Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
Comparative Study
. 2021 Nov 10:15:4603-4614.
doi: 10.2147/DDDT.S327860. eCollection 2021.

Transdermal Delivery of Telmisartan: Formulation, in vitro, ex vivo, Iontophoretic Permeation Enhancement and Comparative Pharmacokinetic Study in Rats

Mahmoud Teaima  1 , Rehab Abdelmonem  2 , Yomna A Adel  3 , Mohamed A El-Nabarawi  1 , Tayseer M El-Nawawy  3
Affiliations
Comparative Study

Transdermal Delivery of Telmisartan: Formulation, in vitro, ex vivo, Iontophoretic Permeation Enhancement and Comparative Pharmacokinetic Study in Rats

Mahmoud Teaima et al. Drug Des Devel Ther. .

Abstract

Purpose: The purpose of this study was to prepare telmisartan transethosomes, incorporate them into a gel, evaluate them for in vitro drug release and in vivo permeation using iontophoresis to enhance their transdermal delivery.

Materials and methods: TE formulae were prepared using various surfactants (SAAs), different ethanol concentrations, and different phospholipid-to-SAA ratios with different cholesterol ratios, characterized according to their entrapment efficiency percentage (EE%), zeta potential (ZP), particle size (PS), and polydispersity index (PDI). The optimum three formulae were incorporated into a gel, evaluated physically, in vitro dissolution, and ex vivo drug permeation using rat skin and Iontophoresis was performed on the best formula.

Results: The optimum three formulae (F29, F31, F32) had an EE% of 97±0.26%, 89±0.25% and 88±0.17%, PS of 244±5.88 nm, 337±4.6 nm and 382.2±3.06 nm, PDI of 0.57±1.9, 0.5±1.4 and 0.63±2.2 and ZP of -31.6±1.59 mV, -28.3±3.79 mV and -31±5.65, respectively. Selecting F29 for in vivo study by iontophoretic enhancement, Cmax was increased by 1.85 folds compared to the commercial oral tablet and by 1.5 folds compared to transdermal gel. Tmax decreased by half using iontophoresis compared to commercial tablets and transdermal gel.

Conclusion: The transethosomal formulation of telmisartan enhanced its transdermal absorption and increased its bioavailability as well. Iontophoresis was used to increase maximum plasma concentration and reduce Tmax by half.

Keywords: EE; TEL; entrapment efficiency; iontophoresis; telmisartan; transethosomes.

PubMed Disclaimer

Conflict of interest statement

The authors report no potential conflicts of interest in this work.

Figures

Figure 1
Figure 1
(A is Conc. of Ethanol, B is Type of SAA, C is Additives (Cholesterol : SAA ratio) and D is SAA : Soyabean ratio), A Graphs of solutions for optimization of Telmisartan Ethosomes, solution 1; B Graphs of solutions for optimization of Telmisartan Ethosomes, solution 2; C Graphs of solutions for optimization of Telmisartan Ethosomes, solution 3; DCar chart of desirability for optimization of telmisartan ethosomes, solution 1; E Bar chart of desirability for optimization of telmisartan ethosomes, solution 2; F Bar chart of desirability for optimization of telmisartan ethosomes, solution 3.
Figure 2
Figure 2
DSC Thermogram of drug (Telmisartan), polymer (Carbopol 940), drug to polymer physical mixture and formula 29
Figure 3
Figure 3
Fourier transform infrared (FT-IR) spectra of drug (Telmisartan), polymer (Carbopol 940) and drug& polymer physical mixture
Figure 4
Figure 4
(Abbreviation TE, transethosome), A Transmission Electron Micrograph of TE29; B Transmission Electron Micrograph of TE31; C Transmission Electron Micrograph of TE32
Figure 5
Figure 5
A In vitro drug release of transethasome different formulae vs drug suspension (mean ±SD, n=3); B Ex vivo drug permeation of transethasome different formulae vs drug suspension(mean± SD, n=3).
Figure 6
Figure 6
A Setting of experiment of application of Telmisartan transethosome gel Iontophoresis; B Comparative study of plasma concentration-time curve for commercial product, formula 29 and formula 29 with Iontophoresis.
See this image and copyright information in PMC

References

    1. Pitt B, Konstam MA. Overview of angiotensin II-receptor antagonists. Am J Cardiol. 1998;82(10A):47S–49S. doi:10.1016/S0002-9149(98)00807-8 - DOI - PubMed
    1. Stangier J, Su CA, Roth W. Pharmacokinetics of orally and intravenously administered telmisartan in healthy young and elderly volunteers and in hypertensive patients. J Int Med Res. 2000;28(4):149–167. doi:10.1177/147323000002800401 - DOI - PubMed
    1. Sentjurc M, Vrhovnik K, Kristl J. Liposomes as a topical delivery system: the role of size on transport studied by the EPR imaging method. J Control Release. 1999;59:87–97. doi:10.1016/S0168-3659(98)00181-3 - DOI - PubMed
    1. Teaima MH, Yasser M, El-Nabarawi MA, Helal DA. Proniosomal telmisartan tablets: formulation, in vitro evaluation and in vivo comparative pharmacokinetic study in rabbits. Drug Des Devel Ther. 2020;14:1319–1331. doi:10.2147/DDDT.S245013 - DOI - PMC - PubMed
    1. Yasser M, Teaima M, El-Nabarawi M, El-Monem RA. Cubosomal based oral tablet for controlled drug delivery of telmisartan: formulation, in-vitro evaluation and in-vivo comparative pharmacokinetic study in rabbits. Drug Dev Ind Pharm. 2019;45(6):981–994. doi:10.1080/03639045.2019.1590392 - DOI - PubMed

Publication types