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Mesophasic proliposomat system for levonorgestrel was developed and evaluated both in vitro and in vivo. The vesicles were mostly unilamellar, however, few vesicles were multilamellar which budded off spontaneously upon hydration. The release of drug from this system adhered to zero order kinetics. The effect of alcohols and volatile oils on transdermal flux was investigated. The flux was found to be the highest for alcohol, and followed by that for lemon oil. The in vivo studies indicate the requirement for a loading dose, since, a significant lag phase was observed before the therapeutic levels were reached. This system was, however, superior to the PEG-based ointment system which was employed as the control formulation. The results demonstrate the potential of proliposomal system for efficaceous transdermal delivery of hydrophobic drugs.