Microsphere Formulation for NAD+ Bioavailability
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Solution Overview
Problem
Current methods for increasing NAD+ levels are inefficient due to the degradation of exogenously supplemented NMN by CD38, a multi-functional enzyme that metabolizes NAD+ and its precursors, leading to reduced bioavailability and utilization.
Innovation Solution
A microsphere formulation where a CD38 inhibitor, such as quercetin or apigenin, is rapidly released followed by the controlled release of NMN, optimizing the inhibition of CD38 and enhancing the bioavailability of NMN, thereby increasing NAD+ levels efficiently.
Engineering Contradictions & Design Principles
Engineering Contradiction Analysis
1Quantity of substance
If NMN is supplemented to increase NAD+ levels, then NAD+ synthesis is enhanced, but NMN is degraded by CD38 enzyme reducing bioavailability
Solution Approach 1:
The patent applies preliminary action by first inhibiting CD38 enzyme activity before NMN supplementation. The composition includes CD38 inhibitors that are administered concurrently or prior to NMN, preventing the enzyme from degrading NMN before it can be converted to NAD+. This temporal sequencing of actions - first blocking the degradation pathway, then providing the substrate - resolves the contradiction by ensuring NMN bioavailability is maintained while still achieving NAD+ level enhancement
Solution Approach 2:
The patent uses CD38 inhibitors as intermediary substances that mediate between NMN supplementation and NAD+ production. The inhibitor acts as a protective intermediary that blocks the harmful interaction between CD38 and NMN, allowing NMN to reach its intended destination and function without being degraded. This intermediary mechanism preserves NMN while still enabling the desired NAD+ synthesis pathway
2Quantity of substance
If CD38 inhibitor and NMN are co-administered, then NAD+ level increases, but incubation time is required for CD38 inhibition reducing efficiency
Solution Approach 1:
The patent achieves continuity of useful action by formulating CD38 inhibitors and NMN together in a single composition that maintains effective concentrations of both components over time. The formulation ensures continuous CD38 inhibition and sustained NMN availability without requiring separate incubation periods, allowing the therapeutic effect to begin immediately upon administration and continue efficiently
Solution Approach 2:
The patent merges the administration of CD38 inhibitors and NMN into a single combined composition rather than requiring separate administration steps. This merging eliminates the need for sequential incubation periods and allows both components to work synergistically from the moment of administration, significantly reducing the total time required to achieve NAD+ level enhancement
Data Source
AI summary
The present disclosure provides a method for improving bioavailability of an NAD+ derivative. The method improves the bioavailability of the NAD+derivative by arranging a CD38 inhibitor and the NAD+ derivative in a same preparation, and controlling the CD38 inhibitor to release first rapidly, and then the NAD+ derivative releases after the CD38 inhibitor has taken effect, thereby increasing the level of NAD+ in vivo.