Ak. Zimmer et al., HYDROCORTISONE DELIVERY TO HEALTHY AND INFLAMED EYES USING A MICELLARPOLYSORBATE-80 SOLUTION OR ALBUMIN NANOPARTICLES, International journal of pharmaceutics, 110(3), 1994, pp. 211-222
Hydrocortisone was loaded onto albumin nanoparticles by sorption. Two
systems were tested, one comprised of a 0.03% saturated drug solution,
the other of a 0.2% micellised drug solution. In both cases 45-70% of
the originally available drug was bound to the carrier surface. The s
ystems were further tested by measuring the in vitro transport of radi
olabelled hydrocortisone through porcine cornea. Nanoparticles led to
sustained drug transport through the cornea. The distribution of both
0.2% hydrocortisone preparations (nanoparticles and solution) was then
evaluated under in vivo conditions in healthy and inflamed eyes of ra
bbits. In all tissues the level of drug was higher in the inflamed tha
n in the healthy eye due to increased cell permeability as a result of
inflammatory processes. The application of nanoparticles led to lower
hydrocortisone tissue concentrations than the reference solution due
to the strong binding of hydrocortisone onto the particle system and t
he resulting slow release. An exception occurred with the reference so
lution in the conjunctiva, as less drug was found in the inflamed than
in the normal tissue, since enhanced lacrimation led to increased dru
g drainage. In contrast, the corresponding nanoparticle preparation wa
s more efficiently retained at the inflamed than at the normal conjunc
tiva. Consequently, in the inflamed eye, hydrocortisone-loaded nanopar
ticles enabled targeting to the precorneal area away from the inner se
gments of the eye.