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Comparative Study
. 2020 Mar 31:14:1319-1331.
doi: 10.2147/DDDT.S245013. eCollection 2020.

Proniosomal Telmisartan Tablets: Formulation, in vitro Evaluation and in vivo Comparative Pharmacokinetic Study in Rabbits

Mahmoud Hasan Teaima  1 , Mohamed Yasser  2   3 , Mohamed Ahmed El-Nabarawi  1 , Doaa Ahmed Helal  4
Affiliations
Comparative Study

Proniosomal Telmisartan Tablets: Formulation, in vitro Evaluation and in vivo Comparative Pharmacokinetic Study in Rabbits

Mahmoud Hasan Teaima et al. Drug Des Devel Ther. .

Abstract

Objective: The purpose of this study was to prepare proniosomal vesicles of Telmisartan (TEL) to be compressed into tablets which will be further evaluated in vitro and in vivo.

Materials and methods: An experimental design was adopted using surfactants of different HLB values (span 40-brij 35), different cholesterol ratios (20-50%) and different phospholipid types (egg yolk-soyabean). Different responses were measured followed by tablet manufacturing. The highest EE was shown in F3 (85%) while the lowest value was obtained in F7 (8.4%). Finally, zeta potential results were in the range of -0.67 to -27.6 mv. Compressibility percent revealed that F5 showed an excellent flowability characteristic with a value of 9.74±1.61 while F3 and F6 showed good flowability characteristics. By the end of the release, F6 showed approximately 90% drug release.

Results: F6 was selected for the in vivo study; Cmax was increased by 1.5-fold while AUC0-∞ also increased significantly by 3-fold when compared with commercial tablet and finally, tmax was increased by 3-fold indicating sustained release pattern. The relative bioavailability was also increased by 3.2-fold.

Conclusion: The results of this study suggested that the formulation of compressed tablets containing more stable proniosomal powder extended the release of TEL and increased its bioavailability as well.

Keywords: EE; TEL; bioavailability; entrapment efficiency; multifactorial design; proniosomal-derived niosomes; sustained-release tablet; telmisartan.

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Conflict of interest statement

The authors declare that they have no conflict of interests.

Figures

Figure 1
Figure 1
F3, F5 and F6 desirability factors according to design expert 7.
Figure 2
Figure 2
Particle size measurement of formula 6.
Figure 3
Figure 3
Transmission electron microscope micrograph of F3.
Figure 4
Figure 4
Scanning electron micrograph of (A) maltodextrin powder (uncoated), (B) proniosomes (F3), and (C) niosomes derived from proniosomes.
Figure 5
Figure 5
Dissolution profile of Telmisartan from different preparations.
Figure 6
Figure 6
HPLC chromatogram of Telmisartan.
Figure 7
Figure 7
Comparative plasma concentration-time profile of Telmisartan from F6 and commercial product.
See this image and copyright information in PMC

References

    1. Baghel S, Cathcart H, O’reilly NJ. Polymeric amorphous solid dispersions: a review of amorphization, crystallization, stabilization, solid-state characterization, and aqueous solubilization of biopharmaceutical classification system class II drugs. J Pharm Sci. 2016;105(9):2527–2544. doi:10.1016/j.xphs.2015.10.008 - DOI - PubMed
    1. Sharma D. Solubility enhancement strategies for poorly water-soluble drugs in solid dispersions: a review. Asian J Pharm. 2016;1.
    1. Dizaj SM, Vazifehasl Z, Salatin S, Adibkia K, Javadzadeh Y. Nanosizing of drugs: effect on dissolution rate. Res Pharm Sci. 2015;10(2):95–108. - PMC - PubMed
    1. Dua J, Rana A, Bhandari A. Liposome: methods of preparation and applications. Int J Pharm Stud Res. 2012;3:14–20.
    1. Ulrich AS. Biophysical aspects of using liposomes as delivery vehicles. Biosci Rep. 2002;22(2):129–150. doi:10.1023/A:1020178304031 - DOI - PubMed

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