Exploring stabilizing agents to prevent crystal growth or aggregation in PTX-NCs generated via diverse...

Area of Science:

• Materials Science
• Pharmaceutical Technology
• Nanotechnology

Background:

• Paclitaxel (PTX) is a poorly water-soluble anticancer drug.
• Developing effective delivery systems for hydrophobic drugs like PTX is crucial for therapeutic efficacy.
• Nanocrystal technology offers a promising approach to enhance the solubility and bioavailability of poorly soluble drugs.

Purpose of the Study:

• To prepare paclitaxel nanocrystals (PTX-NCs) as a delivery platform for poorly water-soluble paclitaxel.
• To compare the melt-based precipitation (MBP) method with ultrasonication followed by freeze-drying for PTX-NC preparation.
• To evaluate the effectiveness of various biocompatible polymer stabilizers in PTX-NC formulation.

Main Methods:

• Formulation of paclitaxel nanosuspensions using two techniques: ultrasonication/freeze-drying and melt-based precipitation (MBP).
• Utilized biocompatible polymers including polyethylene glycol (PEG) derivatives, Pluronic F-68, and myrj 52 as stabilizers.
• Characterization of nanocrystal size, morphology, physical stability, dissolution enhancement, and chemical stability over six months.

Main Results:

• The MBP method using PEG derivatives yielded superior PTX-NCs compared to the ultrasonication method.
• Pluronic F-68 and myrj 52 demonstrated high efficiency in preventing particle growth and agglomeration.
• Optimized formulations produced stable, re-dispersible spherical nanocrystals (approx. 74 nm) with enhanced drug dissolution and chemical stability.

Conclusions:

• The melt-based precipitation (MBP) method is a promising, cost-effective, and efficient technique for producing stable paclitaxel nanocrystals (PTX-NCs).
• Biocompatible polymers like PEG derivatives, Pluronic F-68, and myrj 52 are effective stabilizers for PTX-NCs.
• This approach avoids expensive and time-consuming freeze-drying steps, offering a viable strategy for poorly soluble drug nanocrystal development.