自黏性经皮给药SIS/C5静电纺丝膜的结构及性能调控  

Structure and Performance Modulation of Self‑Adhesive SIS/C5 Electrospun Membranes for Transdermal Drug Delivery

作　　者：刘丰硕 董茜 赵忠夫[1] 刘伟[1] 张春庆[1] LIU Feng-Shuo;DONG Qian;ZHAO Zhong-Fu;LIU Wei;ZHANG Chun-Qing(State Key Laboratory of Fine Chemicals,School of Chemical Engineering,Dalian University of Technology,Dalian 116024,China;Affiliated Cancer Hospital of Dalian University of Technology(Liaoning Cancer Hospital),Shenyang 110042,China)

机构地区：[1]大连理工大学化工学院,精细化工国家重点实验室,大连116024 [2]大连理工大学附属肿瘤医院(辽宁省肿瘤医院),沈阳110042

出　　处：《应用化学》2022年第10期1523-1532,共10页Chinese Journal of Applied Chemistry

基　　金：中央高校基本科研业务费(Nos.DTU21YG132,LD202107);国家自然科学基金项目(Nos.51673034,51877029)资助。

摘　　要：静电纺丝膜能有效提高经皮给药贴剂的透气性及释药性能,然而,它们多数不具有黏结性,难以直接贴敷于皮肤表面,药物到达皮肤表面的路径不通畅,影响经皮给药。以C5树脂赋予聚(苯乙烯-异戊二烯-苯乙烯)(SIS)静电纺丝膜压敏黏结性能,研究纺丝膜组成及模型药物合成辣椒素对SIS/C5静电纺丝膜结构、性能及释药性能的影响及调控规律。结果表明,当SIS与C5质量比为2∶1时,其静电纺丝膜贴剂具有优异的透气性(7.17×10^(−3) g/(h·cm^(2)))及黏附性能(180(°)剥离强度0.2 kN/m,初黏力0.64 N/cm^(2),持粘性大于7 d);药物与聚合物基质相容性良好,无药物结晶析出,药物的载入有利于改善纺丝膜贴剂的水蒸气渗透性;8%(质量分数)载药量时,载药纺丝膜初黏力为0.6~0.8 N/cm^(2),180(°)剥离强度保持为0.2~0.3 kN/m,持粘性大于7 d,剥离时无残留;体外释药呈现缓释特征,不同载药量纺丝膜的药物24 h累计释放率均大于50%,满足外用贴剂使用要求。Electrospun membranes are widely utilized to enhance the water vapor permeability and drug delivery performance of transdermal drug delivery patches.Due to the lack of adhesion property,however,most of them cannot closely contact with skin,which impedes the delivery of drugs to the skin,thus affecting the transdermal administration.C5 resin is used to endow poly(styrene isoprene styrene)(SIS)electrospun membranes with pressure-sensitive adhesion property.Investigation is performed on how to control the structure,adhesion properties and drug delivery performance of SIS/C5 electrospun membranes loaded with synthetic capsaicin via compositions,drugs and electrospinning conditions.The results demonstrate that the electrospun membrane with a SIS/C5 ratio of 2∶1 has excellent water vapor permeability(7.17×10^(-3) g/h·cm^(2))and adhesion properties(180(°)peel strength is 0.2 kN/m,tack force is 0.64 N/cm^(2),holding power is greater than 7 days).The synthetic capsaicin has good compatibility with the SIS/C5 electrospun membranes,in which no drug crystallizes and the drug loading is beneficial to improve the water vapor permeability.As the drug loading is 8%,the tack force is 0.6~0.8 N/cm^(2),the 180(°)peel strength is 0.2~0.3 kN/m,the holding power is greater than 7 days,and no residue is left during peeling tests.In vitro drug release indicates that the drug has a behavior of sustained release with a 24-hour cumulative release rate of greater than 50%for all SIS/C5 electrospun membranes,meeting the requirements of transdermal drug delivery patches.

关 键 词：外用贴剂 静电纺丝 自黏性 药物缓释 

分 类 号：O613[理学—无机化学]