Lipid Based Aqueous Core Nanocapsules (ACNs) for Encapsulating Hydrophillic Vinorelbine Bitartrate: Preparation,...

Area of Science:

• Nanotechnology
• Drug Delivery Systems
• Oncology

Background:

• Vinorelbine bitartrate (VRL) is an FDA-approved antimitotic agent for breast cancer and NSCLC.
• High aqueous solubility and thermal instability of VRL limit its available dosage forms.

Purpose of the Study:

• Develop lipid-based aqueous core nanocapsules (ACNs) for hydrophilic VRL encapsulation.
• Achieve sustained release of VRL using a lipidic shell.
• Optimize ACN formulation for enhanced drug delivery.

Main Methods:

• Prepared ACNs via double emulsification and solvent evaporation.
• Employed Box Behnken Design for formulation optimization.
• Characterized ACNs for particle size, PDI, zeta potential, encapsulation efficiency, morphology (TEM), and in vitro release.
• Assessed safety via in vitro haemocompatibility studies.

Main Results:

• Optimized ACNs achieved up to 78% VRL entrapment efficiency.
• TEM confirmed spherical ACNs with a core-shell structure.
• In vitro release followed Korsemeyer-Peppas kinetics, indicating Fickian diffusion.
• Haemocompatibility studies demonstrated safety for intravenous administration.

Conclusions:

• ACNs are a promising platform for encapsulating highly aqueous-soluble anticancer drugs like VRL.
• The developed nanocapsules offer enhanced entrapment and safety for intravenous delivery.
• This approach addresses limitations of VRL solubility and stability, improving therapeutic potential.