Incorporation of polymeric nanoparticles into solid dosage forms

Area of Science:

• Pharmaceutical Technology
• Materials Science

Background:

• Polymeric nanoparticles are increasingly utilized for oral drug delivery.
• Their successful application depends on maintaining nanoparticle integrity upon release from solid dosage forms.

Purpose of the Study:

• To investigate the compatibility of model polymeric nanoparticles with tabletting excipients.
• To assess the redispersibility of nanoparticles from various solid dosage forms (granules, tablets, pellets, films).
• To identify critical parameters influencing nanoparticle integrity after release.

Main Methods:

• Incorporation of Eudragit(R) and Aquacoat(R) nanoparticle dispersions into solid dosage forms.
• Evaluation of nanoparticle-binder interactions during wet granulation.
• Assessment of nanoparticle redispersibility and particle size post-release.
• Contact angle measurements to determine nanoparticle wettability.

Main Results:

• Phase separation occurred in many nanoparticle/binder systems during wet granulation.
• High minimum film formation temperature (MFT) and good wettability were critical for nanoparticle redispersibility.
• Low MFT led to nanoparticle coalescence and poor redispersibility.
• Contact angle correlated with redispersibility; Eudragit(R) RL showed good redispersibility with low contact angles.

Conclusions:

• Maintaining nanoparticle properties requires careful selection of polymers and excipients.
• Minimum film formation temperature (MFT) and wettability are critical parameters for successful oral nanoparticle formulation.
• Eudragit(R) RL demonstrates favorable characteristics for redispersibility in oral solid dosage forms.