article · Drug Delivery
Non-steroidal anti-inflammatory drugs delivered through the skin can target inflamed tissues directly while avoiding systemic side effects such as gastric haemorrhage and ulcers. Tenoxicam is an anti-inflammatory drug currently restricted to oral tablet forms because of its poor skin absorption. To address this limitation, researchers developed and evaluated six hydrogel formulations containing nanostructured lipid carriers to enhance tenoxicam skin delivery. A chosen formulation, prepared through high-shear homogenisation and ultrasonication, demonstrated a uniform particle size of roughly 680 nanometres, high drug entrapment efficiency of over 92 percent, and no nanoparticle aggregation. In laboratory tests on irradiated rats with induced paw oedema and hyperalgesia, the hydrogel matched the performance of oral tenoxicam in suppressing inflammation. These findings indicate that the carrier-loaded hydrogel represents a viable transdermal alternative to standard oral tablets for treating inflammatory conditions.
Oral anti-inflammatory medications frequently cause severe gastrointestinal side effects, including ulcers and internal bleeding. Developing an effective skin-applied hydrogel allows targeted drug delivery directly to painful, inflamed areas. This method provides the therapeutic benefits of tenoxicam while potentially bypassing the risks associated with long-term oral consumption, offering safer management options for patients with inflammatory conditions.
This research could enable pharmaceutical manufacturers to develop topical pain-relief gels as alternatives to oral tablets. The technology is in the preclinical testing phase, having demonstrated equivalent anti-inflammatory efficacy to oral delivery in irradiated rat models and ex vivo skin tissue. Further development would require human clinical trials to establish safety, skin absorption rates, and therapeutic equivalence before the formulation could reach commercial pharmacy markets.
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Transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) is an effective route of drug administration, as it directs the drug to the inflamed site with reduced incidence of systemic adverse effects such as gastric hemorrhage and ulcers. Tenoxicam (TNX) is a member of NSAIDs that are marketed only as oral tablets due to very poor absorption through the skin. The current study intended to formulate and characterize a hydrogel loaded with nanostructured lipid carriers (NLCs) to enhance the transdermal delivery of TNX. Six formulations of TNX were formulated by slight modifications of high shear homogenization and ultrasonication method. The selected formula was characterized for their particle size, polydispersity index (PDI), zeta potential, entrapment efficiency (EE), <i>in-vitro</i> drug release and <i>ex-vivo</i> skin permeation studies. Moreover, the effectiveness of the developed formula was studied <i>in-vivo</i> using carrageenan-induced paw edema and hyperalgesia model in irradiated rats. Formula F4 was chosen from six formulations, as the average diameter was 679.4 ± 51.3 nm, PDI value of about 0.02, zeta potential of -4.24 mV, EE of 92.36%, globules nanoparticles without aggregations and absence of interactions in the developed formula. Additionally, the <i>in-vivo</i> study showed the efficacy of formula F4 (TNX-NLCs hydrogel) equivalent to oral TNX in reducing the exaggerated inflammatory response induced by carrageenan after irradiation. In conclusion, the present findings suggest that TNX-NLCs hydrogel could be a potential transdermal drug delivery system alternative to the oral formulation for the treatment of various inflammatory conditions.
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DOI: 10.1080/10717544.2020.1803448
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