Title:Sorbitane Monostearate and Cholesterol based Niosomes for Oral Delivery of Telmisartan
Volume: 15
Issue: 2
Author(s): Abdul Ahad*, Mohammad Raish, Fahad I. Al-Jenoobi and Abdullah M. Al-Mohizea
Affiliation:
- Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. Box 2457, Riyadh 11451,Saudi Arabia
Keywords:
Antihypertensive, niosomes, oral, telmisartan, western blot, mRNA.
Abstract: Background: Niosomes are non-ionic surfactant vesicles used as drug carriers for encapsulating
both hydrophobic and hydrophilic drugs. The aim of the present study was to prepare and characterize
niosomes formulations for oral delivery of telmisartan and evaluated for its antihypertensive
activity.
Method: Telmisartan loaded niosomes were prepared using thin film hydration method by varying the
Span 60 and cholesterol at several molar ratios and characterized for vesicles size, polydispersity index,
zeta potential, entrapment efficiency. The in vivo antihypertensive study of optimized formulation
and molecular impact of angiotensin II type-1 receptor (AT1R) messenger Ribonucleic acid (mRNA)
and protein expression on smooth vascular muscles of aorta was determined by real-time polymerase
chain reaction (RT-PCR) and western blot analysis in Wistar albino rats.
Results: The optimized niosomes formulation NS6 presented vesicles size of 618.47 nm, polydispersity
index of 0.86, with entrapment efficiency of 83.83% and possesses negative charge. In vivo study
showed that the optimized formulation could reduce the systolic blood pressure in methyl prednisolone
acetate induced hypertensive rats in close proximity to normal range of systolic blood pressure and
maintain it over an extended period. In addition, telmisartan loaded niosomes treatment to hypertensive
rats significantly attenuates the raised mRNA level and protein level of AT1R gene in comparison to
hypertensive rats.
Conclusion: Results of present study confer the potential of developed niosomes as suitable carriers
for improved oral delivery of telmisartan.
