title: Effects of Labrasol on the corneal drug delivery of baicalin.
abstract: OBJECTIVE
  To investigate the use of Labrasol in ocular drug delivery system.
  
  
  METHODS
  The in vivo ocular irritation of Labrasol was tested by pathological section observation using rabbits. The effects of Labrasol on corneal permeability of baicalin was investigated in vitro, using isolated rabbit corneas. The pharmacokinetics was evaluated by microdialysis in the rabbit aqueous humors.
  
  
  RESULTS
  The results of the ocular irritation studies showed that Labrasol was non-irritant at the concentrations studied (0.5-3.0%(v/v)), while Labrasol produced slight irritation at a concentration of 5.0%(v/v). For the in vitro study, with Labrasol at concentrations of 1.5%, 2.0%, and 3.0%(v/v), the apparent permeability coefficient (P(app)) was 1.69-, 3.14-, and 2.23- fold of baicalin solution, respectively. In the pharmacokinetics studies, the AUC value of baicalin solution with 2.0% and 3.0%(v/v) Labrasol were 4.7- and 5.6-fold of that of the control group (p < 0.01), and the Cmax value of baicalin solution with 2.0% and 3.0%(v/v) Labrasol vs the control group were 3.2- and 5.7-fold (p < 0.01).
  
  
  CONCLUSIONS
  Labrasol may have potential clinical benefits in improving the ocular drug delivery of baicalin.
authors.affiliation: Research Center of Traditional Chinese Medicine, Tianjin University of Traditional Chinese Medicine, Tianjin, PR China. lonerliuzd@163.com
authors.forename: Zhidong
authors.initials: Z
authors.lastname: Liu
authors.forename: Xinhua
authors.initials: X
authors.lastname: Zhang
authors.forename: Jiawei
authors.initials: J
authors.lastname: Li
authors.forename: Rui
authors.initials: R
authors.lastname: Liu
authors.forename: Lexin
authors.initials: L
authors.lastname: Shu
authors.forename: Jun
authors.initials: J
authors.lastname: Jin
mesh_terms: D000818:Animals; D003315:Cornea / Q000187:drug effects / Q000378:metabolism*; D016503:Drug Delivery Systems / Q000379:methods*; D004347:Drug Interactions / Q000502:physiology; D005419:Flavonoids / Q000008:administration & dosage* / Q000378:metabolism; D005989:Glycerides; D009930:Organic Chemicals / Q000008:administration & dosage / Q000378:metabolism; D011817:Rabbits
chemical_list: D005419:Flavonoids; D005989:Glycerides; D009930:Organic Chemicals; C440220:Labrasol; C038044:baicalin