Formulation Design and Evaluation of Ginsenoside Compound K Nanostructured Lipid Carriers Based on Molecular Dynamics Simulations

Abstract

Objective

Ginsenoside compound K (GCK) is a drug with various pharmacological activities and can be used to treat a wide range of diseases. However, water solubility and low membrane permeability, which reduces its permeability in the body and limits its clinical application. To overcome these drawbacks, nanostructured lipid carriers (NLCs) with optimal process prescription were prepared and evaluated in this study.

Methods

Molecular dynamics (MD) simulations were applied to screen the excipients and investigate the blend system. GCK-loaded NLCs (GCK-NLCs) were prepared by high pressure homogenization method, and the morphology was observed by transmission electron microscopy. Differential scanning calorimetry, X-raydiffraction, fourier transform infrared spectroscopy were used to investigate the presence of GCK in GCK-NLCs. The in vitro release study was performed by dialysis, and in vivo studies using in situ intestinal perfusion were investigated in rats.

Results

The prepared GCK-NLCs particles were spherical with smooth surface, particle size of about 128.3 ± 0.9 nm, PDI of 0.202 ± 0.017 and encapsulation efficiency of 92.8%. Spectral analysis showed that the drug was amorphous and was successfully encapsulated in the lipid cavity. In vitro release studies showed that GCK-NLCs exhibited high release characteristics. Single-pass intestinal perfusion experiments showed that GCK-NLCs were absorbed predominantly in the small intestine and the prepared GCK-NLCs enhanced the permeability of the drug.

Conclusion

NLCs formulation can be used as a good delivery system to enhance the solubility and permeability of GCK and provides a promising nanocarrier for the prolonged release of hydrophobic drugs.