CN111374939A - 一种骨质增生治疗凝胶制剂的合成方法 - Google Patents
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Abstract
本发明公布一种骨质增生治疗凝胶制剂的合成方法。主要步骤:1)PLGA‑PEG‑PLGA凝胶溶液的制备；2)混合法制备NSAIDs‑PTT治疗凝胶。其中金纳米颗粒具有优异的光热性能和光热转换性能，可以有效地将光能转化为热能，从而对异常细胞或组织起到清除作用。非甾体类消炎药(NSAIDS)是一类非类固醇激素类的能够消除疼痛、肿胀、四肢僵直及炎症的药物。非甾体类消炎药通常被用于多种情况下的疼痛性疾病:包括关节炎、滑囊炎、肌腱炎、痛风、经期痉挛、扭伤、劳损以及其他的损伤。PLGA‑PEG‑PLGA无毒，生物相容性好，在常温下呈液态，35度左右相变为凝胶，很好地用于体内注射，延长药物在体内的滞留，从而提高治疗效果。
Description
技术领域
本发明涉及凝胶制剂的合成技术领域,具体涉及一种通过PLGA-PEG-PLGA包裹金纳米颗粒和非甾体类消炎药(NSAIDS)的策略,合成NSAIDs-PTT治疗凝胶制剂的方法。
背景技术
骨质增生又叫骨关节炎，也叫退行性骨关节炎，也叫骨关节病，也叫老年性骨关节病也叫增生性骨关节病。它主要是指关节软骨随着年龄的增长，因为劳损、活动量的增多、过多，引起关节软骨的退变、磨损，软骨下骨的裸露。另外在关节的边缘增生了一些新生的骨赘，也就是骨刺，进一步发展会导致关节的变形。
非甾体类消炎药(NSAIDS)是一类非类固醇激素类的能够消除疼痛、肿胀、四肢僵直及炎症的药物。非甾体类消炎药通常被用于多种情况下的疼痛性疾病:包括关节炎、滑囊炎、肌腱炎、痛风、经期痉挛、扭伤、劳损以及其他的损伤。也可用来治疗术后那些不需要麻醉性镇痛药的轻微疼痛，或是作为一段强效镇痛治疗后的后续治疗。非甾体类消炎药还可以作为那些不能够接受麻醉镇痛药物的患者急性疼痛的替代治疗。
金纳米颗粒是很有潜力的光热治疗剂，具有优异的光热性能和光热转换性能，可以有效地将光能转化为热能，从而对异常细胞或组织起到清除作用。改善骨质增生和骨关节畸形的发生。
PLGA-PEG-PLGA是一种三嵌段聚合物。其中PLGA由两种单体——乳酸和羟基乙酸随机聚合而成，是一种可降解的功能高分子有机化合物，其降解产物是乳酸和羟基乙酸，同时也是人代谢途径的副产物，所当它应用在医药和生物材料中时不会有毒副作用，具有良好的生物相容性、无毒、良好的成囊和成膜的性能。PEG具有良好的水溶性，生物相容性好，并赋予了聚合物温敏相变的性质。
发明内容
本发明为克服现有技术的不足，提供一种通过PLGA-PEG-PLGA包裹金纳米颗粒和非甾体类消炎药(NSAIDS)的策略,骨质增生治疗凝胶制剂的合成方法。利用金纳米颗粒抑制机体的特异性细胞免疫和体液免疫反应，抑制类骨质增生的免疫过激反应，防止免疫系统攻击自身正常关节组织，以达到治疗类骨质增生的目的。
本发明的技术方案是一种骨质增生治疗凝胶制剂的合成方法，通过PLGA-PEG-PLGA包裹金纳米颗粒和非甾体类消炎药(NSAIDS)的策略,具体步骤如下：
1)称取PLGA-PEG-PLGA材料，加入水中溶解，得到浓度为0.2-0.4mg/ml的PLGA溶液；
2)称取NSAIDS药物，加入水中溶解，得到浓度为5-8mg/ml的NSAIDS溶液；
3)各取适量混合成骨质增生治疗凝胶。
所述步骤3)具体如下：
(1)在室温下将盛有1ml的PLGA-PEG-PLGA溶液的单口瓶置于旋转搅拌器上，搅拌速度设定为500r/min；
(2)边搅拌边逐滴加入8uL的NSAIDS水溶液和20uL金纳米颗粒溶液，继续搅拌直至完全混匀，最终得到NSAIDs-PTT骨质增生治疗凝胶。
本发明的优势在于：
1)金纳米颗粒具有优异的光热性能和光热转换性能，可以有效地将光能转化为热能，从而对异常细胞或组织起到清除作用。
2)非甾体类消炎药(NSAIDS)是一类非类固醇激素类的能够消除疼痛、肿胀、四肢僵直及炎症的药物。
3)PLGA-PEG-PLGA无毒，生物相容性好，在常温下呈液态，35度左右相变为凝胶，可以很好地用于体内注射，延长药物在体内的滞留，从而提高效果。
附图说明
图1：金纳米颗粒光热图像。
具体实施方式
以下结合附图和具体实施例来对本发明作进一步的说明。
实施例1：
1)准确称取0.25mg的PLGA-PEG-PLGA材料，加入1mL水溶解，得到浓度为0.25mg/ml的PLGA-PEG-PLGA水溶液。
2)准确称取5mg的NSAIDS药物，加入1mL水溶解，得到浓度为5mg/ml的NSAIDS水溶液。
3)混合法合成NSAIDs-PTT骨质增生治疗凝胶的方法如下：
(1)在室温下将盛有1ml的PLGA-PEG-PLGA溶液的单口瓶置于旋转搅拌器上，搅拌速度设定为500r/min；
(2)边搅拌边逐滴加入8uL的NSAIDS水溶液和20uL金纳米颗粒溶液，继续搅拌直至完全混匀，最终得到NSAIDs-PTT骨质增生治疗凝胶。
实施例2：
1)准确称取0.2mg的PLGA-PEG-PLGA材料，加入1mL水溶解，得到浓度为0.2mg/ml的PLGA-PEG-PLGA溶液。
2)准确称取8mg的NSAIDS药物，加入1mL水溶解，得到浓度为8mg/ml的NSAIDS水溶液。
3)混合法合成NSAIDs-PTT骨质增生治疗凝胶的方法如下：
(1)在室温下将盛有1ml的PLGA-PEG-PLGA溶液的单口瓶置于旋转搅拌器上，搅拌速度设定为500r/min；
(2)边搅拌边逐滴加入6uL的NSAIDS水溶液和20uL金纳米颗粒溶液，继续搅拌直至完全混匀，最终得到NSAIDs-PTT骨质增生治疗凝胶。
实施例3：
1)准确称取0.4mg的PLGA-PEG-PLGA材料，加入1mL水溶解，得到浓度为0.4mg/ml的PLGA-PEG-PLGA溶液。
2)准确称取6mg的NSAIDS药物，加入1mL水溶解，得到浓度为6mg/ml的NSAIDS水溶液。
3)混合法合成NSAIDs-PTT骨质增生治疗凝胶的方法如下：
(1)在室温下将盛有1ml的PLGA-PEG-PLGA溶液的单口瓶置于旋转搅拌器上，搅拌速度设定为500r/min；
(2)边搅拌边逐滴加入10uL的NSAIDS水溶液和20uL金纳米颗粒溶液，继续搅拌直至完全混匀，最终得到NSAIDs-PTT骨质增生治疗凝胶。图1为金纳米颗粒光热图像。
Claims (2)
1.一种骨质增生治疗凝胶制剂的合成方法，其特征是，通过PLGA-PEG-PLGA包裹金纳米颗粒和非甾体类消炎药(NSAIDS)的策略,具体步骤如下：
1)称取PLGA-PEG-PLGA材料，加入水中溶解，得到浓度为0.2-0.4mg/ml的PLGA-PEG-PLGA溶液；
2)称取NSAIDS药物，加入水中溶解，得到浓度为5-8mg/ml的NSAIDS溶液；
3)取6-10uL的NSAIDS水溶液和20uL金纳米颗粒溶液加入1mlPLGA-PEG-PLGA水溶液中混合成骨质增生治疗凝胶。
2.根据权利要求1所述的骨质增生治疗凝胶制剂的合成方法，其特征是，所述步骤3)具体如下：
(1)在室温下将盛有1ml的PLGA-PEG-PLGA溶液的单口瓶置于旋转搅拌器上，搅拌速度设定为500r/min；
(2)边搅拌边逐滴加入6-10uL的NSAIDS水溶液和20uL金纳米颗粒溶液，继续搅拌直至完全混匀，最终得到NSAIDs-PTT治疗凝胶。
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Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1861041A (zh) * | 2006-03-29 | 2006-11-15 | 沈阳药科大学 | 局部注射用温敏型缓释凝胶剂及制备方法 |
| CN109701074A (zh) * | 2018-12-29 | 2019-05-03 | 广州贝奥吉因生物科技有限公司 | 一种骨修复支架及其制备方法 |
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- 2020-03-31 CN CN202010246570.4A patent/CN111374939A/zh active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1861041A (zh) * | 2006-03-29 | 2006-11-15 | 沈阳药科大学 | 局部注射用温敏型缓释凝胶剂及制备方法 |
| CN109701074A (zh) * | 2018-12-29 | 2019-05-03 | 广州贝奥吉因生物科技有限公司 | 一种骨修复支架及其制备方法 |
Non-Patent Citations (3)
| Title |
|---|
| ANASANTOVEÑA等: "《Structure-Performance Relationships of Temperature-Responsive PLGA -PEG -PLGA Gels for Sustained Release of Bone Morphogenetic Protein-2》", 《JOURNAL OF PHARMACEUTICAL SCIENCES》 * |
| 马小草等: "《关于金纳米粒子在骨组织再生中作用的研究进展》", 《口腔颌面修复学杂志》 * |
| 高筱萌等: "《生物纳米材料在骨组织工程中的研究进展》", 《口腔医学研究》 * |
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