Ginsenoside CK-loaded self-nanomicellizing solid dispersion with enhanced solubility and oral bioavailability

Area of Science:

• Pharmacology
• Drug Delivery
• Nanotechnology

Background:

• Ginsenoside compound K (CK), a protopanaxadiol metabolite, offers cardioprotective and antidiabetic effects.
• CK's therapeutic use is limited by poor solubility and low oral bioavailability (BA).
• Developing advanced delivery systems is crucial for enhancing CK's clinical efficacy.

Purpose of the Study:

• To prepare a self-nanomicellizing solid dispersion (SSD) of CK.
• To enhance CK's dissolution and oral BA.
• To evaluate CK-SSD's efficacy in managing arrhythmia.

Main Methods:

• Formulation of CK-SSD using self-nanomicellizing technology.
• Characterization via DSC, XRD, FTIR, and SEM.
• Pharmacokinetic analysis using UPLC-MS/MS.
• Arrhythmia assessment using Mapping Lab on perfused hearts.

Main Results:

• CK-SSD8 exhibited a 130-fold increase in solubility compared to free CK.
• CK-SSD particles were <100 nm, indicating successful nanomicellization.
• Oral administration of CK-SSD8 resulted in a 2.02-fold higher AUC(0-24) than pure CK.
• CK-SSD treatment significantly reduced ventricular rate and conduction velocity in arrhythmia models.

Conclusions:

• CK-SSD system effectively enhances CK solubility and oral bioavailability.
• The developed CK-SSD formulation demonstrates significant therapeutic potential for arrhythmia management.
• CK-SSD represents a promising carrier for improving the clinical application of ginsenoside compound K.