Liposomal delivery of NR shows increased bioavailability

Intravenous administration of Liposomal NR demonstrated enhanced brain absorption compared to standard NR in a recent study.

“Intravenous administration of NR liposomes led to a 2.76-fold higher plasma NR concentration.”

Key Points:

Compared to conventional NR solution, Liposomal NR:

  • Increased plasma NR 2.76x after administration
  • Increased NR in healthy mouse brain 2.93x
  • Improved outcomes in mice with reduced blood flow to brain tissue

Study Evaluated Brain Concentration of Liposomal NR Compared To Non-Liposomal Form

Healthy mice or mice with reduced blood flow to their brain were divided into groups:

  • Vehicle-only (control)
  • Liposomal NR
  • Non-liposomal NR

Solutions were injected into the tail vein (40 mg/kg) in healthy mice and in mice after blood flow impairment.

Liposomal Delivery Enhanced NR in Plasma and Brain

Compared with standard formulations, administration of Liposomal NR led to almost 3 times more NR in circulation (2.76x) and in brain tissue (2.93x) at peak concentrations.

The Liposomal NR solution increased NR concentration in brain tissue most dramatically versus other tissue types.

“Liposome-based NR loading is an effective strategy for improving the pharmacokinetics and bioavailability of NR, especially to the brain.”

This figure shows the levels of NR in the brains of the mice.

Mice injected with Liposomal NR (blue line) show higher and longer-lasting levels of NR in the brain compared to mice injected with the standard NR formulation (red line).

Liposomal NR Improved Brain Metabolism After Impaired Blood Flow

“The main biological activity of NR is to enhance NAD+ generation, which potentiates mitochondrial ATP generation.”

Untreated mice showed low NAD+ and ATP levels after reduced blood flow.

However, the mice in the liposomal group experienced notably increased NAD+ and ATP production.

“Significant elevations in both NAD+ and ATP levels were induced by NRC liposomes at the observed time points compared with the NRC solution group.”

Liposomal NR Improved Recovery in Mice with Reduced Blood Flow

Mice in the Liposomal NR group showed the greatest improvement after reduced blood flow events, including:

  • Reduced weight loss
  • Improved behavioral recovery
  • Less damage to brain tissue

“We show that a lower dosage of NR can reduce infarct volume through using NR liposomes.”

Liposomal delivery systems increase bioavailability of the encased molecule, bypassing digestion and entering into circulation where the active molecule can be released directly into cells.

“Systemic improvements in health conditions were reflected after NR treatments, especially by treatment with the liposome form.”

Conclusion

Utilizing Liposomal NR enhances brain tissue concentrations of NR, stimulating production of NAD+ and ATP, due to increased uptake in the brain.

“By increasing drug distribution in the brain, NR liposomes significantly increased NAD+ in the ischemic hemisphere, which stimulates energy production and improves mitochondrial function.”

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