Hadeer A. El-Hashemy, Rawia M. Khalil, Silvia Kocova El Arini, Mona Basha and Ahmed Abdelbary
National Research Centre, Egypt
Cairo University, Egypt
Posters & Accepted Abstracts: J Formul Sci Bioavailab
In the present study, aspasomes were developed to enhance the in-vitro dissolution and the in-vivo performance for tizanidine hydrochloride (TZN), a skeletal muscle relaxant with low oral bioavailability. A Full factorial experimental design was applied to statistically optimize the formulation variables: the amount of drug, amount of ascorbyl palmitate (AP) and the amount of span 60 on the entrapment efficiency, the vesicle size and the invitro release. Aspasomal formulation (TZN-AS 6) composed of 20 mg TZN, 50 mg AP and 50 mg span60 was obtained by employing the desirability function of Design-Expert® software. It exhibited encapsulation efficiency of 95.0 % and smooth surface with particle size 191.8 nm. In addition, skin permeation profile was obtained using static vertical diffusion Franz cells and hairless mouse skin treated with TZN-AS 6 aspasomes 0.2% (w/w) TZN, and compared with unformulated drug. Ex-vivo drug permeation across rat skin for TZN-AS 6 showed a superior skin permeation potential with the highest enhancement ratio value compared to the unformulated drug (ER=4.4). The pharmacokinetic study revealed that aspasomes formulation successively enhanced the bioavailability of TZN compared to oral drug. In conclusion, aspasomes could serve as an effective transdermal delivery of tizanidine hydrochloride.