چکیده (انگلیسی):

This study investigated the
solubilization of cyclosporin A (CsA), a neutral
undecapeptide, by cosolvency, micellization, and
complexation. Cosolvents (ethanol, propylene glycol,
polyethylene glycol, tetrahydrofurfuryl alcohol
polyethyleneglycol ether, and glycerin), surfactants
(polyoxyethylene sorbitan monooleate [(Tween 80)],
polyoxyethylene sorbitan monolaurate [(Tween 20)],
and Cremophor EL), and cyclodextrins (α-cyclodextrin
[(αCD)] and hydroxypropyl-β-cyclodextrin[(HPβCD)]
were used as solubilizing agents in this study.
Surfactants had a noticeable effect in increasing CsA
solubility. Twenty percent solutions of Tween 20, Tween
80, and Cremophor EL increased the solubility by 60 to
160 fold. Cyclodextrins can increase the CsA solubility,
but αCD was more effective than HPβCD. Cosolvents on
the other hand did not increase the solubility of CsA as
much as expected from the LOGP (logrithm of wateroctanol
partition coefficent) value of CsA.