Proniosomal Telmisartan Tablets: Formulation, in vitro Evaluation and in vivo Comparative Pharmacokinetic Study in Rabbits.
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.
['Teaima|Mahmoud Hasan|MH|0000-0002-7565-301X', 'Yasser|Mohamed|M|', 'El-Nabarawi|Mohamed Ahmed|MA|', 'Helal|Doaa Ahmed|DA|']
D000284:Administration, Oral D000818:Animals D000959:Antihypertensive Agents D001682:Biological Availability D004339:Drug Compounding D008081:Liposomes D010316:Particle Size D011817:Rabbits D013499:Surface Properties D013607:Tablets D000077333:Telmisartan
telmisartan TEL EE bioavailability entrapment efficiency multifactorial design proniosomal-derived niosomes sustained-release tablet