Abstract
The objective of the present investigation was to design a vesicular formulation of brimonidine tartrate and evaluate its ability to reduce the dosing frequency and improve the therapeutic efficacy of the drug. Nano-vesicles of brimonidine tartrate were prepared by film hydration method. The prepared vesicles were evaluated for photomicroscopic characteristics, entrapment efficiency, in vitro, and ex-in vitro drug release and in vivo intraocular pressure (IOP) lowering activity. The methods employed for preparation of vesicles produced nano vesicles of acceptable shape and size. The in vitro, and ex-in vitro drug release studies showed that there was slow and prolonged release of the drug, which followed zero-order kinetics. The IOP-lowering activity of nano vesicles was determined and compared with that of pure drug solution and showed that the IOP-lowering action of nano-vesicles sustained for a longer period of time. Stability studies revealed that the vesicle formulations were stable at the temperature range of 2-8°C, with no change in shape and drug content. The results of the study indicate that it is possible to develop a safe and physiologically effective topical formulation that is also convenient for patients.
Highlights
Vesicular drug delivery system using colloidal particulate carriers have distinct advantages over conventional dosage forms because colloidal particles can act as drug containing reservoirs
Vesicle-entrapped drug can be administered in liquid dosage forms such as eye drops with good patient compliance, modulated drug release profile and high drug pay-load
We investigated its intraocular pressure (IOP) lowering activity and its other physical properties and the drug release pattern
Summary
Vesicular drug delivery system using colloidal particulate carriers (liposomes or niosomes) have distinct advantages over conventional dosage forms because colloidal particles can act as drug containing reservoirs. Topical and localized applications are still an acceptable and preferred route for ocular drug delivery, such dosage forms are no longer sufficient to combat ocular diseases such as glaucoma as they have poor bioavailability, which is the result of the efficient mechanisms protecting the eye from harmful materials and agents. Frequent instillation of concentrated medication is required at the Preparation and evaluation of nano-vesicles of brimonidine tartrate site of action and this is inconvenient for the patient.[2] The development of various vesicular drug delivery systems allows the entrapment of the drug molecule into a lipid bilayer or in surfactant vesicles and allows us to increase drug concentration at the site of application and, to improve bioavailability Such vesicles (liposomes and niosomes) act as carriers for controlled ocular drug delivery by preventing metabolism of the drug by enzymes present at the corneal epithelial surface. We investigated its intraocular pressure (IOP) lowering activity and its other physical properties and the drug release pattern
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