Evaluation of Pharmasolve corneal permeability enhancement and its irritation on rabbit eyes.
The aim of this study was to explore the use of Pharmasolve as a new kind of permeability enhancer in ophthalmic drug delivery systems. The ocular irritation of different concentrations of Pharmasolve on rabbit eyes was evaluated in detail. Four drugs ranging from hydrophilic to lipophilic, namely ribavirin, puerarin, enoxacin, and ibuprofen, were used as model compounds to investigate the effects of different concentrations of Pharmasolve on the corneal permeability. The mechanism of ocular permeation enhancement of drugs by Pharmasolve was also discussed. The results showed that Pharmasolve presented no irritation when the concentration used was lower than 10%. Pharmasolve could enhance the ocular permeability of the four test drugs; the maximum enhancement in P(app) was 4.04, 2.76, and 2.67-fold for ribavirin, enoxacin, and puerarin, respectively; 2.5% (v/v) Pharmasovle increased the P(app) by about 1.47-fold for ibuprofen; which suggested that it would have a great potential to be used as a safe and effective penetration enhancer in ocular drug delivery systems in the future.
Li
Xiang
X
Department of Pharmaceutics, Shenyang Pharmaceutical University, PR China.
Pan
Weisan
W
Ju
Chengyi
C
Liu
Zhidong
Z
Pan
Hao
H
Zhang
Huihui
H
Nie
Shufang
S
D000818:Animals; D003315:Cornea / Q000187:drug effects* / Q000502:physiology; D015365:Enoxacin / Q000009:adverse effects; D005123:Eye / Q000187:drug effects* / Q000503:physiopathology; D005131:Eye Injuries / Q000209:etiology; D055103:Hypodermoclysis; D007052:Ibuprofen / Q000009:adverse effects; D007529:Isoflavones / Q000009:adverse effects; D010539:Permeability / Q000187:drug effects; D011759:Pyrrolidines / Q000494:pharmacology*; D011817:Rabbits; D012254:Ribavirin / Q000009:adverse effects; D014665:Vasodilator Agents / Q000009:adverse effects
D007529:Isoflavones; D011759:Pyrrolidines; D014665:Vasodilator Agents; C054965:N-methylpyrrolidine; D015365:Enoxacin; D012254:Ribavirin; D007052:Ibuprofen; C033607:puerarin