Chu Xiao-Qin, Huang Jie, Li Zheng-Guang, Li Qian, Cao Jiao-Jiao, Jiang Jian-Qin, Gui Shuang-Ying
School of Pharmacy, Anhui University of Chinese Medicine, Hefei 230012, China.
Institute of Pharmaceutics, Anhui Academy of Chinese Medicine, Hefei 230012, China.
Curr Drug Deliv. 2018;15(10):1439-1448. doi: 10.2174/1567201815666180910142516.
There has been a growing concern in transdermal drug technology over the past several decades. As a novel transdermal delivery system, Lyotropic liquid crystals (LLC) still face challenges such as drug loading, limited drug permeation and instability of systems. LLC system is so sensitive that a very subtle change in composition may induce a phase transformation or conversion of spatial configuration, and result in a diverse percutaneous delivery subsequently.
To find out the effects of hydrophilic and lipophilic components on the structure and transdermal properties of LLCs, hydrophilic sinomenine hydrochloride (SH) and lipophilic cinnamaldehyde (CA) was chosen as a model drug and a skin permeation enhancer, respectively, several formulations were prepared and compared.
The structure of LLC was evaluated by visual observation, Cross-polarizing light microscopy (CPLM) and Small angle X-ray diffraction (SAXS). The Franz diffusion cell was applied to investigate its skin penetration of SH across the rat skins. Fourier transform infrared spectroscopy (FTIR) was recorded to evaluate the intermolecular interaction between the LC samples and stratum corneum (SC).
The results showed that a controlled transdermal process might be obtained by adjusting the ratios of different drugs or loading doses when LLCs with dual-components were applied.
在过去几十年里,透皮给药技术一直备受关注。作为一种新型的透皮给药系统,溶致液晶(LLC)仍然面临着诸如载药量、药物渗透有限以及系统稳定性等挑战。LLC系统非常敏感,组成上的细微变化可能会引发相变或空间构型的转变,进而导致后续不同的经皮给药效果。
为了探究亲水性和疏水性成分对LLC结构和透皮性能的影响,分别选用亲水性的盐酸青藤碱(SH)和疏水性的肉桂醛(CA)作为模型药物和皮肤渗透促进剂,制备并比较了几种制剂。
通过肉眼观察、偏光显微镜(CPLM)和小角X射线衍射(SAXS)对LLC的结构进行评估。采用Franz扩散池研究SH在大鼠皮肤上的透皮情况。记录傅里叶变换红外光谱(FTIR)以评估LC样品与角质层(SC)之间的分子间相互作用。
结果表明,当应用双组分LLC时,通过调整不同药物的比例或载药量,可以实现可控的透皮过程。