Abstract
Objectives. A major challenge faced with the manufacture of liposomes is the high volumes of organic solvents used and disposed of during manufacturing. Therefore, we have implemented an organic solvent-free production method for drug-loaded liposomes and demonstrated its applicability with both aqueous core loaded and bilayer loaded drugs.
Methods. Liposomes were produced by high-shear mixing dry powder lipids with an aqueous buffer, followed by down-sizing using a Microfluidizer® processor. Liposomes were purified via tangential flow filtration and characterised in terms of size, polydispersity, zeta potential and drug loading.
Key findings. Doxorubicin-loaded PEGylated liposomes can be manufactured using this solvent-free method with particle sizes of 100-110 nm, low PDI (<0.2) and high drug loading (97 - 98%). If required, liposomes can be further down-sized via further microfluidic processing without impacting drug loading. Similar results were achieved with non-PEGylated liposomes. With bilayer loaded amphotericin B liposomes, again liposomes can be prepared within a clinically appropriate size range (100 – 110 nm in size, low PDI) with high drug loading (98 - 100 %).
Conclusions. We apply a simple and scalable solvent-free method for the production of both aqueous core or bilayer drug loaded liposomes.
Methods. Liposomes were produced by high-shear mixing dry powder lipids with an aqueous buffer, followed by down-sizing using a Microfluidizer® processor. Liposomes were purified via tangential flow filtration and characterised in terms of size, polydispersity, zeta potential and drug loading.
Key findings. Doxorubicin-loaded PEGylated liposomes can be manufactured using this solvent-free method with particle sizes of 100-110 nm, low PDI (<0.2) and high drug loading (97 - 98%). If required, liposomes can be further down-sized via further microfluidic processing without impacting drug loading. Similar results were achieved with non-PEGylated liposomes. With bilayer loaded amphotericin B liposomes, again liposomes can be prepared within a clinically appropriate size range (100 – 110 nm in size, low PDI) with high drug loading (98 - 100 %).
Conclusions. We apply a simple and scalable solvent-free method for the production of both aqueous core or bilayer drug loaded liposomes.
Original language | English |
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Pages (from-to) | 1328-1340 |
Number of pages | 13 |
Journal | Journal of Pharmacy and Pharmacology |
Volume | 72 |
Issue number | 10 |
Early online date | 16 Jul 2020 |
DOIs | |
Publication status | Published - 1 Oct 2020 |
Keywords
- liposomes
- manufacturing
- solvent-free
- doxorubicin
- amphotericin B
- particle size
- drug loading
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Data for : "Scalable solvent-free production of liposomes"
Khadke, S. (Creator), Roces Rodriguez, C. B. (Contributor), Donaghey, R. (Contributor), Giacobbo, V. (Contributor), Su, Y. (Contributor) & Perrie, Y. (Supervisor), University of Strathclyde, 25 Feb 2020
DOI: 10.15129/fdcc9a13-f5b4-405e-bc0b-885adfb24ccb
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