Formulation and Evaluation of Transdermal Gel Containing Tacrolimus-Loaded Spanlastics: In Vitro, Ex Vivo and In Vivo Studies

Our goal was to prepare Span 60-based elastic nanovesicles (spanlastics (SPLs)) of tacrolimus (TCR) using the adapted ethanol injection method, characterize them, and evaluate their ability to improve the transdermal permeation of the active substance. The impact of two different concentrations of penetration enhancers, namely, propylene glycol and oleic acid, on the entrapment efficiency, vesicle size, and zeta potential was assessed. Moreover, in vitro release through a semipermeable membrane and ex vivo penetration through hairless rat skin were performed. Morphological examination and pharmacokinetics were performed for one selected formulation (F3OA1). TCR-loaded SPLs were effectively formulated with two different concentrations of permeation enhancers, and the effect of these enhancers on their physicochemical properties differed in accordance with the concentration and kind of enhancer used. The results of in vitro release displayed a considerable (p < 0.05) enhancement compared to the suspension of the pure drug, and there was a correlation between the in vitro and ex vivo results. The selected TCR-loaded nanovesicles incorporated into a gel base showed appreciable advantages over the oral drug suspension and the TCR-loaded gel. Additionally, the pharmacokinetic parameters were significantly (p < 0.05) improved based on our findings. Moreover, the AUC_0–7 ng·h/mL form F3 OA1 was 3.36-fold higher than that after the administration of the TCR oral suspension.

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Materials

TCR was kindly supplied by Adwia Pharmaceuticals Co. (Cairo, Egypt). Sorbitan monoesters (Span 60) were obtained from Loba Chemie (Mumbai, India). Polysorbates (Tween^® 80) were obtained from BDH (Kingston, England). Hydroxypropyl methylcellulose (HPMC) were obtained from Colorcon, UK. Propylene glycol (PG) was purchased from Winlab (Germini-house, England). Oleic acid (OA) was obtained from Lobachemi (Mumbai, India). Chloroform, ethanol, and acetonitrile (HPLC grade) were purchased from Fisher Scientific Co. (Hampton, NH, USA). All other ingredients were of pure analytical grade.

Zaki, R.M.; Ibrahim, M.A.; Alshora, D.H.; El Ela, A.E.S.A. Formulation and Evaluation of Transdermal Gel Containing Tacrolimus-Loaded Spanlastics: In Vitro, Ex Vivo and In Vivo Studies. Polymers 2022, 14, 1528. https://doi.org/10.3390/polym14081528