Replies to post #113 on Biotech Values

[rph_in_wi]

Do we have any medicinal chemists in the house?

While not a medicinal chemist, I was interested in the structure as it pertains to transdermal/nasal administration. My feeling is that, as a water soluble chemical, it would not be an easy formulation to put into a transdermal delivery system. Because the skin is made of fat, usually the best candidates for transdermal delivery are fat soluble chemicals. This limitation could be overcome through the use of a "carrier" molecule attached to squalaimine. DRAWBACK: this will probebly change the potency/SE profile of the drug. This would mean new dose-ranging studies and a potentially long delay.
Another potential problem that I am wrestling with is the localized effects of squalamine as it crosses the blood vessel walls into the blood stream. With IV delivery, the drug never crosses the endothelial wall, espeacially not in a concentrated state. How would the direct inactivation of the blood vessel's endothelial wall at the site be effected?
These questions all make me feel that squalamine is being studied with the proper delivery system. Were any of these other delivery systems suggested by the company or from other posts?
Any comments welcome,
RPh