PubMed · 11198251
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K Landow. 2001. OTC agents for ringworm?. https://doi.org/10.3810/pgm.2001.01.847
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A novel bilayer chitosan membrane was prepared by a combined wet/dry phase inversion method and evaluated as a wound dressing. This new type of bilayer chitosan wound dressing, consisting of a dense upper layer (skin layer) and a sponge-like lower layer (sublayer), is very suitable for use as a topical delivery of silver sulfadiazine (AgSD) for the control of wound infections. Physical characterization of the bilayer wound dressing showed that it has excellent oxygen permeability, that it controls the water vapor transmission rate, and that it promotes water uptake capability. AgSD dissolved from bilayer chitosan dressings to release silver and sulfadiazine. The release of sulfadiazine from the bilayer chitosan dressing displayed a burst release on the first day and then tapered off to a much slower release. However, the release of silver from the bilayer chitosan dressing displayed a slow release profile with a sustained increase of silver concentration. The cultures of Pseudomonas aeruginosa and Staphylococcus aureus in agar plates showed effective antimicrobial activity for 1 week. In vivo antibacterial tests confirmed that this wound dressing is effective for long-term inhibition of the growth of Pseudomonas aeruginosa and Staphylococcus aureus at an infected wound site. The results in this study indicate that the AgSD-incorporated bilayer chitosan wound dressing may be a material with potential antibacterial capability for the treatment of infected wounds.
The solubilities in isopropyl myristate (S(IPM)) and pH 4.0 buffer (S(AQ)) and the partition coefficients between IPM and pH 4.0 buffer (K(IPM:AQ)) have been measured for a series of 1,3-bisalkylcarbonyl-5-fluorouracil prodrugs (1,3-AC-5-FU). The 1,3-AC-5-FU prodrugs were each over 500 times more soluble in IPM, but all members of the series, whose solubilities could be estimated, were much less soluble in pH 4.0 buffer than 5-FU. The abilities of the 1,3-AC-5-FU prodrugs to deliver total 5-FU species through hairless mouse skin from IPM suspensions (J(i)) were also measured. The 1,3-diacetyl derivative 2, which exhibited the highest S(AQ) in the series, gave the highest J(i) value. Although the series of 1,3-AC-5-FU prodrugs was generally effective at increasing J(i) (three to ten times), the best 1,3-AC-5-FU prodrug was not as effective as the best 1- or 3-alkylcarbonyl-5-FU prodrug (1- or 3-AC-5-FU) at increasing J(i) and their ability to increase the concentration of total 5-FU species in the skin was generally less than that of the 1-AC-5-FU prodrugs, but greater than that of the 3-AC-5-FU prodrugs. Thus, the 1-AC-5-FU prodrugs remain the best prodrugs with which to enhance the topical delivery of 5-FU.
OBJECTIVE: To explore the mechanism by which diclofenac sodium eyedrops exert an adverse effect on the cornea. METHODS: In 10 healthy Japanese volunteers, 0.1% diclofenac sodium solution was instilled into one eye 3 times daily for 2 weeks. Only vehicle was applied to the other eye. Tear samples were taken before drug treatment, at 2 weeks (on the final day of treatment), and at 4 weeks. Prostaglandin E(2) and substance P concentrations in tears were measured using enzyme immunoassays. RESULTS: After treatment for 2 weeks, concentrations of both prostaglandin E(2) and substance P in tears from diclofenac sodium-treated eyes had decreased significantly, and both had returned to baseline levels by 4 weeks. No significant changes were seen in prostaglandin E(2) and substance P levels in vehicle-treated eyes at any time points. CONCLUSIONS: Diclofenac sodium eyedrops concurrently reduced concentrations of prostaglandin E(2) and substance P in tears. Depletion of substance P (a pain-associated neurotransmitter) by diclofenac sodium may promote development of corneal complications.