Enhancing Efavirenz Bioavailability Via Polymer-Based Buccal Administration: Optimization and Characterization of...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Efavirenz (EFV) is a key antiretroviral for HIV/AIDS, but side effects limit its use.
• Buccal administration bypasses GI degradation and first-pass metabolism, offering improved drug delivery.
• Developing novel delivery systems is crucial for enhancing EFV efficacy and patient compliance.

Purpose of the Study:

• To design and characterize Efavirenz nanocrystals (EFV-NC) stabilized with Pluronic®F-127.
• To formulate EFV-NC into dissolving microneedles (EFV-NC-DMN) for buccal delivery.
• To evaluate the in vitro and in vivo performance of EFV-NC-DMN for HIV/AIDS management.

Main Methods:

• Molecular docking to assess EFV-polymer interactions.
• Nanocrystal preparation and characterization (particle size, PDI, zeta potential).
• Formulation of dissolving microneedles and assessment of mechanical properties and drug release kinetics.
• Ex vivo and in vivo pharmacokinetic studies to determine bioavailability.

Main Results:

• Pluronic®F-127 showed strong binding affinity to EFV.
• EFV-NC exhibited optimal particle size, PDI, and stability.
• EFV-NC-DMN demonstrated controlled release (Higuchi model) and enhanced solubility.
• In vivo studies showed a 137.40% relative bioavailability for EFV-NC-DMN compared to oral EFV.

Conclusions:

• EFV-NC-DMN is a promising buccal delivery system for enhanced HIV/AIDS therapy.
• This novel formulation improves EFV bioavailability and prolongs drug release.
• Buccal delivery via microneedles offers a superior alternative to conventional oral administration for EFV.