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Microfluidic Post-Insertion Method for the Efficient Preparation of PEGylated Liposomes Using High Functionality and
Yuri Sugimoto1,2, Tadaharu Suga1, Naoya Kato1
1Department of Pharmaceutical Informatics, Graduate School of Biomedical Sciences, Nagasaki University, Nagasaki, Japan.
International Journal of Nanomedicine
|January 4, 2023
Summary
A novel microfluidic post-insertion method enables large-scale preparation of targeted liposomes. This technique maintains liposome quality and achieves cellular association comparable to conventional methods, paving the way for clinical applications.
Area of Science:
- Biotechnology
- Nanotechnology
- Drug Delivery
Background:
- Targeted liposomes utilize ligand peptides for precise therapeutic agent delivery.
- The conventional post-insertion method for liposome modification faces challenges in large-scale clinical applications due to altered physicochemical properties.
- Developing scalable and reproducible methods for targeted liposome preparation is crucial for clinical translation.
Purpose of the Study:
- To develop and optimize a novel microfluidic post-insertion method for large-scale preparation of ligand-peptide-modified liposomes.
- To evaluate the physicochemical properties and cellular association of liposomes prepared using the microfluidic method.
- To compare the efficacy of the microfluidic method with the conventional post-insertion technique for targeted liposome preparation.
Main Methods:
- Utilized integrin αvβ3-targeted GRGDS (RGD) and cyclic RGDfK (cRGD)-modified high functionality and quality (HFQ) lipids.
- Optimized microfluidic device conditions, specifically total flow rate, for modifying polyethylene glycol (PEG)-modified (PEGylated) liposomes.
- Assessed liposome particle size and polydispersity index at varying flow rates (1, 6, and 12 mL/min).
- Evaluated cellular association properties using integrin αvβ3-expressing colon 26 murine colorectal carcinoma cells.
Main Results:
- Microfluidic post-insertion of RGD-HFQ lipid into PEGylated liposomes showed no significant change in particle size with increasing total flow rate.
- The polydispersity index increased with higher total flow rates.
- Liposomes modified at a total flow rate of 1 mL/min demonstrated cellular association properties equivalent to those prepared via the conventional post-insertion method.
- The microfluidic method successfully produced RGD- and cRGD-modified PEGylated liposomes.
Conclusions:
- The microfluidic post-insertion method is a viable technique for the large-scale preparation of targeted liposomes.
- This method maintains desirable physicochemical properties and achieves effective cellular targeting.
- The microfluidic approach holds promise for the clinical application of ligand-peptide-modified liposomes.
