Characterization of the novel ophthalmic drug carrier Sophisen in two of its derivatives: 3A Ofteno and Modusik-A Ofteno.
Author(s): Quintana-Hau JD, Cruz-Olmos E, Lopez-Sanchez MI, Sanchez-Castellanos V, Baiza-Duran L, Gonzalez JR, Tornero-Montano, Mondragon-Flores R, Hernandez-Santoyo A
Affiliation(s): Research and Development Department, Laboratorios Sophia, 797 Hidalgo, Guadalajara, Jalisco 44290, Mexico. invesmol@sophia.com.mx
Publication date & source: 2005-03, Drug Dev Ind Pharm., 31(3):263-9.
Publication type: Clinical Trial; Multicenter Study; Randomized Controlled Trial
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.
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