Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Abstract

A transdermal therapeutic system (TTS) of diclofenac diethylamine (DDE) was developed to obtain a prolonged controlled drug delivery by the solvent evaporation technique. The matrix diffusion controlled systems used various combinations of hydrophilic (polyvinylpyrrolidone K30) and lipophilic (Eudragit RL 100  and Eudragit RS 100  ) polymers containing dimethyl sulfoxide (DMSO) (0, 5 and 10% w/w) as a penetration enhancer. In vitro drug release was improved with an increased fraction of hydrophilic polymer. Formulation F8 containing Eudragit RL 100 and polyvinylpyrrolidone K30 in the ratio 40:60 presented the highest drug release (92.45%) and permeation rate (0.0988±0.010 mg/cm 2 /h) with sustained release action for 48 h. In vivo pharmacodynamic study of DDE-loaded Eudragit RL 100  transdermal system (formulation F8) showed significant higher percent inhibition of rat paw edema compared with the marketed formulation of the drug. Our results suggest that a developed formulation is an efficient system for transdermal diclofenac delivery against inflammation. The optimized formulation was found to be stable and did not show physicochemical interaction. The system is envisaged to be stable for a sufficiently long period (2.52 years) at room temperature.

Development and evaluation of polycaprolactone-based electrospun nanofibers containing timolol maleate as a sustained-release device for treatment of glaucoma: in vivo evaluation in equine eye

“…Similar results were reported in a previous study that developed TIM-loaded PCL nanofibers with 415 times folding endurance ( 16 ). As it is obvious, the addition of both CA and EUD significantly decreased the folding endurance of PCL-CA and PCL-EUD compared to PCL-1 and PCL-2 formulations due to the much lower folding endurance of CA and EUD plain nanofibers which was also reported by previous studies compared to PCL nanofibers ( 31 32 ).…”

Aminated Polysaccharide-Based Nanoassemblies as Stable Biocompatible Vehicles Enabling Crossing of Biological Barriers: An Effective Transdermal Delivery of Diclofenac Medicine

“…The best-known commercial formulation for skin delivery of diclofenac, Voltaren Emulgel, which is an oil-in-water microemulsion gel, has only 10% bioavailability, 15 requiring combination with Voltaren pills to reach the desired therapeutic effect. Therefore, numerous researchers have tried to develop new delivery systems to improve diclofenac's efficiency and bioavailability using vesicular carriers such as liposomes, 16 various kinds of emulsions, 17 synthetic copolymers 18 and stimulation technologies such as ultrasonic stimulation. 19 T h i s c o n t e n t i s Polysaccharides have also been overlooked as potential materials for use in transdermal medicine.…”