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.
Keywords: Antihypertensive, niosomes, oral, telmisartan, western blot, mRNA.
Current Drug Delivery
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.
Export Options
About this article
Cite this article as:
Ahad Abdul *, Raish Mohammad , Al-Jenoobi I. Fahad and Al-Mohizea M. Abdullah , Sorbitane Monostearate and Cholesterol based Niosomes for Oral Delivery of Telmisartan, Current Drug Delivery 2018; 15 (2) . https://dx.doi.org/10.2174/1567201814666170518131934
DOI https://dx.doi.org/10.2174/1567201814666170518131934 |
Print ISSN 1567-2018 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5704 |
Call for Papers in Thematic Issues
Advances of natural products, bio-actives and novel drug delivery system against emerging viral infections
Due to the increasing prevalence of viral infections and the ability of these human pathogens to develop resistance to current treatment strategies, there is a great need to find and develop new compounds to combat them. These molecules must have low toxicity, specific activity and high bioavailability. The most suitable ...read more
Electrospun Fibers as Drug Delivery Systems
In recent years, electrospun fibers have attracted considerable attention as potential platforms for drug delivery due to their distinctive properties and adaptability. These fibers feature a notable surface area-to-volume ratio and can be intentionally designed with high porosity, facilitating an increased capacity for drug loading and rendering them suitable for ...read more
Emerging Nanotherapeutics for Mitigation of Neurodegenerative Disorders
Conditions affecting the central nervous system (CNS) present a significant hurdle due to limited access of both treatments and diagnostic tools for the brain. The blood-brain barrier (BBB) acts as a barrier, restricting the passage of molecules from the bloodstream into the brain. The most formidable challenge facing scientists is ...read more
Nanotechnology Based Chemotherapy for the treatment of Head & Neck Cancer
The escalating recurrence rates observed in Head and Neck cancer, particularly within the chemo-therapeutically treated cohort (50-60%), can be attributed to the non-selective nature of current anticancer drug delivery modalities. In this context, nanotechnology-based drug delivery systems emerge as a promising avenue for achieving precise localization of therapeutic agents to ...read more
- Author Guidelines
- Graphical Abstracts
- Fabricating and Stating False Information
- Research Misconduct
- Post Publication Discussions and Corrections
- Publishing Ethics and Rectitude
- Increase Visibility of Your Article
- Archiving Policies
- Peer Review Workflow
- Order Your Article Before Print
- Promote Your Article
- Manuscript Transfer Facility
- Editorial Policies
- Allegations from Whistleblowers
Related Articles
-
Environmental Pollution and Diabetes Mellitus
Recent Patents on Biomarkers Recent Advances in Management of Diabetic Macular Edema
Current Diabetes Reviews Medical Treatment of Aortic Aneurysms in Marfan Syndrome and other Heritable Conditions
Current Cardiology Reviews Tacrine Derivatives and Alzheimers Disease
Current Medicinal Chemistry Targeting Soluble Epoxide Hydrolase for Inflammation and Pain - An Overview of Pharmacology and the Inhibitors
Inflammation & Allergy - Drug Targets (Discontinued) Vitamin D status in coronary artery disease: association with IL-35 and TGF-β1 and disease severity
Endocrine, Metabolic & Immune Disorders - Drug Targets VEGF Inhibitors in Metastatic Renal Cell Carcinoma: Current Therapies and Future Perspectives
Current Clinical Pharmacology Rheumatoid Arthritis: An Autoimmune Disease with Female Preponderance and Cardiovascular Risk Equivalent to Diabetes Mellitus: Role of Cardiovascular Magnetic Resonance
Inflammation & Allergy - Drug Targets (Discontinued) Editorial (Thematic Issue: The Crosstalk between Non-Pharmaceutical and Pharmaceutical Approaches to Prevention and Treatment of Chronic Diseases: Current Concepts and Perspectives)
Current Pharmaceutical Design Editorial (Thematic Issue: Modifying Cardiovascular Risk Factors: Current Opinion and Future Trends)
Current Pharmaceutical Design Chronotherapeutic Drug Delivery Systems - An Approach to Circadian Rhythms Diseases
Current Drug Delivery Advanced Therapies For End-Stage Heart Failure
Current Cardiology Reviews Epoxyeicosatrienoic Acids as a Therapeutic Target for Nephropathy Associated with Diabetes and Hypertension
Current Hypertension Reviews Effect of the NMDA-Receptor Antagonist Dextromethorphan in Infant Rat Pneumococcal Meningitis
Current Drug Metabolism Threes Company: Regulation of Cell Fate by Statins
Current Drug Targets - Cardiovascular & Hematological Disorders Editorial [Hot Topic: Waiting for Action on the Osteoarthritis Front (Guest Editors: Virginia Byers Kraus and Thomas Aigner)]
Current Drug Targets Coarctation of the Aorta - An Evolution of Therapeutic Options
Current Cardiology Reviews Binding Interactions of Forskolin with Human Serum Albumin: Insights from In silico and Spectroscopic Studies
Current Chemical Biology Secondary Hypertension: Novel Insights
Current Hypertension Reviews Glycosaminoglycan Sulodexide Inhibition of MMP-9 Gelatinase Secretion and Activity: Possible Pharmacological Role Against Collagen Degradation in Vascular Chronic Diseases
Current Vascular Pharmacology