Development and Characterization of Olaparib-Loaded Solid Self-Nanoemulsifying Drug Delivery System (S-SNEDDS) for...

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Olaparib, a BCS class IV drug, suffers from poor solubility and bioavailability.
• Effective oral delivery of such drugs requires advanced formulation strategies.

Purpose of the Study:

• To enhance Olaparib's solubility and oral bioavailability using a solid self-nanoemulsifying drug delivery system (S-SNEDDS).
• To evaluate the physicochemical properties, stability, and in vitro performance of the developed S-SNEDDS formulation.

Main Methods:

• Self-nanoemulsifying drug delivery system (SNEDDS) formulations were prepared using Capmul MCM, Tween 80, and PEG 400.
• Optimal SNEDDS formulation (OLS-352) was solidified using spray drying with Aerosil® 200 and PVP K30 as carriers.
• Physicochemical characterization, drug content, stability studies, dissolution testing, and Caco-2 cell permeability assays were performed.

Main Results:

• The optimal SNEDDS formulation (OLS-352) exhibited a small droplet size (87.0 ± 0.4 nm) and high drug content.
• S-SNEDDS demonstrated excellent storage stability over 4 weeks with no significant drug degradation.
• Enhanced drug release profiles were observed under simulated gastric and intestinal conditions compared to raw Olaparib.
• The S-SNEDDS formulation showed a fourfold increase in absorption in Caco-2 assays, indicating improved oral bioavailability.

Conclusions:

• S-SNEDDS is a viable and effective strategy for enhancing the oral delivery and bioavailability of poorly soluble drugs like Olaparib.
• The developed S-SNEDDS formulation offers a potent and potentially cost-effective pharmaceutical solution for improved therapeutic outcomes.
• This approach holds significant promise for overcoming oral absorption challenges in drug development.