Please use this identifier to cite or link to this item:
Title: Lyophilization of cholesterol-free PEGylated liposomes and its impact on drug loading by passive equilibration
Authors: Chaudhury, A.
Das, S.
Lee, R.F.S.
Tan, K.-B.
Ng, W.-K. 
Tan, R.B.H. 
Chiu, G.N.C. 
Keywords: Carboplatin
Cholesterol free PEGylated liposomes
Passive equilibration
Issue Date: 1-Jul-2012
Citation: Chaudhury, A., Das, S., Lee, R.F.S., Tan, K.-B., Ng, W.-K., Tan, R.B.H., Chiu, G.N.C. (2012-07-01). Lyophilization of cholesterol-free PEGylated liposomes and its impact on drug loading by passive equilibration. International Journal of Pharmaceutics 430 (1-2) : 167-175. ScholarBank@NUS Repository.
Abstract: The obstacles in translating liposome formulations into marketable products could be attributed to their physical instabilities upon long-term storage as aqueous dispersions. Lyophilization is the most commonly used technique to improve physical stability of liposomes. The development of stable, lyophilized liposomes is focused primarily on the cholesterol-containing liposomes or pure phosphatidylcholine-based liposomes, with minimal studies on cholesterol-free, pegylated (CF-PEG) liposomes which have emerged as an important class of liposome drug carriers. Hence, it is our interest to investigate the effect of lyophilization on CF-PEG liposomes, and specifically, on drug loading via the passive equilibration method. Three different sugar cryoprotectants were used at two different sugar-to-lipid molar ratios (S/L). Our results demonstrated that CF-PEG liposomes lyophilized with sucrose at S/L = 5:1 yielded the best cryoprotective effect, as characterized by size, polydispersity indices, and microscopic examination upon liposome reconstitution. The lyophilized liposomes had low water content of 2.59 ± 0.18%. Of note, lyophilized CF-PEG liposomes exhibited two-fold increase in drug content when carboplatin was loaded via the passive equilibration method, and the in vitro drug release profile of these liposomes were not different from that of the non-lyophilized counterparts. Taken together, we envisioned that a stable, lyophilized empty CF-PEG liposome system could be coupled to hydrophilic drug loading via the passive equilibration method to produce a liposomal drug kit product. © 2012 Elsevier B.V. All rights reserved.
Source Title: International Journal of Pharmaceutics
ISSN: 03785173
DOI: 10.1016/j.ijpharm.2012.04.036
Appears in Collections:Staff Publications

Show full item record
Files in This Item:
There are no files associated with this item.


checked on May 9, 2022


checked on May 9, 2022

Page view(s)

checked on May 12, 2022

Google ScholarTM



Items in DSpace are protected by copyright, with all rights reserved, unless otherwise indicated.