Preparation and evaluation of cyclosporine A-containing proliposomes: A comparison of the supercritical antisolvent process with the conventional film method

Pankaj Ranjan Karn, Su Eon Jin, Benjamin Joon Lee, Bo Kyung Sun, Min Soo Kim, Jong Hyuk Sung, Sung Joo Hwang

Research output: Contribution to journalArticle

20 Citations (Scopus)

Abstract

Objectives: The objectives of this study were to prepare cyclosporin A (CsA)-containing proliposomes using the supercritical antisolvent (SAS) process and the conventional thin film method for the comparative study of proliposomal formulations and to evaluate the physicochemical properties of these proliposomes.

Methods: CsA-containing proliposomes were prepared by the SAS process and the conventional film method, composed of natural and synthetic phospholipids. We investigated particle size, polydispersity index, and zeta potential of CsA-containing proliposomes. In addition, both production yield and entrapment efficiency of CsA in different proliposomes were analyzed. Physicochemical properties of CsA-containing proliposomes were also evaluated, using differential scanning calorimetry and X-ray diffraction. The morphology and size of CsA-containing proliposomes were confirmed, using scanning electron microscopy. We checked the in vitro release of CsA from CsA-containing proliposomes prepared by different preparation methods, comparing them with Restasis® as a positive control and the stability of SAS-mediated proliposomes was also studied.

Results: CsA-containing proliposomes formed by the SAS process had a relatively smaller particle size, with a narrow size distribution and spherical particles compared with those of conventionally prepared proliposomes. The yield and entrapment efficiency of CsA in all proliposomes varied from 85% to 92% and from 86% to 89%, respectively. Differential scanning calorimetry and X-ray diffraction studies revealed that the anhydrous lactose powder used in this formulation retained its crystalline form and that CsA was present in an amorphous form. Proliposome powders were rapidly converted to liposomes on contact with water. The in vitro release study of proliposomal formulations demonstrated a similar pattern to Restasis®. The SAS-mediated CsA-containing proliposomes were stable on storage, with no significant changes in particle size, polydispersity index, and entrapment efficiency.

Conclusion: These results show promising features of CsA-containing proliposomal formulations, using the SAS process for the large-scale industrial application.

Original languageEnglish
Pages (from-to)5079-5091
Number of pages13
JournalInternational journal of nanomedicine
Volume9
Issue number1
DOIs
Publication statusPublished - 2014 Nov 3

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Cyclosporine
Particle size
Polydispersity
Differential scanning calorimetry
Powders
X ray diffraction
Liposomes
Phospholipids
Zeta potential
Industrial applications
Crystalline materials
Particle Size
Thin films
Scanning electron microscopy
Differential Scanning Calorimetry
X-Ray Diffraction
Water
Lactose
Electron Scanning Microscopy

All Science Journal Classification (ASJC) codes

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

Cite this

@article{d77dfabcdc71434a9b5113f61a43a202,
title = "Preparation and evaluation of cyclosporine A-containing proliposomes: A comparison of the supercritical antisolvent process with the conventional film method",
abstract = "Objectives: The objectives of this study were to prepare cyclosporin A (CsA)-containing proliposomes using the supercritical antisolvent (SAS) process and the conventional thin film method for the comparative study of proliposomal formulations and to evaluate the physicochemical properties of these proliposomes.Methods: CsA-containing proliposomes were prepared by the SAS process and the conventional film method, composed of natural and synthetic phospholipids. We investigated particle size, polydispersity index, and zeta potential of CsA-containing proliposomes. In addition, both production yield and entrapment efficiency of CsA in different proliposomes were analyzed. Physicochemical properties of CsA-containing proliposomes were also evaluated, using differential scanning calorimetry and X-ray diffraction. The morphology and size of CsA-containing proliposomes were confirmed, using scanning electron microscopy. We checked the in vitro release of CsA from CsA-containing proliposomes prepared by different preparation methods, comparing them with Restasis{\circledR} as a positive control and the stability of SAS-mediated proliposomes was also studied.Results: CsA-containing proliposomes formed by the SAS process had a relatively smaller particle size, with a narrow size distribution and spherical particles compared with those of conventionally prepared proliposomes. The yield and entrapment efficiency of CsA in all proliposomes varied from 85{\%} to 92{\%} and from 86{\%} to 89{\%}, respectively. Differential scanning calorimetry and X-ray diffraction studies revealed that the anhydrous lactose powder used in this formulation retained its crystalline form and that CsA was present in an amorphous form. Proliposome powders were rapidly converted to liposomes on contact with water. The in vitro release study of proliposomal formulations demonstrated a similar pattern to Restasis{\circledR}. The SAS-mediated CsA-containing proliposomes were stable on storage, with no significant changes in particle size, polydispersity index, and entrapment efficiency.Conclusion: These results show promising features of CsA-containing proliposomal formulations, using the SAS process for the large-scale industrial application.",
author = "Karn, {Pankaj Ranjan} and Jin, {Su Eon} and Lee, {Benjamin Joon} and Sun, {Bo Kyung} and Kim, {Min Soo} and Sung, {Jong Hyuk} and Hwang, {Sung Joo}",
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Preparation and evaluation of cyclosporine A-containing proliposomes : A comparison of the supercritical antisolvent process with the conventional film method. / Karn, Pankaj Ranjan; Jin, Su Eon; Lee, Benjamin Joon; Sun, Bo Kyung; Kim, Min Soo; Sung, Jong Hyuk; Hwang, Sung Joo.

In: International journal of nanomedicine, Vol. 9, No. 1, 03.11.2014, p. 5079-5091.

Research output: Contribution to journalArticle

TY - JOUR

T1 - Preparation and evaluation of cyclosporine A-containing proliposomes

T2 - A comparison of the supercritical antisolvent process with the conventional film method

AU - Karn, Pankaj Ranjan

AU - Jin, Su Eon

AU - Lee, Benjamin Joon

AU - Sun, Bo Kyung

AU - Kim, Min Soo

AU - Sung, Jong Hyuk

AU - Hwang, Sung Joo

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N2 - Objectives: The objectives of this study were to prepare cyclosporin A (CsA)-containing proliposomes using the supercritical antisolvent (SAS) process and the conventional thin film method for the comparative study of proliposomal formulations and to evaluate the physicochemical properties of these proliposomes.Methods: CsA-containing proliposomes were prepared by the SAS process and the conventional film method, composed of natural and synthetic phospholipids. We investigated particle size, polydispersity index, and zeta potential of CsA-containing proliposomes. In addition, both production yield and entrapment efficiency of CsA in different proliposomes were analyzed. Physicochemical properties of CsA-containing proliposomes were also evaluated, using differential scanning calorimetry and X-ray diffraction. The morphology and size of CsA-containing proliposomes were confirmed, using scanning electron microscopy. We checked the in vitro release of CsA from CsA-containing proliposomes prepared by different preparation methods, comparing them with Restasis® as a positive control and the stability of SAS-mediated proliposomes was also studied.Results: CsA-containing proliposomes formed by the SAS process had a relatively smaller particle size, with a narrow size distribution and spherical particles compared with those of conventionally prepared proliposomes. The yield and entrapment efficiency of CsA in all proliposomes varied from 85% to 92% and from 86% to 89%, respectively. Differential scanning calorimetry and X-ray diffraction studies revealed that the anhydrous lactose powder used in this formulation retained its crystalline form and that CsA was present in an amorphous form. Proliposome powders were rapidly converted to liposomes on contact with water. The in vitro release study of proliposomal formulations demonstrated a similar pattern to Restasis®. The SAS-mediated CsA-containing proliposomes were stable on storage, with no significant changes in particle size, polydispersity index, and entrapment efficiency.Conclusion: These results show promising features of CsA-containing proliposomal formulations, using the SAS process for the large-scale industrial application.

AB - Objectives: The objectives of this study were to prepare cyclosporin A (CsA)-containing proliposomes using the supercritical antisolvent (SAS) process and the conventional thin film method for the comparative study of proliposomal formulations and to evaluate the physicochemical properties of these proliposomes.Methods: CsA-containing proliposomes were prepared by the SAS process and the conventional film method, composed of natural and synthetic phospholipids. We investigated particle size, polydispersity index, and zeta potential of CsA-containing proliposomes. In addition, both production yield and entrapment efficiency of CsA in different proliposomes were analyzed. Physicochemical properties of CsA-containing proliposomes were also evaluated, using differential scanning calorimetry and X-ray diffraction. The morphology and size of CsA-containing proliposomes were confirmed, using scanning electron microscopy. We checked the in vitro release of CsA from CsA-containing proliposomes prepared by different preparation methods, comparing them with Restasis® as a positive control and the stability of SAS-mediated proliposomes was also studied.Results: CsA-containing proliposomes formed by the SAS process had a relatively smaller particle size, with a narrow size distribution and spherical particles compared with those of conventionally prepared proliposomes. The yield and entrapment efficiency of CsA in all proliposomes varied from 85% to 92% and from 86% to 89%, respectively. Differential scanning calorimetry and X-ray diffraction studies revealed that the anhydrous lactose powder used in this formulation retained its crystalline form and that CsA was present in an amorphous form. Proliposome powders were rapidly converted to liposomes on contact with water. The in vitro release study of proliposomal formulations demonstrated a similar pattern to Restasis®. The SAS-mediated CsA-containing proliposomes were stable on storage, with no significant changes in particle size, polydispersity index, and entrapment efficiency.Conclusion: These results show promising features of CsA-containing proliposomal formulations, using the SAS process for the large-scale industrial application.

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