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Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
Published on: August 31, 2019
Unilamellar liposomes with enhanced boron content
Tiejun Li1, Julie Hamdi, M Frederick Hawthorne
1Department of Chemistry and Biochemistry, University of California, Los Angeles, 607 Charles E. Young Drive East, Los Angeles, California 90095, USA.
Bioconjugate Chemistry
|January 19, 2006
Summary
New boron-rich liposomes were created using a novel lipid, DAC-16, eliminating the need for DSPC. These stable, small liposomes offer high boron content for in vitro applications.
Area of Science:
- Lipid nanoparticle formulation
- Boron neutron capture therapy (BNCT) delivery systems
- Materials science
Background:
- Conventional liposomes often require specific lipids like DSPC for stability.
- Achieving high boron concentration in liposomes for therapeutic applications is challenging.
- The development of novel lipids is crucial for advancing drug delivery systems.
Purpose of the Study:
- To develop novel boron-rich liposomes using a new ionic nido-carborane lipid (DAC-16).
- To assess the stability and physical characteristics of these DSPC-free liposomes.
- To evaluate the potential of DAC-16 liposomes for in vitro boron delivery applications.
Main Methods:
- Synthesis and characterization of the novel ionic nido-carborane lipid, K[nido-7-(C16H33OCH2)2CHOCH2-7,8-C2B9H11] (DAC-16).
- Formation of unilamellar liposomes using DAC-16 and cholesterol, without DSPC.
- Analysis of liposome size distribution, boron concentration, and bilayer incorporation efficiency.
- Assessment of liposome stability under various storage conditions (temperature, time).
Main Results:
- Stable, unilamellar liposomes were successfully formed using DAC-16 and cholesterol, without DSPC.
- DSPC-free DAC-16 liposomes achieved a high boron concentration (approx. 8.8 wt %) with 98% bilayer incorporation efficiency.
- Liposomes exhibited a desirable size distribution (40-60 nm) for potential tumor uptake and maintained stability for months.
- Optimized formulations with DAC-16, DSPC, and cholesterol also showed long-term storage stability.
Conclusions:
- The novel ionic nido-carborane lipid DAC-16 enables the creation of highly boronated liposomes without DSPC.
- These DSPC-free liposomes possess favorable characteristics for in vitro boron delivery.
- While animal studies suggest toxicity, DAC-16 liposomes represent a promising platform for specific in vitro research applications requiring high boron payloads.
