Transdermal Delivery of An Analgesic Agent Using Elastic Liposomes: Preparation, Characterization and Performance Evaluation

Abstract

The aim of the present study was to prepare and characterize novel vesicular carrier elastic liposomes, of most commonly used non-steroidal anti-inflammatory agent diclofenac for its sustained and targeted delivery. Elastic liposomes of diclofenac were prepared and characterized in vitro and in vivo. The effect of different formulation variables like type of surfactant, concentration of surfactant and dose of drug on transdermal flux, amount of drug deposited into the skin, muscle and plasma concentration was investigated. The biological activity of optimized formulation was evaluated using carrageenan induced rat paw edema model and results were compared with commercial hydrogel formulation. The elastic liposomal formulations achieved muscle drug concentration between 2.2+/-0.14 to 5.3+/-0.22 microg/g at 12 hr. The same dose of commercial hydrogel formulation produced drug levels between 0.41+/-0.07 to 1.1+/-0.09 microg/g in the muscle. Plasma concentration study showed regiospecificity of elastic liposomal formulation. The results of in vivo study revealed that incorporation of diclofenac in elastic liposomes increased its biological activity two fold as compared to commercial hydrogel formulation. The results of the present study demonstrated greater effectiveness of dermaly applied diclofenac elastic liposomal formulation in comparison to conventional delivery system. The optimized elastic liposomal formulation offers a promising means for the non-invasive treatment of local pain and inflammation by topical application.

Proultraflexible lipid vesicles for effective transdermal delivery of levonorgestrel: Development, characterization, and performance evaluation

“…7 Phosphatidyl choline (PC)-Span 80 elastic vesicles were recently reported to be more effective in enhancing the skin permeation of dexamethasone, diclofenac, zidovudine, and norgestrel as compared to PC-cholesterol rigid vesicles. [8][9][10][11][12] Despite the strong rationale for use of vesicles in transdermal drug delivery, the major problem in the development of vesicular systems at industrial and clinical levels is their poor stability. Different approaches have been proposed to enhance the stability of vesicles.…”

Elastic Liposomal Formulation for Sustained Delivery of Colchicine: In Vitro Characterization and In Vivo Evaluation of Anti-gout Activity

“…In the present study, results of skin deposition and CLSM study revealed the skin deposition potential of elastic liposomes. Our previous study using elastic liposomal formulations of diclofenac (11) and rizatriptan (15) also indicates the increase in skin deposition and reduction in systemic absorption of these molecules. Colchicine medication is inexpensive than most immunosuppressive agents; however, present therapy associated with toxic effects limited its use as first line therapy in different dermatological conditions.…”

“…Different batches of elastic liposomes were prepared with Span 80 and PC using conventional rotary evaporation sonication method (18). Span 80 was selected as an edge activator because it is biocompatible, pharmaceutically acceptable (22), and provide optimum elasticity to vesicle membrane as optimized in our previous study (11). PC was used as bilayer-forming agent.…”

“…However, the effectiveness of a vesicular system is strongly dependent on its physicochemical characteristics, in particular its thermodynamic state. Deformable vesicles like elastic liposomes have been found to be more effective in enhancing drug transport as compared to rigid vesicles like conventional liposomes for number of drug molecules like dexamethasone (10), diclofenac (11), zidovudine (12), lamivudine (13), propranolol (14), and rizatriptan (15). It was found that high elasticity of these vesicles could facilitate drug transport across the skin as compared to vesicles with rigid membranes.…”

Topical ethosomal capsaicin attenuates edema and nociception in arthritic rats

“…The skin tolerance of prepared formulations was determined by the method described by Jain et al (2005) in normal rats. Hairs were removed from the back (area 2.54 cm 2 ) of each animal using commercial hair remover 24 h before commencement of the experiment.…”