Kwon Soon Sik, Kong Bong Ju, Park Soo Nam
Department of Fine Chemistry, Seoul National University of Science and Technology, 232 Gongreung-ro, Nowon-gu, Seoul 139-743, South Korea.
Department of Fine Chemistry, Seoul National University of Science and Technology, 232 Gongreung-ro, Nowon-gu, Seoul 139-743, South Korea.
Eur J Pharm Biopharm. 2015 May;92:146-54. doi: 10.1016/j.ejpb.2015.02.025. Epub 2015 Mar 6.
We investigated the physicochemical properties of pH-sensitive hydroxyethyl cellulose (HEC)/hyaluronic acid (HA) complex hydrogels containing isoliquiritigenin (ILTG), and discussed potential applications as transdermal delivery systems for the treatment of skin lesions caused by pH imbalance. HA has skin compatibility and pH functional groups and HEC serves as scaffold to build hydrogels with varied HCE:HA mass ratio. Hydrogels were synthesized via chemical cross-linking, and three-dimensional network structures were characterized via scanning electron microscopy (SEM). The swelling properties and polymer ratios of the hydrogels were investigated at pH values in the range 1-13. HECHA13 (i.e., an HEC:HA mass ratio of 1:3) was found to have optimal rheological and adhesive properties, and was used to investigate the drug release efficiency as a function of pH; the efficiency was greater than 70% at pH 7. Antimicrobial activity assays against Propionibacterium acnes were conducted to take advantage of the pH-sensitive properties of HECHA13. At pH 7, we found that HECHA13, which contained ILTG, inhibited the growth of P. acnes. Furthermore, HECHA13 was found to exhibit excellent permeability into the skin, which penetrated mostly via the hair follicle. These results indicate that this pH-sensitive hydrogel is effective as a transdermal delivery system for antimicrobial therapeutics, with potential applications in the treatment of acne.
我们研究了含有异甘草素(ILTG)的pH敏感型羟乙基纤维素(HEC)/透明质酸(HA)复合水凝胶的物理化学性质,并讨论了其作为透皮给药系统治疗由pH失衡引起的皮肤损伤的潜在应用。HA具有皮肤相容性和pH官能团,HEC作为构建具有不同HCE:HA质量比水凝胶的支架。通过化学交联合成水凝胶,并通过扫描电子显微镜(SEM)对三维网络结构进行表征。研究了水凝胶在pH值为1-13范围内的溶胀性能和聚合物比例。发现HECHA13(即HEC:HA质量比为1:3)具有最佳的流变学和粘附性能,并用于研究药物释放效率与pH的关系;在pH 7时效率大于70%。利用HECHA13的pH敏感特性,对痤疮丙酸杆菌进行了抗菌活性测定。在pH 7时,我们发现含有ILTG的HECHA13抑制了痤疮丙酸杆菌的生长。此外,发现HECHA13对皮肤具有优异的渗透性,主要通过毛囊渗透。这些结果表明,这种pH敏感型水凝胶作为抗菌治疗的透皮给药系统是有效的,在痤疮治疗中具有潜在应用。