Vora B, Khopade A J, Jain N K
Department of Pharmaceutical Sciences, Dr. Harisingh Gour University, Sagar, India.
J Control Release. 1998 Jul 31;54(2):149-65. doi: 10.1016/s0168-3659(97)00100-4.
A proniosome based transdermal drug delivery system of levonorgestrel (LN) was developed and extensively characterized both in vitro and in vivo. The proniosomal structure was liquid crystalline-compact niosomes hybrid which could be converted into niosomes upon hydration. The system was evaluated in vitro for drug loading, rate of hydration (spontaneity), vesicle size, polydispersity, entrapment efficiency and drug diffusion across rat skin. The effect of composition of formulation, amount of drug, type of Spans, alcohols and sonication time on transdermal permeation profile was observed. The stability studies were performed at 4 degrees C and at room temperature. The biological assay for progestational activity included endometrial assay and inhibition with the formation of corpora lutea. The study demonstrated the utility of proniosomal transdermal patch bearing levonorgestrel for effective contraception.
开发了一种基于前体脂质体的左炔诺孕酮（LN）透皮给药系统，并在体外和体内进行了广泛表征。前体脂质体结构是液晶-致密脂质体的混合物，水化后可转化为脂质体。该系统在体外评估了药物负载量、水化速率（自发性）、囊泡大小、多分散性、包封效率以及药物在大鼠皮肤上的扩散情况。观察了制剂组成、药物用量、司盘类型、醇类和超声处理时间对透皮渗透曲线的影响。在4℃和室温下进行了稳定性研究。孕激素活性的生物学测定包括子宫内膜测定和对黄体形成的抑制作用。该研究证明了含左炔诺孕酮的前体脂质体透皮贴剂在有效避孕方面的实用性。
