Technology Behind
While bioavailability is vital, true clinical impact requires targeted delivery — reaching the heart cells where nutrients are most needed. CardioDrone® is a peptide-based smart targeting system, specifically designed to guide bioactives to cardiomyocytes, especially under stress or injury.
Cardiac Targeting Peptides (CTPs): Selectively bind to NPR-A receptors expressed on healthy and failing cardiac cells, anchoring nutrients precisely where needed.
Cardiac Penetrating Peptides (CPPs): Interact with heparan sulfate proteoglycans (HSPGs) to initiate endocytosis, enabling deep intracellular transport to mitochondria and the nucleus.
RGD Peptides: Target integrins αvβ3, α5β1, and α7β1, which are upregulated in ischemic or inflamed tissues, enhancing delivery to damaged zones and minimizing systemic dispersion.
Key Challenges
Systemic Dilution: Conventional delivery methods lead to nutrient dispersion across multiple organs.
Limited Cardiac Tissue Targeting: Less than 5% of nutrients reaching cardiac tissues.
Low Cellular Uptake: Many nutrients fail to penetrate cardiac cells or reach critical intracellular targets, such as mitochondria.
Poor Bioavailability: Nutrient degradation in the GIT tract significantly reduces systemic absorption.
Cardiac Peptides (CP):
-
-
- Cardiac Penetrating Peptides (CPP): Facilitate penetration into cardiac cells by interacting with membrane components (heparan sulfate proteoglycans (HSPGs)), enhancing intracellular delivery of active agents.
- Cardiac Targeting Peptides (CTP): Bind specifically to cardiac cell receptors (NPR-A), ensuring selective retention in myocardial tissues.
-
RGD Ligand
Highly specific ligands for targeting for αvβ3, α5β1, and α7β1 integrins on ischemic/ infarcted cells this feature increases local efficacy of CoQ10.
Mechanism of Action
CardioDrone® operates through a series of precise mechanisms that optimize the delivery and efficacy of payloads:
- Specific Binding: CPP and CTP ligands bind to cardiac-specific receptors, enabling selective targeting and adherence to myocardial cells.
- Efficient Uptake: Ligand-receptor interactions enhance internalization of active agents into cardiac cells.
- Optimized Retention: These ligands ensure that therapeutic agents remain localized to cardiac tissues, reducing systemic waste and maximizing efficacy.
Tissue Specificity
Nutrients are concentrated in the heart, minimizing systemic distribution and waste.
Cellular Uptake
Ligand-receptor binding facilitates efficient internalization into cardiac cells.
Maximized Bioavailability
Protects therapeutic agents from degradation, ensuring improved systemic absorption and efficacy.
Pharmacokinetics
Biodistribution of Cardiotrition® with CardioDrone® Technology
Cardiotrition®’s pharmacokinetics have been comprehensively studied using a CardioDrone dual-ligand technology comprising Cardiac Peptides (CPs) — specifically CPP (Cardiac Penetrating Peptide) and CTP (Cardiac Targeting Peptide) — combined with RGD Peptides for enhanced targeting.
Key Assays
Biodistribution Study:
- Analyzed drug concentration across tissues (heart, liver, spleen, lung, kidney, and brain) at 1 hour and 24 hours post-administration.
- Focused on cardiac targeting efficiency and systemic distribution.
Cellular Uptake Assay:
- Evaluated the percentage of cellular uptake of CardioDrone® CoQ10 by cardiomyocytes at 4-, 24-, and 48-hours post-administration.
- Measured the ability of the formulation to penetrate cardiac cells effectively.
No chart data available for this technology.