The objective of work was to optimize, formulate, evaluate and compare the transdermal gel containing vesicle based: Transfersomes and liposomes, containing Ketoconazole, an anti-fungal bioactive. Ketoconazole loaded Transfersomes were prepared using thin film hydration method with different concentration of surfactant (Span80, Tween80, and Sodium Deoxycholate) and soya lecithin and characterized for various parameters including Vesicles Size, Morphology, Entrapment Efficiency, Drug Loading Capacity, Turbidity measurement and Stability Evaluation. Optimization of the formulations was done by selecting three process variables: a) concentration of soya lecithin b) concentration of surfactants (Sodium deoxycholate, Tween 80 and span80) and c)
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The Entrapment Efficiency of transfersome formulations was significantly higher than the liposome formulation K21 (30.54±0.452). Transfersomal gel containing 10mg of the drug, 85mg soya lecithin and 15mg of span 80 was concluded to be the optimized formulation (KS19), as it showed maximum drug content (99.78±0.029%), maximum cumulative percent drug release (86.923±0.429%) and good stability at the end of 3 month at 4-8⁰C, 37±0.5ºC and 45±1°C compared to liposome gel and plain gel. In vitro drug release studies showed that the optimized Transfersomes formulation KS19 exhibits sustained drug release over a prolonged period of time. Antifungal activity showed that the developed ketoconazole formulation KS19 was more active against activity of yeast Candida albicans compared to liposome gel (KL21) and plain gel (KG26). This research suggests that ketoconazole loaded transfersomes can be potentially used as a transdermal drug delivery …show more content…
The concentration range of independent variables under study was shown in Table 1 and Table 2 along with their low, medium, and high levels, which were selected based on the results from preliminary experimentation [16]. Sixteen formulations were prepared according to the experimental design shown in Table 3.Accurately weighed quantities of drug, soya lecithin, and edge activators (surfactant) in various ratios as listed in Table 3 was dissolved in chloroform: methanol (2:1) in 250 ml round bottom flasks. The solvent mixture was evaporated at optimized temperature under reduced pressure at 80 rpm using rotary vacuum film evaporator (Heidolph loborata 4011 digital, Switzerland). After complete evaporation of the solvent, the flask was kept under vacuum oven for 24 h to allow complete removal of the residual solvent. The obtained thin lipid film was hydrated at room temperature with 10 ml of aqueous phase (ethanol 7%v/v) as the hydrating medium at 60 rpm using rotary vacuum film evaporator to obtain a homogenous suspension of KTFs(ketoconazole loaded transfersomes) [17]. The suspension was kept for 1 h at ambient temperature for complete hydration process (swelling of phospholipids) to get large multilamellar vesicles (LMLV). The thick suspension thus obtained was broken by vortexing (Vortex shaker, Jyoti scientific industry, India) for 5 minutes [18]. These
The Entrapment Efficiency of transfersome formulations was significantly higher than the liposome formulation K21 (30.54±0.452). Transfersomal gel containing 10mg of the drug, 85mg soya lecithin and 15mg of span 80 was concluded to be the optimized formulation (KS19), as it showed maximum drug content (99.78±0.029%), maximum cumulative percent drug release (86.923±0.429%) and good stability at the end of 3 month at 4-8⁰C, 37±0.5ºC and 45±1°C compared to liposome gel and plain gel. In vitro drug release studies showed that the optimized Transfersomes formulation KS19 exhibits sustained drug release over a prolonged period of time. Antifungal activity showed that the developed ketoconazole formulation KS19 was more active against activity of yeast Candida albicans compared to liposome gel (KL21) and plain gel (KG26). This research suggests that ketoconazole loaded transfersomes can be potentially used as a transdermal drug delivery …show more content…
The concentration range of independent variables under study was shown in Table 1 and Table 2 along with their low, medium, and high levels, which were selected based on the results from preliminary experimentation [16]. Sixteen formulations were prepared according to the experimental design shown in Table 3.Accurately weighed quantities of drug, soya lecithin, and edge activators (surfactant) in various ratios as listed in Table 3 was dissolved in chloroform: methanol (2:1) in 250 ml round bottom flasks. The solvent mixture was evaporated at optimized temperature under reduced pressure at 80 rpm using rotary vacuum film evaporator (Heidolph loborata 4011 digital, Switzerland). After complete evaporation of the solvent, the flask was kept under vacuum oven for 24 h to allow complete removal of the residual solvent. The obtained thin lipid film was hydrated at room temperature with 10 ml of aqueous phase (ethanol 7%v/v) as the hydrating medium at 60 rpm using rotary vacuum film evaporator to obtain a homogenous suspension of KTFs(ketoconazole loaded transfersomes) [17]. The suspension was kept for 1 h at ambient temperature for complete hydration process (swelling of phospholipids) to get large multilamellar vesicles (LMLV). The thick suspension thus obtained was broken by vortexing (Vortex shaker, Jyoti scientific industry, India) for 5 minutes [18]. These