Transdermal self-assembled Xanthine/hybrid needle nanofibers for management of abdominal obesity via phosphodiesterase 4B suppression.

The objective of this study was to develop transdermal applicated XOH needle nanofibers (XOH/nNFs) with the ability to target adipocytes in high fat-induced obese rats. Xanthine/Oxime/Hybrid (XOH) which is a methylxanthine analogue with a PDE4 inhibitory activity, was reported as biologically limited by lipophilicity and impaired bioavailability, that was improved by loading in nanofibers for transdermal application. The formulated nanofibers were characterized in-vitro, in-vivo and evaluated on obese rats for their activity as slimming treatment. Nanofibers show good characters regarding drug loading (4.3%), encapsulation (63.3%), particle size (415 nm) and ʓ-potential (+ 55.4 mV). Additionally, The XOH/nNFs were investigated in a high fat diet-induced obesity model in rats where forty-two Sprague Dawley rats (4 weeks old) were used throughout the present study divided into 6 groups (7 rats each group). The XOH/nNFs significantly reduced abdominal circumference of obese rats by 6.59% compared to 3.59% of caffeine, supported by histopathological evidence of enhanced lipolysis and promoted beige adipogenesis. The study states that XOH/nNFs promoted lipolysis and inhibited adipogenesis which can be highlighted as a promising strategy in treatment of obesity.