Abstract:
Background and Aim: Telmisartan (TEL) is an angiotensin II receptor blocker (ARB) antihypertensive agent. The aim of
the present investigation was to develop a self-nanoemulsifying drug delivery system (SNEDDS) to enhance the oral
bioavailability of poorly water soluble TEL. Materials and Methods: The solubility of TEL in various oils was determined
to identify the oil phase of a SNEDDS. Various surfactants and co-surfactants were screened for their ability to emulsify
the selected oil. Pseudoternary phase diagrams were constructed to identify the efficient self-emulsifying region. A
SNEDDS was further evaluated for its percentage transmittance, emulsification time, drug content, phase separation,
dilution, droplet size, zeta potential, pH, refractive index, and viscosity. Results: The developed SNEDDS formulation
contained TEL (20mg), Tween®
20 (43.33%w/w), Carbitol®
(21.67%w/w), and Acrysol®
EL 135 (32%w/w). The optimized
formulation of the TEL-loaded SNEDDS exhibited a complete in vitro drug release in 15min as compared with the plain
drug, which had a limited dissolution rate. It was also compared with the pure drug suspension by oral administration
in male Wister rats. The in vivo study exhibited a 7.5-fold increase in the oral bioavailability of TEL from the SNEDDS
compared with the pure drug suspension. Conclusions: These results suggest the potential use of the SNEDDS to improve
the dissolution and oral bioavailability of poorly water soluble TEL.
Description:
The authors are very thankful to Abitec Corp. (USA), Gettefosse (India),
BASF (India), Sasol (Germany), Nikko Chemicals (Japan), and Corel
Pharma (India) for providing gift samples.