Yoo Jin-Wook, Dharmala Kiran, Lee Chi H
Department of Pharmaceutical Sciences, School of Pharmacy, University of Missouri, Kansas City, MO 64110, USA.
Int J Pharm. 2006 Feb 17;309(1-2):139-45. doi: 10.1016/j.ijpharm.2005.11.020. Epub 2006 Jan 10.
To develop an efficient female controlled drug delivery system (FcDDS) against sexually transmitted diseases (STDs), the polymeric films containing sodium dodecyl sulfate (SDS) were prepared with various compositions of Carbopol 934P, hydroxypropyl methylcellulose (HPMC) and polyethylene glycol (PEG). The physicochemical properties of mucoadhesive polymeric films, such as tensile strength, contact angle, swelling ratio and erosion rate in a vaginal fluid stimulant (VFS), were characterized. In addition, the drug release profile of SDS from the films and mucosal residence time were evaluated using a simulated dynamic vaginal system. It was demonstrated that the films made of Carbopol, HPMC and PEG were colorless, thin and soft and had proper physicodynamic properties for FcDDS. An increase in Carbopol content elevated tensile strength and swelling ratio but decreased the contact angle, erosion rate and the SDS release rate from the films. The films containing 0.25% (w/v) PEG as well as 0.75% (w/v) of combining Carbopol and HPMC remained on the vaginal tissue for up to 6h. The films containing the ratio of Carbopol:HPMC:PEG=1.5:1.5:1 and 1:2:1 seem to be optimal compositions for FcDDS, as they showed good peelability, relatively high swelling index and moderate tensile strength, and achieved the target release rate of SDS for 6h.
为开发一种高效的针对性传播疾病(STD)的女性控制药物递送系统(FcDDS),制备了含有十二烷基硫酸钠(SDS)的聚合物薄膜,其由不同组成的卡波姆934P、羟丙基甲基纤维素(HPMC)和聚乙二醇(PEG)构成。对粘膜粘附性聚合物薄膜的物理化学性质进行了表征,如拉伸强度、接触角、溶胀率以及在阴道液模拟物(VFS)中的侵蚀速率。此外,使用模拟动态阴道系统评估了SDS从薄膜中的药物释放曲线以及在粘膜上的停留时间。结果表明,由卡波姆、HPMC和PEG制成的薄膜无色、薄且柔软,具有适合FcDDS的物理动力学性质。卡波姆含量的增加提高了拉伸强度和溶胀率,但降低了接触角、侵蚀速率以及薄膜中SDS的释放速率。含有0.25%(w/v)PEG以及0.75%(w/v)卡波姆与HPMC混合物的薄膜在阴道组织上可保留长达6小时。含有卡波姆:HPMC:PEG = 1.5:1.5:1和1:2:1比例的薄膜似乎是FcDDS的最佳组成,因为它们显示出良好的可剥离性、相对较高的溶胀指数和适度的拉伸强度,并实现了SDS 6小时的目标释放速率。