CN105908373A - 一种缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法 - Google Patents
一种缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法 Download PDFInfo
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Abstract
本发明公开了一缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，包括将醋酸纤维素溶于有机溶剂中，超声振荡使醋酸纤维素充分溶解，然后在溶解好的溶液中分别加入萘普生前药以及表面活性剂，超声振荡使其充分均匀溶解，得到纺丝液等步骤，本发明方法简单，安全，容易操作，且具较高的效率，在载药纳米纤维制备和药物控释研究方面有很好的应用前景；所得的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜可以实现萘普生前药的缓慢释放，可以应用到医用载药纤维经皮释放的释药动力学释放特征研究以及局部炎症和疼痛的针对性治疗。
Description
技术领域
本发明属含药物的纺织材料制备领域，特别涉及一缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法。
背景技术
萘普生(Naproxen)是优良的非甾体解热镇痛抗炎药物，具有消炎、镇痛、解热作用，临床广泛用于风湿性、类风湿性关节炎等疾病的治疗。但是它们口服对胃肠道刺激性较大，易引起消化道溃疡和出血，因此它们的经皮给药研究已受到人们的高度重视，尤其适于局部炎症和疼痛的治疗。其中，前体药物方法作为改善酮洛芬经皮吸收特性的一种重要手段已有报道。
静电纺丝(Electrospinning)是一种利用聚合物溶液或熔体在强电场中的喷射作用进行纺丝加工的工艺。近年来，静电纺丝作为一种可制备超细纤维的新型加工方法，引起了广泛的关注。由于静电纺丝所得到的纤维比常规方法得到的纤维细度小，所以其非织造膜具有超高的特异性比表面积和孔隙率，可用于增强聚合物纳米复合材料、过滤膜材、功能性织物保护涂层、传感器、纳米模板和生物医用材料等。目前国内外对静电纺丝的研究发展迅速，成果也非常多。静电纺丝是获得纳米纤维的一项简便技术。在静电纺丝工艺过程中所用到的主要设备有3个部分：高压电源、喷丝头和接收屏。它利用电场作用，迫使聚合物溶液通过一个小孔挤出，在电场力作用下，处于纺丝喷头的聚合物溶液或熔体液滴，克服自身的表面张力而形成带电细流，在喷射过程中细流分裂多次，经溶剂挥发或固化后而形成超细纤维，最终被收集在接收屏上，形成非织造超细纤维膜。
近几年来，静电纺丝技术已经用于几十种不同的聚合物既包括大品种的采用传统技术生产的合成纤维如：聚酯、尼龙、聚乙烯醇等柔性高分子，又包括聚氨酯、丁二烯-苯乙烯嵌段共聚物等弹性体电纺以及液晶态的刚性高分子聚对苯二甲酰对苯二胺等的电纺。此外，包括蚕丝、蛛丝在内的蛋白质和核酸等生物大分子也进行过静电纺丝。纤维素是地球上最丰富的多糖化合物，广泛存在于自然界。纤维素不溶于水，但溶于浓盐酸和浓硫酸。纤维素酯是天然聚合物的衍生物，其溶液或熔体易被加工成膜和纤维，近年来关于纤维素静电纺丝的报道也较多。
本发明采用传统静电纺丝方法制备载有萘普生前药的醋酸纤维素纳米纤维，以实现药物的缓释，具有较好的研究前景。
发明内容
本发明所要解决的技术问题是提供一种缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法。本发明方法简单，安全，容易操作，且具较高的效率，在载药纳米纤维制备和药物控释研究方面有很好的应用前景；本发明所得的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜可以实现萘普生前药的缓慢释放，可以应用到医用载药纤维经皮释放的释药动力学释放特征研究以及局部炎症和疼痛的针对性治疗。
本发明是通过以下计算方案来实现的：
本发明公开了一种缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，具体步骤如下：
1)、将醋酸纤维素溶于有机溶剂中，超声振荡使醋酸纤维素充分溶解，然后在溶解好的溶液中分别加入萘普生前药以及表面活性剂，超声振荡使其充分均匀溶解，得到纺丝液；
2)、将配置好的溶液倒入溶液储存器中并置于微量注射泵上，储存器出口连接削平的注射针头，将高压电源正极与针头相连，负极与铝箔纤维接收平板连接，打开电源；
3)、依据合适的电纺条件进行静电纺丝得缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜。
作为进一步地改进，本发明所述步骤1)所选用的有机溶剂为纺丝溶剂为比例为2/1ml或4/1ml或6/1ml的丙酮/DMAc混合溶剂或者比例为4/1/1ml的丙酮/DMAc/乙醇混合溶剂。
作为进一步地改进，本发明所述的步骤1)所选用的萘普生前药是萘普生甲酯、萘普生乙酯或者萘普生异丙酯。
作为进一步地改进，本发明所述步骤1)表面活性剂是SDS、CTAB或者Triton X-100。
作为进一步地改进，本发明所述步骤1)中醋酸纤维素在纺丝液中浓度为5-20％(w/v)，萘普生前药相对于醋酸纤维素质量浓度为5％，表面活性剂加入量为醋酸纤维素质量的1％。
作为进一步地改进，本发明所述步骤2)中的溶液储存器为5毫升注射器，注射器针头为9号针头。
作为进一步地改进，本发明所述步骤3)中纺丝工艺参数为：电压8-15千伏，注射器推进速度为1.0毫升/小时，接收距离为150毫米，所接收的纳米电纺纤维膜的面积为10cm*10cm。
本发明的有益效果如下：
(1)本发明方法简单，安全，容易操作，且具较高的效率，在载药纳米纤维制备和药物控释研究方面有很好的应用前景；
(2)本发明所得的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜可以实现萘普生前药的缓慢释放，可以应用到医用载药纤维经皮释放的释药动力学释放特征研究以及局部炎症和疼痛的针对性治疗。
附图说明
图1是实施例1中得到的缓释萘普生甲酯的醋酸纤维素纳米电纺纤维膜(醋酸纤维素浓度为10％)的纤维表面扫描电镜照片；
图2是实施例2中得到的缓释萘普生乙酯的醋酸纤维素纳米电纺纤维膜(醋酸纤维素浓度为15％)的纤维表面扫描电镜照片；
图3是实施例1,2,3中得到的可释放萘普生酯类前药醋酸纤维素纳米电纺纤维膜，在磷酸盐缓冲液(pH 7.4)中的药物体外溶出曲线。
具体实施方式
下面结合具体实施例，进一步阐述本发明。应理解，这些实施例仅用于说明本发明而不用于限制本发明的范围。此外应理解，在阅读了本发明讲授的内容之后，本领域技术人员可以对本发明作各种改动或修改，这些等价形式同样落于本申请所附权利要求书所限定的范围。实施例1
用电子天平称取干燥的醋酸维生素0.5克，投入到5毫升丙酮/DMAc/乙醇(4/1/1)混合溶剂中完全溶解，再称取0.025克萘普生甲酯以及0.005克CTAB加入到溶解好的醋酸纤维素溶液中，超声振荡使其充分均匀溶解，得到纺丝液。将配置好的溶液倒入5毫升注射器中，采用削平的9号注射针头作为喷射细流的毛细管，将高压电源正极与针头相连，负极与铝箔纤维接收平板连接，打开电源。调节电压为12千伏，注射器推进速度为1.0毫升/小时，接收距离为150毫米，铝箔纸接收得到大小为10厘米x10厘米的缓释抗疱疹类病毒药物的聚丙烯腈纳米电纺纤维膜。
实施例2
用电子天平称取干燥的醋酸维生素0.75克，投入到5毫升丙酮/DMAc(2/1)混合溶剂中完全溶解，再称取0.0375克萘普生甲酯以及0.0075克SDS加入到溶解好的醋酸纤维素溶液中，超声振荡使其充分均匀溶解，得到纺丝液。将配置好的溶液倒入5毫升注射器中，采用削平的9号注射针头作为喷射细流的毛细管，将高压电源正极与针头相连，负极与铝箔纤维接收平板连接，打开电源。调节电压为8千伏，注射器推进速度为1.0毫升/小时，接收距离为150毫米，铝箔纸接收得到大小为10厘米x10厘米的缓释抗疱疹类病毒药物的聚丙烯腈纳米电纺纤维膜
实施例3
用电子天平称取干燥的醋酸维生素1.0克，投入到5毫升丙酮/DMAc(6/1)混合溶剂中完全溶解，再称取0.05克萘普生甲酯以及0.01克Triton X-100加入到溶解好的醋酸纤维素溶液中，超声振荡使其充分均匀溶解，得到纺丝液。将配置好的溶液倒入5毫升注射器中，采用削平的9号注射针头作为喷射细流的毛细管，将高压电源正极与针头相连，负极与铝箔纤维接收平板连接，打开电源。调节电压为15千伏，注射器推进速度为1.0毫升/小时，接收距离为150毫米，铝箔纸接收得到大小为10厘米x10厘米的缓释抗疱疹类病毒药物的聚丙烯腈纳米电纺纤维膜。
本发明所述的实施例1～3仅仅是对本发明的优选实施方式进行的描述，并非对本发明构思和范围进行限定，在不脱离本发明设计思想的前提下，本领域中工程技术对本发明的技术方案作出的各种变型和改进，均应落入本发明的保护范围。
Claims (8)
1.一种缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，其特征在于，具体步骤如下：
1)、将醋酸纤维素溶于有机溶剂中，超声振荡使醋酸纤维素充分溶解，然后在溶解好的溶液中分别加入萘普生前药以及表面活性剂，超声振荡使其充分均匀溶解，得到纺丝液；
2)、将配置好的溶液倒入溶液储存器中并置于微量注射泵上，储存器出口连接削平的注射针头，将高压电源正极与针头相连，负极与铝箔纤维接收平板连接，打开电源；
3)、依据合适的电纺条件进行静电纺丝得缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜。
2.根据权利要求1所述的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，其特征在于，所述步骤1)所选用的有机溶剂为纺丝溶剂为比例为2/1ml或4/1ml或6/1m的丙酮/DMAc混合溶剂或者比例为4/1/1ml的丙酮/DMAc/乙醇混合溶剂。
3.根据权利要求1所述的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，其特征在于，所述步骤1)所选用的萘普生前药是萘普生甲酯、萘普生乙酯或者萘普生异丙酯。
4.根据权利要求1或2或3所述的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，其特征在于，所述步骤1)表面活性剂是SDS、CTAB或者Triton X-100。
5.根据权利要求4所述的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，其特征在于，所述步骤1)中醋酸纤维素在纺丝液中浓度为5-20％(w/v)，萘普生前药相对于醋酸纤维素质量浓度为5％，表面活性剂加入量为醋酸纤维素质量的1％。
6.根据权利要求1或2或3或5所述的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，其特征在于，所述步骤2)中的溶液储存器为5毫升注射器，注射器针头为9号针头。
7.根据权利要求6所述的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，其特征在于，所述步骤3)中纺丝工艺参数为：电压8-15千伏，注射器推进速度为1.0毫升/小时，接收距离为150毫米，所接收的纳米电纺纤维膜的面积为10cm*10cm。
8.根据权利要求1或2或3或5或7所述的缓释萘普生酯类前药的醋酸纤维素纳米电纺纤维膜制备方法，其特征在于，所述步骤3)中纺丝工艺参数为：电压8-15千伏，注射器推进速度为1.0毫升/小时，接收距离为150毫米，所接收的纳米电纺纤维膜的面积为10cm*10cm。
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Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN114939114A (zh) * | 2022-05-31 | 2022-08-26 | 北京化工大学 | 一种熔体静电纺丝的透皮贴剂及其生产工艺 |
| CN115825187A (zh) * | 2022-11-04 | 2023-03-21 | 军事科学院系统工程研究院卫勤保障技术研究所 | 一种用于细菌及生物分子检测的电化学传感器及其制备和检测方法 |
| WO2023060027A1 (en) * | 2021-10-07 | 2023-04-13 | Matregenix, Inc. | Electrospun nanofibrous polymer membrane for use in air filtration applications |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050276841A1 (en) * | 2004-06-07 | 2005-12-15 | California Institute Of Technology | Biodegradable drug-polymer delivery system |
| CN101250763A (zh) * | 2008-03-11 | 2008-08-27 | 东华大学 | 可部分降解的长效载药聚丙烯腈纤维、其制备及应用 |
| CN101327182A (zh) * | 2008-07-25 | 2008-12-24 | 东华大学 | 一种水难溶性药物的纳米晶体纤维毡的制备 |
| CN101785760A (zh) * | 2010-03-25 | 2010-07-28 | 东华大学 | 一种自组装壳聚糖载药纳米粒及其制备方法 |
| CN102218019A (zh) * | 2011-06-17 | 2011-10-19 | 上海理工大学 | 高压静电喷雾制备疏水性药物纳米颗粒状固体分散体的方法 |
| CN103757743A (zh) * | 2013-12-25 | 2014-04-30 | 中国科学院化学研究所 | 包载脂质体的核壳纳米纤维 |
-
2016
- 2016-04-13 CN CN201610226769.4A patent/CN105908373A/zh active Pending
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20050276841A1 (en) * | 2004-06-07 | 2005-12-15 | California Institute Of Technology | Biodegradable drug-polymer delivery system |
| CN101250763A (zh) * | 2008-03-11 | 2008-08-27 | 东华大学 | 可部分降解的长效载药聚丙烯腈纤维、其制备及应用 |
| CN101327182A (zh) * | 2008-07-25 | 2008-12-24 | 东华大学 | 一种水难溶性药物的纳米晶体纤维毡的制备 |
| CN101785760A (zh) * | 2010-03-25 | 2010-07-28 | 东华大学 | 一种自组装壳聚糖载药纳米粒及其制备方法 |
| CN102218019A (zh) * | 2011-06-17 | 2011-10-19 | 上海理工大学 | 高压静电喷雾制备疏水性药物纳米颗粒状固体分散体的方法 |
| CN103757743A (zh) * | 2013-12-25 | 2014-04-30 | 中国科学院化学研究所 | 包载脂质体的核壳纳米纤维 |
Non-Patent Citations (1)
| Title |
|---|
| XIAO-MEI WU ET AL: "Ester prodrug-loaded electrospun cellulose acetate fiber mats as transdermal drug delivery systems", 《JOURNAL OF MATERIALS SCIENCE:MATERIALS IN MEDICINE》 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023060027A1 (en) * | 2021-10-07 | 2023-04-13 | Matregenix, Inc. | Electrospun nanofibrous polymer membrane for use in air filtration applications |
| CN114939114A (zh) * | 2022-05-31 | 2022-08-26 | 北京化工大学 | 一种熔体静电纺丝的透皮贴剂及其生产工艺 |
| CN115825187A (zh) * | 2022-11-04 | 2023-03-21 | 军事科学院系统工程研究院卫勤保障技术研究所 | 一种用于细菌及生物分子检测的电化学传感器及其制备和检测方法 |
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