Preparation, characterization, and in vivo pharmacokinetic study of the supercritical fluid-processed liposomal amphotericin B

Chang Baek Lim, Sharif Md Abuzar, Pankaj Ranjan Karn, Wonkyung Cho, Hee Jun Park, Cheong Weon Cho, Sung Joo Hwang

Research output: Contribution to journalArticle

Abstract

Here, we aimed to prepare and optimize liposomal amphotericin B (AmB) while using the supercritical fluid of carbon dioxide (SCF-CO2) method and investigate the characteristics and pharmacokinetics of the SCF-CO2-processed liposomal AmB. Liposomes containing phospholipids, ascorbic acid (vit C), and cholesterol were prepared by the SCF-CO2 method at an optimized pressure and temperature; conventional liposomes were also prepared using the thin film hydration method and then compared with the SCF-CO2-processed-liposomes. The optimized formulation was evaluated by in vitro hemolysis tests on rat erythrocytes and in vivo pharmacokinetics after intravenous administration to Sprague-Dawley rats and compared with a marketed AmB micellar formulation, Fungizone®, and a liposomal formulation, AmBisome®. The results of the characterization studies demonstrated that the SCF-CO2-processed-liposomes were spherical particles with an average particle size of 137 nm (after homogenization) and drug encapsulation efficiency (EE) was about 90%. After freeze-drying, mean particle size, EE, and zeta potential were not significantly changed. The stability study of the liposomes showed that liposomal AmB that was prepared by the SCF method was stable over time. In vivo pharmacokinetics revealed that the SCF-CO2-processed-liposomes were bioequivalent to AmBisome®; the hemolytic test depicted less hematotoxicity than Fungizone®. Therefore, this method could serve as a potential alternative for preparing liposomal AmB for industrial applications.

Original languageEnglish
Article number589
JournalPharmaceutics
Volume11
Issue number11
DOIs
Publication statusPublished - 2019 Nov

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Liposomes
Pharmacokinetics
Amphotericin B
Particle Size
Freeze Drying
Hemolysis
Carbon Dioxide
Intravenous Administration
Ascorbic Acid
Sprague Dawley Rats
liposomal amphotericin B
Phospholipids
Erythrocytes
Cholesterol
Pressure
Temperature
Pharmaceutical Preparations

All Science Journal Classification (ASJC) codes

  • Pharmaceutical Science

Cite this

Lim, Chang Baek ; Abuzar, Sharif Md ; Karn, Pankaj Ranjan ; Cho, Wonkyung ; Park, Hee Jun ; Cho, Cheong Weon ; Hwang, Sung Joo. / Preparation, characterization, and in vivo pharmacokinetic study of the supercritical fluid-processed liposomal amphotericin B. In: Pharmaceutics. 2019 ; Vol. 11, No. 11.
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Preparation, characterization, and in vivo pharmacokinetic study of the supercritical fluid-processed liposomal amphotericin B. / Lim, Chang Baek; Abuzar, Sharif Md; Karn, Pankaj Ranjan; Cho, Wonkyung; Park, Hee Jun; Cho, Cheong Weon; Hwang, Sung Joo.

In: Pharmaceutics, Vol. 11, No. 11, 589, 11.2019.

Research output: Contribution to journalArticle

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AU - Karn, Pankaj Ranjan

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AU - Park, Hee Jun

AU - Cho, Cheong Weon

AU - Hwang, Sung Joo

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