Proniosomal gel for transdermal delivery of lornoxicam: optimization using factorial design and in vivo evaluation in rats

Abstract

Objective Clinical utility of lornoxicam in oral therapy is primarily restricted by the low solubility and gastric adverse effects. This study evaluated the prospective of optimized proniosomal gel to improve the clinical efficacy of lornoxicam and compare with oral therapy. Methods Proniosomes were formulated by coacervation phase separation technique using span 60, lecithin and cholesterol. A four-factor three-level Box-Behnken design was used to evaluate the effect of amount of four independent variables; span 60 (X 1 ), cholesterol (X 2 ), lecithin (X 3 ) and lornoxicam (X 4 ) on response variables; vesicle size (Y 1 ), entrapment efficiency (Y 2 ) and transdermal flux (Y 3 ). The selected proniosomal gel (F19) was characterized, and evaluated for the transdermal efficacy by ex vivo and in vivo experiments. Results Optimization study signifies that amount of formulation components (span 60, cholesterol, lecithin and lornoxicam) influence the vesicle size, entrapment efficiency and/or transdermal flux. Optimized formulation F19 exhibited nano size with high entrapment efficiency, adequate zeta potential, greater transdermal flux and better stability (at refrigerated conditions). The entrapment of lornoxicam in the bilayers of proniosome vesicles was confirmed by differential scanning calorimeter. Release profile of F19 was distinct (p < 0.001) from gel prepared using hydroxypropyl methylcellulose (control) and displayed steady lornoxicam release by Fickian diffusion. Transdermal administration of F19 significantly inhibited the carrageenan induced hindpaw edema in rats as compared to oral lornoxicam group. Conclusions The data observed in this study demonstrated that the developed proniosomal gel (F19) improved the clinical efficacy of lornoxicam as compared to oral therapy.

Effect of nanostructured lipid carriers on transdermal delivery of tenoxicam in irradiated rats

“…However, both the hydrogel TNX-NLCs and the oral TNX were guarded against these changes to roughly the same extent. Similar findings were reported by other authors (Goindi et al., 2016 ; Baranowski et al., 2018 ; Shah et al., 2019 ). Although the present study did not measure the pharmacokinetics of the drug, our findings suggested that TNX-NLCs hydrogel reached the dermis of the skin and then passed into the systemic circulation and showed its anti-inflammatory effect almost similar to the oral TNX by decreasing the production of free radicals and pro-inflammatory mediators that were accelerated 3 h after carrageenan inoculation.…”

Development and Optimization of Naringenin-Loaded Chitosan-Coated Nanoemulsion for Topical Therapy in Wound Healing

“…The increase in droplet size with increase oil% in the formulation might be explained by the fact that increase ratio of oil to Smix is reflected by reduction of interfacial tension between the interface of two immiscible liquids. Additionally, the inverse relation between percentage of Smix and droplet size can be explained by the fact of that increased Smix% helps in reducing interfacial tension between oil and aqueous phase and thereby provides successful coating over the nano droplets which further leads to stabilization of the developed NEs [ 40 ]. These findings are in agreement with reported literatures [ 41 , 42 ].…”

<p>Bilosomes as Promising Nanovesicular Carriers for Improved Transdermal Delivery: Construction, in vitro Optimization, ex vivo Permeation and in vivo Evaluation</p>

“…It has potential gastrointestinal, liver, cardiac and renal toxicities. 9 Many approaches were previously used to overcome the side effects of LX such as liposomes, 9 proniosomal gel, 10 and niosomes. 11 Transdermal delivery system provides an approach to avoid the side effects of NSAIDs and extend duration of action.…”