Dissolution testing

Biotechnology

Organic chemistry

In vivo

Biopharmaceutics Classification System

Membrane

Biology

Pharmacokinetics

Solubility

Bioavailability

Chemistry

In vitro

Ex vivo

Drug delivery

Drug

Chromatography

Permeation

Biochemistry

Medicine

Pharmacology

Frontiers in Pharmacology

Objective: The aim of this study was to investigate the in vitro and in vivo performance of self-nanoemulsifying drug delivery systems (SNEDDS) of talinolol (TAL), a poorly water soluble drug. Method: SNEDDS of TAL were prepared using various oils, non-ionic surfactants and/or water-soluble co-solvents and assessed visually/by droplet size measurement. Equilibrium solubility of TAL in the anhydrous and diluted SNEDDS was conducted to achieve the maximum drug loading. The in vitro dissolution experiments and human red blood cells (RBC) toxicity test, ex vivo gut permeation studies, and bioavailability of SNEDDS in rats were studied to compare the representative formulations with marketed product Cordanum® 50mg and raw drug. Results: The results from the characterization and solubility studies showed that SNEDDS formulations were stable with lower droplet sizes and higher TAL solubility. From the dissolution studies, it was found that the developed SNEDDS provided significantly higher rate of TAL release (˃97% in 2.0 hours) compared to raw TAL and marketed product Cordanum®. The RBC lysis test suggested negligible toxicity of the formulation to the cells. The ex vivo permeability assessment and in vivo pharmacokinetics study of a selected SNEDDS formulation (F6) showed about 4-fold increase in permeability and 1.58-fold enhanced oral bioavailability of TAL in comparison to pure drug, respectively. Conclusion: TAL loaded SNEDDS formulations could be a potential oral pharmaceutical product with high drug-loading capacity, improved drug dissolution, increased gut permeation, reduced/no human RBC toxicity and enhanced oral bioavailability.

Evaluation of Self-Nanoemulsifying Drug Delivery Systems (SNEDDS) for Poorly Water-Soluble Talinolol: Preparation, in vitro and in vivo Assessment