Abstract

DEVELOPMENT AND EVALUATION OF ORAL NANOEMULSION FOR THE BIOAVAILABILITY ENHANCEMENT OF TELMISARTAN

*Ahmad Hassan, Dr. Jasjeet Kaur Sahni, and Dr. Javed Ali

ABSTRACT

The present study aimed at developing an optimal oral nanoemulsion of telmisartan and evaluating its stability, pharmacodynamic and pharmacokinetic potential. Solubility of telmisartan was determined in various oils, surfactants & cosurfactants. Formulations were selected from the o/w nanoemulsion region from the help of pseudoternary phase diagrams and were subjected to various thermodynamic stability and dispersibility tests. Optimized formulations were characterized for their percentage transmittance, refractive index, viscosity, droplet size and zeta potential & TEM. Release rate of optimized formulations was determined using an in vitro dissolution test. The formulation used for lowering of induced hypertension contained Soyabean oil (10%, v/v), Tween 20 (22.50%, v/v), Transcutol HP (7.5%, v/v) & double distilled water (60% v/v). The release of drug from the nanoemulsion formulations was highly significant (p < 0.01) in comparison to the drug suspension. More than 40% of the drug was released in the initial 1 h of the dissolution study in comparison to the drug suspension. The lowering of blood pressure in the group administered with the formulation F2 was highly significant (p < 0.01) with respect to the group administered with the marketed formulation. The plasma concentration time profile of telmisartan from oral nanoemulsion represented greater improvement of drug absorption than the marketed formulation. The shelf life of the nanoemulsion was found to be 1.5 years at room temperature. The present study established oral nanoemulsion formulation to be one of the possible alternatives to traditional oral formulations of telmisartan to improve its bioavailability.

Keywords: Nanoemulsion, Telmisartan, Pharmacodynamic, and Pharmacokinetic, thermodynamic, pseudoternary phase, Bioavailability, Solubility, surfactants.