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. 2014 Jul;22(3):240-5.
doi: 10.1016/j.jsps.2013.03.001. Epub 2013 Mar 30.

A novel approach to formulation factor of aceclofenac eye drops efficiency evaluation based on physicochemical characteristics of in vitro and in vivo permeation

Vivek Dave  1 , Sarvesh Paliwal  1
Affiliations

A novel approach to formulation factor of aceclofenac eye drops efficiency evaluation based on physicochemical characteristics of in vitro and in vivo permeation

Vivek Dave et al. Saudi Pharm J. 2014 Jul.

Abstract

The purpose of the present study was to evaluate aceclofenac eye drop through excised goat cornea. Raising pH of the formulation from 6.0 to 8.0, effect of different preservatives or effect of viscosity enhancer decreases apparent permeability coefficient. Topical ophthalmic NSAID are used to treat ocular surface and anterior segment inflammation as well as post operative management of pain and inflammation. Aceclofenac's unique chemical structure makes it both a potent anti inflammatory drug and lipophilic molecule that penetrates ocular tissue, ensuring relief of pain in cataract and refractive surgery and corneal abrasion. The octanol/water partition coefficient of aceclofenac drug is 1.86 ± 0.75. Permeation characteristics of the drug were evaluated by putting 1 ml formulation on freshly excised goat cornea fixed between donor and receptor compartments of an all-glass modified Franz diffusion cell and measuring the drug permeated in the receptor by spectrophotometry at 275 nm, after 120 min. The results suggest that aceclofenac ophthalmic solution (pH 7) containing BAC provides increased in vitro ocular availability through goat corneas. The combination of methyl paraben and propyl paraben MP-PP preservative in aceclofenac ophthalmic eye drop 0.1% formulated in phosphate buffer increases transcorneal permeation. The developed formulations were evaluated for their pharmacodynamics in albino rabbits, by measuring in-vivo study and were compared to a marketed voltrane ophthalmic solution.

Keywords: Aceclofenac; Cornea; Permeation; Transcorneal.

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Figures

Figure 1
Figure 1
Goat cornea.
Figure 2
Figure 2
Effect of pH on aceclofenac transcorneal permeation by goat cornea. Values are mean ± S.D. (n = 3)
Figure 3
Figure 3
Effect of preservative on aceclofenac transcorneal permeation by goat cornea. Values are mean ± S.D. (n = 3).
Figure 4
Figure 4
Effect of viscosity enhancer of aceclofenac on transcorneal permeation by goat cornea.
Figure 5
Figure 5
In-vivo study of eye drop.
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