载多西紫杉醇Poloxamer188复合PEG100k电纺纤维的表征  

Characterization of Docetaxel Loaded Poloxamer188 Composite PEG100k Electro-spun Fibers

作　　者：邱志越 王瑛颖 吕蕴麒 王浩 Qiu Zhiyue;Wang Yingying;Lv Yunqi;Wang Hao(School of Pharmacy,Jinzhou Medical University,Jinzhou 121000 China)

机构地区：[1]锦州医科大学药学院,辽宁锦州121000

出　　处：《锦州医科大学学报》2024年第2期9-17,共9页Journal of Jinzhou Medical University

基　　金：辽宁省药物作用与质量评价专业技术创新中心与辽宁省海洋生物活性物质重点实验室主任基金项目,项目编号:2020-06,2021-4。

摘　　要：目的考察Poloxamer188复合PEG100k电纺纤维的形态及载多西紫杉醇后的形态、材料复合,以及载药纤维水化后药物增溶和包裹情况。方法将多西紫杉醇、Poloxamer188和PEG100k溶解在二氯甲烷中形成共溶液后静电纺丝。考察了Poloxamer188的复合量从10%直至100%以及多西紫杉醇载量为5%、10%、15%、20%等情况。扫描电子显微镜考察纤维形态、差示热分析、热重分析和X-射线衍射考察材料复合及载药。分别在纯水/载药纤维为40/100和5/100(V/m,mL/mg)两种水化条件下水化载药纤维,前者得到液体后者溶胀。在10000 r/min下离心3 min后,前者得到固体沉淀和上清液,后者得到水凝胶沉淀和上清液。采用高效液相色谱-紫外分光光度法测定两种不同处理方法下上清液中多西紫杉醇的含量,分别计算药物增溶百分率和渗漏百分率。结果所得电纺纤维直径均小于5μm,直径较为均一且完全无珠子结构存在。物质之间发生复合,但是在纤维表面有PEG100k片段的衍射峰。水化后所得的液体,5%多西紫杉醇载量的纤维药物增溶百分率最高,大部分样品在70%~80%之间,载药量升高至10%、15%时,增溶百分率降至20%以下,载药量升高至20%时,大部分样品增溶量接近于0。5%载药量系列纤维随着Poloxamer188复合量的增高药物增溶百分率先升高后降低,F-5%-40%中多西紫杉醇的增溶百分率可达80%。多西紫杉醇载量为5%时,水化后所得的凝胶渗漏百分率大于其他载药量的情况,但是未超过5%的渗漏百分率,载药量为10%、15%、20%时,渗漏百分率均小于2%。结论通过均相溶液静电纺丝技术可以制备形态较为理想的载多西紫杉醇PEG100k纤维,水化后纤维中的药物增溶量可以达到药典标准,多西紫杉醇载量及Poloxamer188复合量对药物增溶量影响明显,且所得水化凝胶渗漏率很低。Objective To investigate the morphology and material composition of Poloxamer188 composite PEG100k electro-spun fibers before and after loading docetaxel,as well as the drug solubilization and encapsulation after fibers hydration.Methods Docetaxel,Poloxamer188,and PEG100k were dissolved in dichloromethane to form co-solutions and be electro-spun.The composite contents of Poloxamer188 from 10%to 100%and the loading of docetaxel of 5%,10%,15%,and 20%were investigated.Scanning electron microscopy was used to investigate fiber morphology,and differential thermal analysis,thermogravimetric analysis,and X-ray diffraction were used to investigate materials recombination and drug loading.Under the hydration conditions of pure water/drug-loaded fiber 40/100 and 5/100(V/m,mL/mg)respectively,the former obtained liquid and the latter swelled.After centrifugation at 10000 r/min for 3 min,solid precipitate and supernatant were obtained in the former and hydrogel precipitate and supernatant in the latter.The content of docetaxel in supernatant under two different treatment methods was determined by high performance liquid chromatography-ultraviolet spectrophotometry,and the percentage of solubilization and percentage of leakage were calculated respectively.Results The obtained electro-spun fibers are all less than 5μm in diameter,with uniform diameters and no bead structure.Recombination occurs between the materials,but there are diffraction peaks of PEG100k fragments on the fiber surface.In the liquid obtained after hydration,the solubilization percentage of fiber drug with 5%docetaxel load was the highest,and most samples were between 70%and 80%.When the drug load increased to 10%and 15%,the solubilization percentage decreased to below 20%,and when the drug load increased to 20%,the solubilization percentage of most samples was close to 0.With the increase of Poloxamer188 compound amount,the solubilization percentage of the 5%drug load series fiber first increased and then decreased,and the solubilization percentage of docet

关 键 词：多西紫杉醇 电纺纤维 聚乙二醇 泊洛沙姆 增溶 

分 类 号：R965[医药卫生—药理学]