In order to develop a novel transdermal drug delivery system that facilitates the skin permeation of lovastatin encapsulated in novel lipid-based ethanolic vesicular carriers (ethosomes) were constructed and further characterized for vesicular size, entrapment efficiency, in-vitro drug release study and stability. Effect of different concentration of lipid (1-3 % w/w), ethanol (25-40% w/w) and sonication time (10-30 minute) on different properties formulations (R-1 to R-17) was studied. The optimized formulation of lovastatin loaded ethosomes, were selected on criteria, of attaining the maximum value of transdermal flux and entrapment efficiency with minimized vesicle size by applying the point prediction method of the design expert software. Upon “trading off” various response variables and comprehensive evaluation of feasibility search and exhaustive grid search, the formulation composition with lipid (2%), ethanol (25%) and sonication time (30 min.) was found to fulfill the requirements of an optimum formulation (R-5), having entrapment efficacy of 78.28±2.13%, vesicle size of 65±6.08 nm and transdermal flux across rat skin of 51.02±3.68 µg/cm2/hr. The entrapment efficacy was found in the range between the lowest (59.34±2.7%) for the formulation (R6) and maximum entrapment efficacy was found (82.35±1.25%) for (R7). It is concluded from the experimental design that entrapment efficacy has a direct positive relationship with the concentration of ethanol and the sonication time. The In-vitro skin permeation profile of ethosomes shows the formulation R5 showing the maximum flux of 51.02±3.68 µg/cm2/hr with respect to the flux of normal ethanolic drug solution i.e. 3.76±0.36 µg/cm2/hr thus showing the enhancement ratio of 13.77±1.30.it has been observed that the transdermal flux increased with increasing the ethanol concentration and sonication time whereas the transdermal flux decreased with increasing the lipid concentration. Stability studies were performed for R-5ethosomes to study the effect of different temperature conditions on percent entrapment and optimized formulation to study content uniformity and physical appearance for 3 months. Finally, in light of the current data, it can be concluded that ethosomes were a promising candidate for transdermal delivery of Lovastatin and the results advocates the potential of ethosomes of being a safe and very efficient drug carrier for systemic as well as topical delivery of drug.
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