摘要
该研究以聚乙烯醇(PVA)和甲基乙烯基醚/马来酸共聚物(PVM/MA)或甲基乙烯基醚/马来酸酐共聚物(PMVE/MAH)作为复合基质材料,采用热交联法制备水凝胶微针,考察热交联温度、时间以及复合材料种类对水凝胶微针形态、溶胀率的影响,筛选并优化热交联工艺条件。PVM/MA和PVA(1∶1)在80℃/2 h、95℃/0.5 h和110℃/0.5 h以及PMVE/MAH和PVA(1∶1)在80℃/2 h、95℃/1 h和110℃/0.5 h条件下制备的水凝胶微针均显示出良好的溶胀率(>200%)、凝胶组分百分比(>80%)、疗效和安全性。对制备的水凝胶微针进行XRD和DSC分析,结果显示,与物理混合物相比,以PMVE/MAH和PVA(1∶1)制备的水凝胶微针的XRD图谱中2θ为19.45°处PVA衍射峰的消失,玻璃化转变温度(Tg)从约150℃降至约58℃,说明聚合物发生了酯化反应,成功交联。该研究为PVA和PVM/MA或PMVE/MAH复合基质水凝胶微针的透皮给药应用提供了参考。
Polyvinyl alcohol(PVA) and methyl vinyl ether and maleic acid copolymer(PVM/MA) or methyl vinyl ether and maleic anhydride copolymer(PMVE/MAH) were used as composite matrix materials to prepare hydrogel microneedles by thermal crosslinking method.The effects of crosslinking temperature,time,and material type on the morphology and swelling rate of hydrogel microneedles were investigated to optimize the thermal crosslinking conditions.Hydrogel microneedles prepared with PVM/MA and PVA(1∶1) at 80 ℃/2 h,95 ℃/0.5 h and 110 ℃/0.5 h,and PMVE/MAH and PVA(1∶1) at 80 ℃/2 h,95 ℃/1 h,110 ℃/0.5 h showed good swelling rate(>200%),percentage of gel fraction(>80%),efficacy,and safety.The results of differential scanning calorimetry(DSC) and X-ray diffraction(XRD)analyses showed that compared with the physical mixture group,the PVA diffraction peak at 2θ of 19.45° in the XRD pattern of hydrogel microneedles disappeared and glass transition temperature(Tg) was decreased from about 150 ℃ to 58 ℃,which confirmed that the polymers underwent esterification and were successfully crosslinked.This study provided references for transdermal drug delivery applications of PVA and PVM/MA or PMVE/MAH composite matrix hydrogel microneedles.
作者
王方园
侯俞如
任晓庆
赵姚姚
郭旻彤
WANG Fangyuan;HOU Yuru;REN Xiaoqing;ZHAO Yaoyao;GUO Mintong(School of Pharmaceutical Sciences,Zhengzhou University,Zhengzhou 450001;Pingyuan Lab.and National Key Lab.of Innovative Drugs for Antiviral Infectious Diseases,Xinxiang 453000)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2023年第10期1475-1484,1492,共11页
Chinese Journal of Pharmaceuticals
