A new polymer-excipient for ethanol-resistant, sustained-release oral dosage forms

Area of Science:

• Materials Science
• Pharmaceutical Sciences
• Polymer Chemistry

Background:

• Alcohol consumption can lead to uncontrolled drug release from sustained-release oral dosage forms, posing significant patient health risks.
• Existing ethanol-resistant excipient blends often require complex formulation strategies, including plasticizers, and can increase processing times.

Purpose of the Study:

• To design and synthesize a novel polymeric excipient with intrinsic ethanol resistance for sustained-release drug formulations.
• To evaluate the impact of polymer composition on ethanol resistance and drug release profiles.

Main Methods:

• Systematic design and synthesis of polymers via emulsion polymerization.
• Characterization of polymer properties, including glass transition temperature (Tg) and minimum film forming temperature (MFFT).
• In vitro drug release studies of model formulations in the presence and absence of ethanol, analyzed using Weibull regression to determine an alcohol resistance factor.

Main Results:

• Polymers with Tg between 10-18°C and MFFT between 10-25°C were successfully synthesized, suitable for aqueous film-coating.
• In vitro results demonstrated a clear structure-function relationship: nonionic hydrophilic groups enhanced ethanol resistance compared to cationic hydrophilic groups.
• The alcohol resistance factor ranged from -44±2% (reduced release in ethanol) to +34±0% (increased release in ethanol), dependent on comonomer ratio.

Conclusions:

• The developed polymeric excipients exhibit inherent ethanol resistance, effectively controlling drug release in the presence of alcohol.
• These novel excipients offer advantages over traditional blends, including ease of use, elimination of plasticizers, and reduced coating times.
• The findings support the potential of these polymers to enhance the safety and efficacy of sustained-release oral drug formulations.