Valsartan Loaded Solid Self-Nanoemulsifying Delivery System to Enhance Oral Absorption and Bioavailability

Area of Science:

• Pharmaceutical Sciences
• Drug Delivery Systems
• Nanotechnology

Background:

• Valsartan (VST) is an essential angiotensin II receptor antagonist for hypertension management.
• Low oral bioavailability of VST limits its therapeutic efficacy.
• Novel drug delivery systems are needed to enhance VST oral absorption.

Purpose of the Study:

• To develop and characterize a solid self-nanoemulsifying drug delivery system (S-SNEDDS) for valsartan (VST).
• To enhance the oral absorption and bioavailability of VST using the S-SNEDDS formulation.
• To evaluate the in vitro and in vivo performance of the developed VST-loaded S-SNEDDS.

Main Methods:

• Preparation of VST-loaded liquid SNEDDS (VST@L-SNEDDS) by solubility studies and pseudo-ternary phase diagrams.
• Adsorption of VST@L-SNEDDS onto a solid carrier (Neusilin® UFL2) to form VST@S-SNEDDS.
• In vitro assessments including dissolution, stability, cytotoxicity, and Caco-2 cell uptake.
• In vivo pharmacokinetic studies to determine oral bioavailability enhancement.

Main Results:

• VST@L-SNEDDS exhibited optimal characteristics (19.90 nm size, -20.57 mV zeta potential) and was successfully adsorbed onto Neusilin® UFL2.
• VST@S-SNEDDS showed rapid drug release (>90% in 60 min) independent of pH and improved long-term stability compared to VST@L-SNEDDS.
• Both formulations significantly increased Caco-2 cell uptake.
• In vivo studies revealed a 2.28-fold increase in AUC0-24h and a 4.86-fold increase in Cmax for VST@S-SNEDDS compared to raw VST.

Conclusions:

• The developed VST@S-SNEDDS is an effective system for enhancing valsartan oral absorption and bioavailability.
• This novel S-SNEDDS formulation holds significant promise for improving hypertension treatment.
• Solid self-nanoemulsifying drug delivery systems represent a viable strategy for improving the oral delivery of poorly bioavailable drugs like valsartan.