title: In vitro assessment of pharmaceutical potential of ethosomes entrapped with terbinafine hydrochloride.
abstract: The present study investigates the entrapment of terbinafine hydrochloride (TH) in ethosomal vesicles via unsonicated and sonication method. Carbopol 934P was incorporated in the best formulation, F6, obtained by sonication method. The formulated ethosomal gel obtained as such i.e. F6(∗) was exploited to achieve a zero order release profile of TH. The composition includes phospholipid, ethanol and propylene glycol. Drug entrapment efficiency (DEE), in-vitro and ex-vivo drug diffusion studies, FT-IR and stability studies of the prepared ethosomes were investigated. The size and shape of F6 ethosomes vesicles were characterized by SEM. In-vitro drug release studies were performed using sigma dialysis membrane in phosphate buffer, pH 7.4 for 12 h while drug content was determined by HPLC. DEE was ranked from 55.33 ± 1.32% to 69.11 ± 2.11%. Highest DEE was seen with F6 ethosomal formulation with a vesicle size of 248 ± 1.02 nm. FT-IR studies confirmed that there was no chemical interaction between drug and excipients used in the formulation. Ex-vivo result suggested that drug diffusion observed after 12 h from F6(∗) and marketed cream (MR) formulations was 74.01 ± 0.62% and 61.45 ± 0.86%, respectively. The results of similarity factor (f 2 values) for MR and F6(∗) ethosomal gel were 85.14 and 42.63, respectively. It revealed that F6(∗) showed dissimilar dissolution profiles. Transdermal flux value for F6(∗) and MR was found to be 144.61 ± 1.28 μg/cm(2)/h and 121.6 ± 1.16 μg/cm(2)/h, respectively. This study disclosed that F6(∗) resides at targeted site for a relatively longer period of time thereby signifying the improved patient compliance.
authors.affiliation: Department of Pharmaceutical Sciences, Ibn Sina National College of Medical Studies, Jeddah 21418, Saudi Arabia.
authors.forename: Syed Ahmed
authors.initials: SA
authors.lastname: Iizhar
authors.affiliation: Department of Basic Sciences, Ibn Sina National College of Medical Studies, Jeddah 21418, Saudi Arabia.
authors.forename: Ismail Ahmed
authors.initials: IA
authors.lastname: Syed
authors.affiliation: Department of Biochemistry, Ibn Sina National College of Medical Studies, Jeddah 21418, Saudi Arabia.
authors.forename: Rukhsana
authors.initials: R
authors.lastname: Satar
authors.affiliation: Center of Excellence in Genomic Medicine Research, King Abdulaziz University, Jeddah 21589, Saudi Arabia.
authors.forename: Shakeel Ahmed
authors.initials: SA
authors.lastname: Ansari
keywords: DEE, drug entrapment efficiency; Ethosomes; In-vitro drug diffusion; MR, marketed cream; PEG, polyethylene glycol; PI, polydispersity index; TH, Terbinafine Hydrochloride; Terbinafine Hydrochloride; Transdermal flux