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. 2011 Apr;1(2):112-8.
doi: 10.4103/2230-973X.82431.

Design and development of a self-nanoemulsifying drug delivery system for telmisartan for oral drug delivery

Jaydeep Patel  1 , Garala Kevin, Anjali Patel, Mihir Raval, Navin Sheth
Affiliations

Design and development of a self-nanoemulsifying drug delivery system for telmisartan for oral drug delivery

Jaydeep Patel et al. Int J Pharm Investig. 2011 Apr.

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 (20 mg), 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 15 min 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.

Keywords: Bioavailability; poor water solubility; self-nanoemulsifying drug delivery system; telmisartan.

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Conflict of interest statement

Conflict of Interest: None declared.

Figures

Figure 1
Figure 1
Pseudoternary phase diagram with surfactant/cosurfactant (km) = 2:1
Figure 2
Figure 2
Zeta potential determination of the optimized TEL-loaded SNEDDS
Figure 3
Figure 3
In vitro drug release of TEL from the SNEEDS in water and phosphate buffer, pH 1.2 and pH 7.5, compared with the pure drug
Figure 4
Figure 4
Plasma concentration versus time profiles after the oral administration of the TEL-loaded SNEDDS, compared with TEL pharmacokinetics after the dosing aquoues suspension
See this image and copyright information in PMC

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