title: Characterization of the novel ophthalmic drug carrier Sophisen in two of its derivatives: 3A Ofteno and Modusik-A Ofteno.
abstract: 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.
authors.affiliation: Research and Development Department, Laboratorios Sophia, 797 Hidalgo, Guadalajara, Jalisco 44290, Mexico. invesmol@sophia.com.mx
authors.forename: J D
authors.initials: JD
authors.lastname: Quintana-Hau
authors.forename: E
authors.initials: E
authors.lastname: Cruz-Olmos
authors.forename: M I
authors.initials: MI
authors.lastname: López-Sánchez
authors.forename: V
authors.initials: V
authors.lastname: Sánchez-Castellanos
authors.forename: L
authors.initials: L
authors.lastname: Baiza-Durán
authors.forename: J R
authors.initials: JR
authors.lastname: González
authors.lastname: Tornero-Montaño
authors.forename: R
authors.initials: R
authors.lastname: Mondragón-Flores
authors.forename: A
authors.initials: A
authors.lastname: Hernández-Santoyo
mesh_terms: D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage* / Q000032:analysis; D002851:Chromatography, High Pressure Liquid; D016572:Cyclosporine / Q000008:administration & dosage* / Q000032:analysis; D004008:Diclofenac / Q000008:administration & dosage* / Q000032:analysis; D004337:Drug Carriers; D015352:Dry Eye Syndromes / Q000188:drug therapy*; D005260:Female; D006801:Humans; D007166:Immunosuppressive Agents / Q000008:administration & dosage* / Q000032:analysis; D009883:Ophthalmic Solutions / Q000032:analysis / Q000627:therapeutic use*; D011817:Rabbits
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D007166:Immunosuppressive Agents; D009883:Ophthalmic Solutions; D004008:Diclofenac; D016572:Cyclosporine