Paclitaxel-Loaded β-Cyclodextrin-Modified Poly(Acrylic Acid) Nanoparticles through Multivalent Inclusion for...

Area of Science:

• Nanotechnology
• Materials Science
• Pharmacology

Background:

• Paclitaxel (PTX) is a potent anticancer drug with poor aqueous solubility.
• Developing effective drug delivery systems is crucial for enhancing PTX's therapeutic index.
• Host-guest interactions offer a promising strategy for drug encapsulation and controlled release.

Purpose of the Study:

• To develop a nanoassembled drug delivery system for paclitaxel (PTX) using β-cyclodextrin (β-CD) modified poly(acrylic acid) (PCDAA).
• To evaluate the enhanced aqueous solubility, sustained release, and in vitro/in vivo anticancer efficacy of the prepared nanoparticles.
• To investigate the tumor targeting capability and biodistribution of the novel drug delivery system.

Main Methods:

• Host-guest complexation of PTX with β-CD modified poly(acrylic acid) (PCDAA) to form PCDAA-PTX nanoparticles (NPs).
• Assessment of aqueous solubility and in vitro drug release kinetics.
• In vitro cytotoxicity assays using tumor cells.
• In vivo near-infrared fluorescence imaging for biodistribution studies.
• In vivo antitumor efficacy evaluation in H22 tumor-bearing mice.

Main Results:

• PCDAA-PTX NPs significantly increased PTX aqueous solubility from 0.34 to 36.02 μg mL(-1).
• Sustained PTX release was observed in vitro, with significant accumulation and retained pharmacological activity in tumor cells.
• In vivo imaging confirmed effective tumor targeting via the enhanced permeability and retention (EPR) effect.
• PCDAA-PTX NPs demonstrated superior tumor growth inhibition compared to commercial Taxol®.

Conclusions:

• The developed nanoassembled system effectively enhances PTX solubility and provides sustained release.
• PCDAA-PTX NPs exhibit excellent tumor targeting and accumulation, leading to improved in vivo anticancer efficacy.
• This novel nanodelivery system holds significant potential for advanced anticancer therapy.