Amorepacific Corporation R&D Center, 314-1, Bora-ri, Giheug-eup, Yeongin-si, Gyeonggi-do 446-729, Republic of Korea.
Int J Pharm. 2010 Mar 30;388(1-2):251-6. doi: 10.1016/j.ijpharm.2009.12.049. Epub 2010 Jan 7.
We have studied how the transdermal delivery of lidocaine hydrochloride (LHC) is affected by the morphology of lipid carriers, liposomes and micelles, having the same lipid composition of 1-stearoyl-sn-glycero-3-phosphocholine (LPC) and cholesteryl hemisuccinate (CHEMS). In vitro drug permeation study, carried out on guinea pig skin, has revealed that the liposomes made of LPC and CHEMS significantly enhance the permeation rate of entrapped LHC; by contrast, the mixed micelles with the same composition decrease the degree of delivering co-existing LHC. Basically, we have also investigated the release kinetics of LHC through the cellulose membrane and found that both liposomes and micelles have a similar releasing profile. To experimentally demonstrate this unique behavior, we have observed the fluidity of stratum corneum liposomal membranes in the presence of either our liposomes or micelles. From this study, we have found that LPC/CHEMS liposomes fluidize the lipid membrane of stratum corneum lipids; however, lipid micelles rather make the membrane rigid. These findings highlight that controlling the morphology of drug carriers provides us with a means to modulate the permeability of encapsulated drug molecules.
我们研究了盐酸利多卡因（LHC）的经皮传递如何受到脂质载体、脂质体和胶束形态的影响，这些载体具有相同的脂质组成，即 1-硬脂酰基-sn-甘油-3-磷酸胆碱（LPC）和胆固醇半琥珀酸酯（CHEMS）。在豚鼠皮肤上进行的体外药物渗透研究表明，由 LPC 和 CHEMS 制成的脂质体显著提高了包封 LHC 的渗透速率；相比之下，具有相同组成的混合胶束降低了共存在的 LHC 的递送程度。基本上，我们还通过纤维素膜研究了 LHC 的释放动力学，发现脂质体和胶束都具有相似的释放曲线。为了实验证明这种独特的行为，我们观察了存在我们的脂质体或胶束时角质层脂质体膜的流动性。从这项研究中，我们发现 LPC/CHEMS 脂质体使角质层脂质的膜流动性增加；然而，脂质胶束使膜变硬。这些发现强调了控制药物载体的形态为我们提供了调节包裹药物分子的渗透性的手段。
