title: Supercritical fluid-mediated liposomes containing cyclosporin A for the treatment of dry eye syndrome in a rabbit model: comparative study with the conventional cyclosporin A emulsion.
abstract: BACKGROUND
  The objective of this study was to compare the efficacy of cyclosporin (CsA)-encapsulated liposomes with the commercially available CsA emulsion (Restasis) for the treatment of dry eye syndrome in rabbits.
  
  
  METHODS
  Liposomes containing CsA were prepared by the supercritical fluid (SCF) method consisted of phosphatidylcholine from soybean (SCF-S100) and egg lecithins (SCF-EPCS). An in vitro permeation study was carried out using artificial cellulose membrane in Franz diffusion cells. Dry eye syndrome was induced in male albino rabbits and further subdivided into untreated, Restasis-treated, EPCS, and S100-treated groups. Tear formation in the dry-eye-induced rabbits was evaluated using the Schirmer tear test. All formulations were also evaluated by ocular irritation tests using the Draize eye and winking methods with the determination of CsA concentration in rabbit tears.
  
  
  RESULTS
  After the treatment, the Schirmer tear test value significantly improved in EPCS-treated (P=0.005) and S100-treated (P=0.018) groups compared to the Restasis-treated group. The AUC₀₋₂₄ h for rabbit's tear film after the administration of SCF-S100 was 32.75±9.21 μg·h/mg which was significantly higher than that of 24.59±8.69 μg·h/mg reported with Restasis. Liposomal CsA formulations used in this study showed lower irritation in rabbit eyes compared with Restasis.
  
  
  CONCLUSIONS
  These results demonstrate that the novel SCF-mediated liposomal CsA promises a significant improvement in overcoming the challenges associated with the treatment of dry eyes.
authors.affiliation: Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea.
authors.forename: Pankaj Ranjan
authors.initials: PR
authors.lastname: Karn
authors.affiliation: Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea ; College of Pharmacy, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea.
authors.forename: Hyun Do
authors.initials: HD
authors.lastname: Kim
authors.affiliation: Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea ; College of Pharmacy, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea.
authors.forename: Han
authors.initials: H
authors.lastname: Kang
authors.affiliation: Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea ; College of Pharmacy, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea.
authors.forename: Bo Kyung
authors.initials: BK
authors.lastname: Sun
authors.affiliation: College of Pharmacy, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea.
authors.forename: Su-Eon
authors.initials: SE
authors.lastname: Jin
authors.affiliation: Yonsei Institute of Pharmaceutical Sciences, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea ; College of Pharmacy, Yonsei University, Yeonsu-gu, Incheon, Republic of Korea.
authors.forename: Sung-Joo
authors.initials: SJ
authors.lastname: Hwang
mesh_terms: D000818:Animals; D001767:Blinking; D016572:Cyclosporine / Q000032:analysis / Q000737:chemistry* / Q000493:pharmacokinetics / Q000627:therapeutic use; D004195:Disease Models, Animal; D015352:Dry Eye Syndromes / Q000188:drug therapy*; D008081:Liposomes / Q000737:chemistry* / Q000627:therapeutic use; D008297:Male; D008954:Models, Biological; D010539:Permeability; D011817:Rabbits; D013666:Tears / Q000737:chemistry
chemical_list: D008081:Liposomes; D016572:Cyclosporine
keywords: cyclosporin A; dry eye syndrome; liposomes; supercritical fluid