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

Pankaj Ranjan Karn, Hyun Do Kim, Han Kang, Bo Kyung Sun, Su Eon Jin, Sung Joo Hwang

Research output: Contribution to journalArticle

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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-eyeinduced 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{dot operator}h/mg which was significantly higher than that of 24.59±8.69 μg{dot operator}h/mg reported with Restasis®. Liposomal CsA formulations used in this study showed lower irritation in rabbit eyes compared with Restasis®. Conclusion: 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.

Original languageEnglish
Pages (from-to)3791-3800
Number of pages10
JournalInternational journal of nanomedicine
Volume9
Issue number1
DOIs
Publication statusPublished - 2014 Aug 8

Fingerprint

Dry Eye Syndromes
Supercritical fluids
Liposomes
Emulsions
Cyclosporine
Tears
Rabbits
Lecithin
Therapeutics
Lecithins
Artificial Membranes
Blinking
Phosphatidylcholines
Permeation
Cellulose
Soybeans
Ovum
Membranes

All Science Journal Classification (ASJC) codes

  • Biophysics
  • Bioengineering
  • Biomaterials
  • Pharmaceutical Science
  • Drug Discovery
  • Organic Chemistry

Cite this

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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{\circledR}) 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{\circledR}-treated, EPCS, and S100-treated groups. Tear formation in the dry-eyeinduced 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{\circledR}-treated group. The AUC0-24 h for rabbit's tear film after the administration of SCF-S100 was 32.75±9.21 μg{dot operator}h/mg which was significantly higher than that of 24.59±8.69 μg{dot operator}h/mg reported with Restasis{\circledR}. Liposomal CsA formulations used in this study showed lower irritation in rabbit eyes compared with Restasis{\circledR}. Conclusion: 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.",
author = "Karn, {Pankaj Ranjan} and {Do Kim}, Hyun and Han Kang and Sun, {Bo Kyung} and Jin, {Su Eon} and Hwang, {Sung Joo}",
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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. / Karn, Pankaj Ranjan; Do Kim, Hyun; Kang, Han; Sun, Bo Kyung; Jin, Su Eon; Hwang, Sung Joo.

In: International journal of nanomedicine, Vol. 9, No. 1, 08.08.2014, p. 3791-3800.

Research output: Contribution to journalArticle

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T1 - Supercritical fluid-mediated liposomes containing cyclosporin A for the treatment of dry eye syndrome in a rabbit model

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N2 - 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-eyeinduced 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{dot operator}h/mg which was significantly higher than that of 24.59±8.69 μg{dot operator}h/mg reported with Restasis®. Liposomal CsA formulations used in this study showed lower irritation in rabbit eyes compared with Restasis®. Conclusion: 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.

AB - 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-eyeinduced 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{dot operator}h/mg which was significantly higher than that of 24.59±8.69 μg{dot operator}h/mg reported with Restasis®. Liposomal CsA formulations used in this study showed lower irritation in rabbit eyes compared with Restasis®. Conclusion: 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.

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