Nano-appended transdermal gel of Tenoxicam via ultradeformable drug carrier system

Abstract

Tenoxicam is one of the potent non-steroidal anti-inflammatory drugs (NSAIDs), which is used clinically in the treatment of rheumatoid arthritis. Like other NSAIDs, Tenoxicam also suffers from the drawback of being associated with gastrointestinal side effects. Further, transdermal penetration of this drug is very poor, which circumvents the use of transdermal route. The main objective of this study is to exploit the concept of ultradeformable vesicles to increase the transport of Tenoxicam through transdermal route, and also to present it as a possible replacement for the oral NSAID therapy for rheumatoid arthritis. Three concentrations (5%, 15% and 25%) of three different surfactants (Tween-80, Span-80 and sodium desoxycholate) were used along with soya lecithin to prepare the ultradeformable vesicles. Among nine different types of vesicles, T3 vesicles (with 25% Tween-80) were found to have shown the smallest size (82.80 AE 0.74 nm), highest release in 24 h (98.01 AE 0.33%) and highest deformability (31.27 AE 0.28) and hence chosen for formulating into the gel. Among three different Carbopol Õ 934 concentrations (1%, 1.5% and 2%), G-2 with 1.5% carbopol was chosen as the final formulation. The formulation has shown almost twice the transdermal flux as compared to the gel with free Tenoxicam. The in vivo performance was also found to be significantly better than the oral Tenoxicam and marketed aceclofenac gel (Hifenac Õ ). This study concluded that the gel containing Tenoxicam encapsulated in ultradeformable vesicles has a better prospective for the transdermal use to treat rheumatoid arthritis.

Investigating the potential of employing bilosomes as a novel vesicular carrier for transdermal delivery of tenoxicam

“…TX adverse effects' profile is comparable to that of other NSAIDs as it mainly affects the GI tract initiating epigastric pain, indigestion, dyspepsia, vomiting, and GI ulceration (Gonzalez and Todd, 1987). Further, it has been reported that transdermal penetration of TX is very poor limiting its use transdermally (Gwak and Chun 2001;Negi et al, 2013). Accordingly, the aim of the present work was to investigate the ability of bilosomes to increase the transdermal transport of TX, thereby, avoid unnecessary GI side effects associated with oral administration.…”

Formulation Design and Characterization of Silver Sulfadiazine Loaded Nano Gel in the Treatment of Burn

“…Although, some particles were found to be clusters but mostly was in uniform dispersion and uniform distribution in respect to overall formulation [21]. Average Particle size and Zeta potential: Particle size of SSD loaded nanogel were subjected initially through Zeta sizer which result was revealed that the size of the particle was affected by concentration of noveon polycarbophil AA1 and homogenization time [23]. Although particle size of the formulation FG-5 was found to be within the range i.e.…”

Modulation of Inflammatory Mediators by Polymeric Nanoparticles Loaded with Anti-Inflammatory Drugs

“…Injectable formulations like in situ-forming microparticles, showed promising results as TNX delivery vehicles in terms of anti-inflammatory and antioxidant activity for rheumatoid arthritis [ 29 ]. Moreover, TNX has been encapsulated into delivery systems such as microemulsion-based formulations [ 30 ], proniosomes [ 31 ] and ultradeformable vesicles based on surfactant molecules [ 32 ], for transdermal and topical applications.…”