DSPC:Chol liposomes are vesicles composed of distearoylphosphatidylcholine (DSPC) and cholesterol. This composition provides a balance between fluidity and rigidity, enhancing the stability of the liposomes in biological environments.
The inclusion of cholesterol enhances the structural integrity of these liposomes, making them less permeable and more stable in the bloodstream. This helps in maintaining the encapsulated drug's integrity until it reaches the target site, making these liposomes effective for controlled drug release.
These liposomes are widely used in the delivery of chemotherapeutic agents and other therapeutic molecules, especially where prolonged circulation time and targeted delivery are crucial. They are also used in the study of lipid-based drug delivery mechanisms.
Key considerations include ensuring the correct molar ratio of DSPC to cholesterol for optimal vesicle formation, particle size control, and achieving high encapsulation efficiency. The preparation method must also ensure that the liposomes are sterile and free from extraneous particles.
Yes, these liposomes can encapsulate both types of drugs. DSPC provides a stable bilayer matrix suitable for incorporating hydrophobic drugs within the membrane, while hydrophilic drugs can be encapsulated within the aqueous core of the vesicles.
Percent of injected dose for cisplatin (a), lipid (b) and percent initial cisplatin/lipid ratio (c) in plasma following i.v. administration of cisplatin-containing liposomes into BDF-1 mice
This research investigates the optimization of liposomal cisplatin formulations to enhance therapeutic efficacy by manipulating the membrane composition, specifically focusing on the use of DSPC:Chol (55:45) liposomes. The study addresses the challenge in clinical applications where efficient drug delivery does not translate into increased therapeutic effectiveness, potentially due to inadequate drug release at the tumor site. By altering the lipid composition in the liposomes, particularly the ratios of DSPC, DPPC, and DSPG, researchers aimed to control the fluidity of the membrane, which in turn affects the drug's release rate and plasma half-life.
The study found that liposomes with a high phase transition temperature (Tm) retained drugs longer but showed minimal anti-tumor activity due to limited drug release. Conversely, liposomes with a low Tm released drugs too quickly, reducing drug availability at the tumor site and also resulting in lower anti-tumor activity. The formulation that balanced these extremes-DSPC:DPPC:DSPG:Chol (35:35:20:10)-exhibited an intermediate drug release rate and achieved the highest therapeutic effectiveness in a murine leukemia model. This formulation demonstrated that a critical balance in drug release kinetics is essential for optimizing liposomal formulations for cancer therapy, highlighting the significant role of membrane composition in the design of effective drug delivery systems.
Zisman, N., Dos Santos, N., et al. Optimizing liposomal cisplatin efficacy through membrane composition manipulations. Chemotherapy Research and Practice. 2011, 2011.
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