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

Drug Dev Ind Pharm. 2005 Mar;31(3):263-9. doi: 10.1081/ddc-52058.

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.

Publication types

  • Clinical Trial
  • Multicenter Study
  • Randomized Controlled Trial

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / administration & dosage*
  • Anti-Inflammatory Agents, Non-Steroidal / analysis
  • Chromatography, High Pressure Liquid
  • Cyclosporine / administration & dosage*
  • Cyclosporine / analysis
  • Diclofenac / administration & dosage*
  • Diclofenac / analysis
  • Drug Carriers*
  • Dry Eye Syndromes / drug therapy*
  • Female
  • Humans
  • Immunosuppressive Agents / administration & dosage*
  • Immunosuppressive Agents / analysis
  • Ophthalmic Solutions / analysis
  • Ophthalmic Solutions / therapeutic use*
  • Rabbits

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Drug Carriers
  • Immunosuppressive Agents
  • Ophthalmic Solutions
  • Diclofenac
  • Cyclosporine