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作为酮咯酸透皮给药载体的前体脂质体

Proniosomes as a drug carrier for transdermal delivery of ketorolac.

作者信息

Alsarra Ibrahim A, Bosela A A, Ahmed S M, Mahrous G M

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh, Kingdom of Saudi Arabia.

出版信息

Eur J Pharm Biopharm. 2005 Apr;59(3):485-90. doi: 10.1016/j.ejpb.2004.09.006.

Abstract

Niosomes are nonionic surfactant vesicles that have potential applications in the delivery of hydrophobic and hydrophilic drugs. Permeation of a potent nonsteroidal anti-inflammatory, ketorolac, across excised rabbit skin from various proniosome gel formulations was investigated using Franz diffusion cells. Each of the prepared proniosomes significantly improved drug permeation and reduced the lag time (P<0.05). Proniosomes prepared with Span 60 provided a higher ketorolac flux across the skin than did those prepared with Tween 20 (7- and 4-fold the control, respectively). A change in the cholesterol content did not affect the efficiency of the proniosomes, and the reduction in the lecithin content did not significantly decrease the flux (P>0.05). The encapsulation efficiency and size of niosomal vesicles formed by proniosome hydration were also characterized by specific high performance liquid chromatography method and scanning electron microscopy. Each of the prepared niosomes achieved about 99% drug encapsulation. Vesicle size was markedly dependent on the composition of the proniosomal formulations. Proniosomes may be a promising carrier for ketorolac and other drugs, especially due to their simple production and facile up.

摘要

非离子表面活性剂囊泡在疏水性和亲水性药物递送方面具有潜在应用。使用Franz扩散池研究了强效非甾体抗炎药酮咯酸从各种前体脂质体凝胶制剂中透过切除的兔皮的渗透情况。所制备的每种前体脂质体均显著改善了药物渗透并缩短了滞后时间(P<0.05)。用司盘60制备的前体脂质体比用吐温20制备的前体脂质体在皮肤表面提供了更高的酮咯酸通量(分别为对照的7倍和4倍)。胆固醇含量的变化不影响前体脂质体的效率,卵磷脂含量的降低也未显著降低通量(P>0.05)。还通过特定的高效液相色谱法和扫描电子显微镜对前体脂质体水合形成的非离子表面活性剂囊泡的包封效率和大小进行了表征。所制备的每种非离子表面活性剂囊泡的药物包封率均达到约99%。囊泡大小明显取决于前体脂质体制剂的组成。前体脂质体可能是酮咯酸和其他药物的一种有前景的载体,特别是由于其生产简单且易于放大。

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