Nevirapine-polycaprolactone crystalline inclusion complex as a potential long-acting injectable solid form.

Area of Science:

• Pharmaceutical Sciences
• Materials Science
• Biomedical Engineering

Background:

• Nevirapine (NVP) is crucial for preventing mother-to-child HIV transmission but oral administration leads to poor patient compliance.
• A long-acting injectable formulation of NVP is highly desirable to improve treatment adherence and efficacy.

Purpose of the Study:

• To develop a long-acting injectable formulation of Nevirapine (NVP) using drug-polymer inclusion complexes (IC).
• To investigate the potential of NVP-PCL IC microparticles for sustained drug delivery and improved patient compliance.

Main Methods:

• Formation of crystalline inclusion complexes (IC) between Nevirapine (NVP) and poly(ε-caprolactone) (PCL) was confirmed using single-crystal X-ray diffraction.
• Characterization of NVP-PCL IC microparticles, including solubility, dissolution rate, particle size, and injectability, was performed using spray drying and other methods.

Main Results:

• NVP-PCL IC crystals exhibited significantly reduced solubility and slower dissolution rates compared to pure NVP.
• Spray-dried NVP-PCL IC microparticles (<10 μm) were easily injectable through a 25G needle, indicating suitability for long-acting injections.
• The NVP-PCL IC formulation demonstrated potential for sustained-release profiles, outperforming NVP/polylactide microparticles.

Conclusions:

• Drug-polymer inclusion complexes (IC) offer a viable strategy for creating long-acting injectable drug formulations.
• NVP-PCL IC microparticles represent a promising new approach for sustained-release drug products, enhancing HIV prevention therapy.
• This innovative formulation could significantly improve patient compliance and therapeutic outcomes in preventing mother-to-child HIV transmission.