Transdermal Delivery of an Anti-Cancer Drug via W/O Emulsions Based on Alkyl Polyglycosides and Lecithin: Design, Characterization, and In Vivo Evaluation of the Possible Irritation Potential in Rats

The purpose of this work was to develop w/o emulsions that could be safely used to promote transdermal delivery of 5-fluorouracil (5-FU). Two pseudo-ternary phase diagrams comprising oleoyl-macrogol glycerides, water, and a surfactant/co-surfactant (S/CoS) mixture of lecithin, ethanol, and either co...

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Bibliographic Details
Published in:AAPS PharmSciTech 2011-03, Vol.12 (1), p.1-9
Main Authors: ElMeshad, Aliaa Nabil, Tadros, Mina Ibrahim
Format: Article
Language:English
Subjects:
Administration, Cutaneous
Animals
Antineoplastic Agents - administration & dosage
Antineoplastic Agents - chemistry
Antineoplastic Agents - toxicity
Biochemistry
Biomedical and Life Sciences
Biomedicine
Biotechnology
Drug Delivery Systems
Drug Stability
Emulsions
Fluorouracil - administration & dosage
Fluorouracil - chemistry
Fluorouracil - toxicity
Glycosides - chemistry
Indexing in process
Irritants - analysis
Irritants - chemistry
Lecithins - chemistry
Male
Mice
Particle Size
Permeability
Pharmacology/Toxicology
Pharmacy
Polyethylene Glycols - analysis
Polyethylene Glycols - chemistry
Polymers - chemistry
Rats
Research Article
Skin
Skin Irritancy Tests
Surface-Active Agents - chemistry
Water
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Summary:The purpose of this work was to develop w/o emulsions that could be safely used to promote transdermal delivery of 5-fluorouracil (5-FU). Two pseudo-ternary phase diagrams comprising oleoyl-macrogol glycerides, water, and a surfactant/co-surfactant (S/CoS) mixture of lecithin, ethanol, and either coco glucoside or decyl glucoside were investigated for their potential to develop promising 5-FU emulsions. Six systems were selected and subjected to thermodynamic stability tests; heat–cool cycles, centrifugation, and finally freeze–thaw cycles. All systems passed the challenges and were characterized for transmission electron microscopy, droplet size, rheological behavior, pH, and transdermal permeation through newly born mice skin in Franz diffusion cells. The systems had spherical droplets ranging in diameter from 1.81 to 2.97 μm, pH values ranging from 7.50 to 8.49 and possessed Newtonian flow. A significant ( P  
ISSN:1530-9932
1530-9932
DOI:10.1208/s12249-010-9557-y