Characterization of the novel ophthalmic drug carrier Sophisen in two of its derivatives: 3A Ofteno and Modusik-A Ofteno.

Sophisen, a new ophthalmic drug carrier, was characterized using physicochemical and morphological criteria. Diclofenac belongs to a nonsteroidal anti-inflammatory molecule group and its ophthalmic use avoids side effects produced by steroid drugs. Cyclosporine-A is a cyclic peptide used as an immunosuppressive when administrated systemically. Its application in ophthalmology has been reported, but it is a very poor soluble drug. Diclofenac sodium and Cyclosporine-A were mixed with Sophisen to render two new ophthalmic solutions that were named 3A Ofteno and Modusik-A Ofteno, respectively. Based on transmission electron microscopy and dynamic light scattering studies, we concluded that Sophisen is a polydisperse solution with a molecular weight of 413 +/-122 kDa, whereas 3A Ofteno and Modusik-A Ofteno are monodisperse solutions with molecular weights of 169 +/- 44 and 153 +/- 10, respectively. Sophisen was shown to be a good carrier for diclofenac sodium as evaluated by passive diffusion through the cornea. A comparative study suggests that diclofenac applied as eye drops was better tolerated when associated with Sophisen. In addition, Modusik-A Ofteno, a new aqueous solution of Cyclosporine-A, improved tear production in patients with moderate or severe dry eye condition.