Nanoparticles for drug delivery

Purpose To test dorzolamide cyclodextrin microparticle eye drops applied once a day (QD)for intraocular pressure control,compared with Trusopt® 3 times a day (TID). Methods Self aggregating cyclodextrin microparticle eye drops (DorzNP) containing 3% dorzolamide were formulated. The effect of the DorzNP eye drops QD was compared to Trusopt® TID in a prospective randomized single masked crossover trial over 24 hours. Seventeen healthy volunteers with intraocular pressure (IOP) over 18 mmHg were recruited. IOP was measured with an Icare tonometer pro and each patient underwent full eye examination. Results DorzNP eye drops QD and Trusopt® TID lower IOP in a similar manner. At no time point was there a significant difference in IOP between the two groups. The peak effect in both groups was at 4 hours: In the DorzNP group IOP decreased from 21.7 ± 2.4 mmHg at baseline to 17.9 ± 3.9 mmHg, which is 3.8 ± 2.6 mmHg and 18% IOP decrease. In the Trusopt® group IOP decreased from 20.9 ± 2.2 mmHg at baseline to 17.9 ± 3.3, at 4 hours which is 3.1 ± 3.7 mmHg ,14%, (p = 0.97 between groups) IOP drop. At trough at 24 hours the IOP drop was 1.4 ± 2.8 (6%) in DorzNP eyes and 1.5 ± 2.0 (7%) in Trusopt eyes (p = 0.23). Burning in DorzNP eyes on the scale 1‐100 was 12±15 and in Trusopt® eyes 37±30 (p=0.0038). Vision aquity and redness did not differ between the two groups Conclusion The results suggest that once a day dorzolamide nanoparticle eye drops have a similiar effect on intraocular pressure as Trusopt® applied 3 times a day. The dorzolamide microparticle eye drops are well tolerated, less burning than Trusopt®and significantly reduce intraocular pressure.Commercial interest