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.
Quintana-Hau
J D
JD
Research and Development Department, Laboratorios Sophia, 797 Hidalgo, Guadalajara, Jalisco 44290, Mexico. invesmol@sophia.com.mx
Cruz-Olmos
E
E
López-Sánchez
M I
MI
Sánchez-Castellanos
V
V
Baiza-Durán
L
L
González
J R
JR
Tornero-Montaño
Mondragón-Flores
R
R
Hernández-Santoyo
A
A
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
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004337:Drug Carriers; D007166:Immunosuppressive Agents; D009883:Ophthalmic Solutions; D004008:Diclofenac; D016572:Cyclosporine