5553
Hadeer Ahmed Mohamed Abd El-Ghafar El-Hashemy
Formulation and Evaluation of Nanocarriers for Transdermal Delivery of ýCertain ýMuscle Relaxant Drug
Nano Carriers, transdermal, drug delivery
Tizanidine hydrochloride (TZN), is a skeletal muscle relaxant, clinically used for the symptomatic treatment of muscle stiffness and spasms resulting from multiple sclerosis, injury or disease of the spinal cord. Its principal site of action is the spinal cord, as a centrally acting alpha 2-receptor agonist which regulates the relaxant effects on skeletal muscles. TZN is only available in the form of oral tablets short-acting muscle relaxant used to relieve muscle spasms and stiffness. Unfortunately, TZN exhibits a short half-life of 2.5 hours, a poor oral bioavailability (30- 40 %) and suffers extensive first pass metabolism after oral administration. Therefore, it is important to develop an alternative dosage form to avoid the problems associated with the oral route. Delivering drugs to the general circulation through the skin via transdermal drug delivery (TDD) offers many advantages over the conventional dosage forms; in particular it could bypass the first-pass metabolism by the liver therefore it enhances the bioavailability, it improves patient compliance by reducing the frequency of dosing, it provides less adverse effects. Moreover, it is suitable for patients who are unconscious or vomiting or those who rely on self-administration. In the present study, novel TZN-loaded vesicles were designed and characterized for effective transdermal permeation and enhanced therapeutic bioavailability. Vesicular carriers have been widely investigated to overcome the penetration barriers of stratum corneum aiming for effective transdermal drug delivery. Vesicular systems are self-assembled structures composed of one or several concentric lipid bilayers formed when certain amphiphilic building blocks are confronted with water.
2019
Ph.d
Cairo
Pharmacy