery formulations, achieving fluorescein isothiocyanate-labeled bovine serum albumin (FITC-BSA) penetration of up to 86μm into porcine skin, reaching the viable epidermis where the immunocompetent Langerhans cells are located. Enzyme-linked immunosorbent assay was performed to observe the effect of the emulsification process and ethanol content on the ability of BSA to form antigen–antibody complexes; results indicated that ethanol content and the emulsification process did not diminish the BSA–antibody complex formation when compared with a BSA standard aqueous solution. Therefore, it is shown that oil-frozen W1/O/W2 DE, with penetration-enhancing ethanol in the W2 phase, can potentially be used for cutaneous vaccine delivery formulations.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.22362