Enhancement of Bioavailability of Non-nucleoside Reverse Transciptase Inhibitor Using Nanosponges.

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Efavirenz, a non-nucleoside reverse transcriptase inhibitor, is crucial for HIV treatment but suffers from poor solubility and bioavailability (BCS Class II).
• Enhancing efavirenz solubility is critical for improving its therapeutic efficacy in patients.

Purpose of the Study:

• To improve the solubility, dissolution, and oral bioavailability of efavirenz using beta-cyclodextrin-based nanosponges.
• To develop and characterize efavirenz-loaded nanosponges and their complexes for enhanced drug delivery.

Main Methods:

• Preparation of beta-cyclodextrin nanosponges by crosslinking with carbonates.
• Loading efavirenz into nanosponges via solvent evaporation and characterization of binary/ternary complexes (EFA, NS, PVP K30).
• Evaluation using phase solubility, spectral analysis (FTIR, XRD, DSC, FESEM), saturation solubility, in vitro dissolution, and in vivo pharmacokinetics.

Main Results:

• Spectral analysis confirmed the formation of inclusion complexes.
• Ternary complexes exhibited a 17-fold increase in saturation solubility in distilled water and a 4-fold increase in simulated gastric fluid.
• In vitro dissolution rate improved threefold, and oral bioavailability increased twofold compared to plain efavirenz.

Conclusions:

• Beta-cyclodextrin nanosponges effectively enhance efavirenz solubility and dissolution.
• Ternary nanosponge complexes represent a promising formulation for improving the oral bioavailability of efavirenz.
• This approach offers a viable strategy for overcoming bioavailability challenges in BCS Class II drugs.