新型姜黄素纳米胶束丝素凝胶的制备及其质量表征  

Preparation and characterization of a novel curcumin-nanomicelles gel

作　　者：钟松阳[1] 郑宏亮[1] 毛凯丽 王思为[1] ZHONG Songyang;ZHENGHongliang;MAO Kaili;WANG Siwei(Department of Pharmacy, People’s Hospital of Quzhou, Quzhou 324000,China)

机构地区：[1]衢州市人民医院药剂科,浙江衢州324000

出　　处：《温州医科大学学报》2019年第3期184-188,共5页Journal of Wenzhou Medical University

基　　金：浙江省药学会医院专项科研基金资助项目(2017ZYY35)

摘　　要：目的:采用自主合成新材料VES-g-PLL制备姜黄素纳米胶束(CUR-NMs)并评价其质量,结合丝素水凝胶制备成CUR-NMs丝素凝胶,为治疗银屑病的姜黄素药物新制剂开发提供参考。方法:应用注入法制备包载姜黄素的VES-g-PLL纳米胶束,测定其微观形态、粒径、Zeta电位、包封率、载药量及释放度等质量评价指标后与丝素蛋白溶液混合超声处理形成CUR-NMs丝素凝胶。通过扫描电镜、HPLC及激光共聚焦显微镜测定CUR-NMs丝素凝胶的微观形态、体外药物释放度及皮肤渗透性。结果:载药纳米胶束呈标准的椭球形、分散均匀、粘连少;粒径为(31.14±7.86)nm、Zeta为(16.70±1.45)mV,包封率高达(82.21%±4.32%)。CUR-NMs丝素凝胶的微观形态为3D网状结果,CUR-NMs以絮状物形式黏附于凝胶3D结构表面,体外药物释放度实验结果显示78 h后CUR-NMs药物累计释放约49%,而CUR-NMs丝素凝胶的药物累计释放约为30%;同时在体皮肤渗透试验显示相比于姜黄素溶液凝胶,应用CUR-NMs丝素凝胶能够显著增加药物的透皮渗透性能。结论:应用新材料VES-g-PLL制备的载药纳米胶束结合丝素凝胶能够实现难溶性药物姜黄素的缓释及透皮吸收,有望成为治疗银屑病等慢性皮肤炎症疾病的一种新方法。Objective:To prepare the curcumin-loaded nanomicelles with a novel polymer, RRR-a tocopheryl succinate-grafted-ε-polylysine conjugate (VES-g-ε-PLL), and to characterize it to use silk fibroin as a hydrogel-based matrix to further facilitate topical delivery of curcumin in exploration of a promising potential of this drug delivery system in the treatment of psoriasis. Methods:VES-g-PLL nanomicelles encapsulated with curcumin were prepared by injection method, and the micromorphology, particle size, Zeta potential, encapsula-tion efficiency, drug loading, and release rate were evaluated. CUR-NMs-gel was then prepared by mixing the CUR-NMs with the SF solution followed by a sonication-induced gelation method. The microscopic morphol-ogy, in vitro drug release and skin permeability of CUR-NMs-gel were determined by scanning electron micros-copy, HPLC and confocal laser scanning microscopy. Results:The CUR-NMs was granulate-like particles with uniform dispersion. The nanomicelles exhibited an ultra-small hydrodynamic diameter (31.14±7.86) nm and a positive Zeta potential (16.70±1.45) mV. Moreover, curcumin could effectively be encapsulated in the polymeric nanoparticles with encapsulating efficiency of 82.21%±4.32%. The CUR-NMs-gel displayed a 3D network with flocculate of CUR-NMs adhering to its surface. The CUR release curves from the CUR-NMs-gel exhibited an obvious sustained release of DTX in physiological media with no evidence of burst effect, and only 30% of CUR was released from the CUR-NMs-gel at 72 h in pH 7.4 PBS, while 49% of CUR was released from the CUR-NMs. Vivo studies on skin penetration showed that the application of CUR-NMs-gel can significantly increase the transdermal permeability of the drug compared with the curcumin solution gel. Conclusion:The permeable nanomicelles-gel system could realize the sustained release and transdermal absorption of the soluble drug cur-cumin, which suggested a promising potential of this drug delivery system to treat such inflammatory skin disor-ders as psoriasi

关 键 词：姜黄素 丝素蛋白 纳米胶束 银屑病 

分 类 号：R94[医药卫生—药剂学]