Effect of the chemical structure on the drug release from brinzolamide based nano eye-drops

Yoshitaka Koseki, Yoshikazu Ikuta, Kota Sato, Shigenobu Aoyagi, Satoshi Inada, Tsunenobu Onodera, Hidetoshi Oikawa, Koji Nishiguchi, Toru Nakazawa, Hitoshi Kasai

Research output: Contribution to journalArticlepeer-review

3 Citations (Scopus)


Commercially available eye-drops scarcely penetrate the eye because of the cornea, which is located at the surface of the eye and function of barrier to keep out foreign matter. To enhance the penetration ratio of eye-drop, we have proposed nanometer-sized eye-drops called “nano eye-drops.” A series of prodrug compounds derived from brinzolamide, a glaucoma therapeutic agent, connected with a trimethyl lock (TML) group were synthesized and the nano eye-drops of the resulting prodrugs were successfully fabricated by the reprecipitation method. We found that the drug release of nano eye-drops critically depended on the chemical structure of the prodrugs comprising the nano eye-drops. As a result, the timing of the ocular hypotensive effect was controlled by altering the chemical structure of brinzolamide prodrug. These results provide insight into drug design for effective controlled release.

Original languageEnglish
Pages (from-to)122-128
Number of pages7
JournalMolecular crystals and liquid crystals
Issue number1
Publication statusPublished - 2020 Jul 23


  • brinzolamide
  • nano eye-drops
  • reprecipitation method
  • trimethyl lock group

ASJC Scopus subject areas

  • Chemistry(all)
  • Materials Science(all)
  • Condensed Matter Physics


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