Deo M R, Sant V P, Parekh S R, Khopade A J, Banakar U V
Bharati Vidyapeeth's Poona College of Pharmacy, Erandwane Pune, India.
J Biomater Appl. 1997 Jul;12(1):77-88. doi: 10.1177/088532829701200105.
Mesophasic proliposomal 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 efficacious transdermal delivery of hydrophobic drugs.
开发了用于左炔诺孕酮的中间相前体脂质体系统，并进行了体外和体内评估。这些囊泡大多为单层，但也有少数多层囊泡，水化时会自发脱落。该系统中药物的释放符合零级动力学。研究了醇类和挥发油对透皮通量的影响。发现醇类的通量最高，其次是柠檬油。体内研究表明需要负荷剂量，因为在达到治疗水平之前观察到了明显的滞后阶段。然而，该系统优于用作对照制剂的基于聚乙二醇的软膏系统。结果证明了前体脂质体系统用于有效透皮递送疏水药物的潜力。
