CN101756904A - 壳聚糖微球制备工艺 - Google Patents
壳聚糖微球制备工艺 Download PDFInfo
- Publication number
- CN101756904A CN101756904A CN200810154879A CN200810154879A CN101756904A CN 101756904 A CN101756904 A CN 101756904A CN 200810154879 A CN200810154879 A CN 200810154879A CN 200810154879 A CN200810154879 A CN 200810154879A CN 101756904 A CN101756904 A CN 101756904A
- Authority
- CN
- China
- Prior art keywords
- matrine
- magnetic
- preparation
- magnetic fluid
- preparation process
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
Abstract
本发明公开了一种苦参碱磁性壳聚糖微球制备工艺，其特征在于应用化学沉淀法制备磁流体，应用离子凝聚法制备苦参碱磁性壳聚糖微球，微球粒径呈正态分布，且分布均匀。制备过程未引入有毒的试剂，未产生不必要的影响。属于医药技术领域。
Description
技术领域
本发明涉及苦参碱磁性壳聚糖微球的制备工艺，属于医药技术领域。
背景技术
苦参碱(matrine)是广泛存在于豆科植物苦参，苦豆子及广豆根中的四环喹诺里西啶类生物碱，对肿瘤有抑制作用。
磁靶向给药系统(magnetic targeting drug delivery system，MTDDS)是近年来研究的一类新型靶向药物传递系统，属于第四代给药系统--靶向给药系统，目前国内外研究尚处于起步阶段。该系统系将药物和磁性物质与适当的载体材料制成稳定体系，在一定强度的外磁场作用下，使药物定位于靶区，浓集并释放，从而在病变部位发挥疗效，具有高效、速效、低毒的特点[1]。该系统克服了同一代的脂质体、纳米粒、微球等靶向给药系统的缺点和不足，可以靶向定位释药，很大程度上避免了药物被网状内皮系统(RES)的巨噬细胞吞噬，实现了主动靶向给药，是抗肿瘤治疗的理想剂型。此外，MTDDS还有不易被RES吞噬、载药量大、磁响应性好等优点。作为药物靶向应用的新载体，可采用生物可降解的高分子聚合物如壳聚糖、聚乳酸、白蛋白等作为靶向给药的载体，将药物包裹或嵌入，制备出载药的微球。根据其直径大小不同，可以被肺、肝、肾、脾等截留，从而实现生物物理靶向作用，用于各种实体癌，如肝癌、肺癌、食道癌、胃癌、宫颈癌等的治疗。
发明内容
为了克服现有技术的不足，本发明的目的在于提供一种苦参碱磁性壳聚糖微球制备工艺。
本发明是通过以下技术方案来实现的：苦参碱磁性壳聚糖微球制备工艺，其特征在于包括以下步骤：
磁流体的制备：准确称取0.01mol(2.703g)FeCl3.6H2O，0.005moL(0.995g)FeCl2.4H2O(即摩尔比2∶1)，放入500mL三颈烧瓶中，加入200mL二次蒸馏水溶解并水浴加热至40℃，在超声与搅拌条件下滴加新制2moL/L NaOH至pH＝11，陈化30min，用注射器在5min内滴入5mL油酸，保温反应2h后用0.5mol/L HCl调节pH＝7，用蒸馏水反复冲洗，并以1000r/min的速度离心10min除去较大颗粒，就得到稳定的磁流体。
载药苦参碱磁性微球的制备：分别用醋酸溶液配制4mg/mL壳聚糖溶液，用蒸馏水配制1mg/mL多聚磷酸盐，取壳聚糖溶液10mL，加入0.67mL磁流体和0.1g苦参碱，在1000r/min搅拌下，将5mL多聚磷酸盐注入到壳聚糖溶液中，搅拌、分离、干燥即得载药苦参碱磁性微球。
本发明的有益效果是：本发明采用离子凝聚法制备苦参碱磁性壳聚糖微球，其过程由静电引发物理交联反应，避免在化学交联过程中引入有毒的试剂，未产生不必要的影响，获得的微球具有强靶向，生物可降解性。
附图说明
图1为磁流体粒径和粒径分布图；
图2为磁性微球粒径和粒径分布图
具体实施方式
下面将详细说明本发明的具体实施方式：
1、仪器与试剂：
仪器：D-1型无级调速磁力搅拌器(巩义市英峪予华仪器厂)；Zetasizer-3000HSA激光粒度测试仪(英Malvern)；TDL-5离心机(上海安亭科学仪器厂)。
试剂
氯化铁(FeCl3.6H2O)、氯化亚铁(FeCl2.6H2O)(天津市大港亿中化工厂，分析纯)；壳聚糖(浙江玉环海洋生物公司，Mw90万，脱乙酰度92％)，多聚磷酸盐(TPP)，双蒸水，其余试剂均为分析纯。
2、实验及结果
磁流体的制备：准确称取0.01mol(2.703g)FeCl3.6H2O，0.005moL(0.995g)，FeCl2.4H2O，(即摩尔比2∶1)，放入500mL三颈烧瓶中，加入200mL二次蒸馏水溶解并水浴加热至40℃，在超声与搅拌条件下滴加新制2moL/L NaOH至pH＝11，陈化30min，用注射器在5min内滴入5mL油酸，保温反应2h后用0.5mol/L HCl调节pH＝7，用蒸馏水反复冲洗，并以1000r/min的速度离心10min除去较大颗粒，就得到稳定的磁流体。
载药苦参碱磁性微球的制备：分别用醋酸溶液配制4mg/mL壳聚糖溶液，用蒸馏水配制1mg/mL多聚磷酸盐，取壳聚糖溶液10mL，加入0.67mL磁流体和0.1g苦参碱，在1000r/min搅拌下，将5mL多聚磷酸盐注入到壳聚糖溶液中，搅拌、分离、干燥即得载药苦参碱磁性微球。
取一定量的磁流体和苦参碱磁性壳聚糖微球，超声分散后用Zetasizer 3000HSA激光粒度测试仪测试其粒径及其粒径分布，见图1和图2所示，磁流体的平均粒径为152.2nm，苦参碱磁性微球的平均粒径为682.4nm，粒径呈正态分布，且分布均匀。
以上已以较佳实施例公开了本发明，然其并非用以限制本发明，凡采用等同替换或者等效变换方式所获得的技术方案，均落在本发明的保护范围之内。
Claims (1)
1.苦参碱磁性壳聚糖微球制备工艺，其特征在于包括以下步骤：
(1)磁流体的制备：准确称取0.01mol(2.703g)FeCl3.6H2O，0.005moL(0.995g)FeCl2.4H2O(即摩尔比2∶1)，放入500mL三颈烧瓶中，加入200mL二次蒸馏水溶解并水浴加热至40℃，在超声与搅拌条件下滴加新制2moL/L NaOH至pH＝11，陈化30min，用注射器在5min内滴入5mL油酸，保温反应2h后用0.5mol/L HCl调节pH＝7，用蒸馏水反复冲洗，并以1000r/min的速度离心10min除去较大颗粒，就得到稳定的磁流体；
(2)载药苦参碱磁性微球的制备：分别用醋酸溶液配制4mg/mL壳聚糖溶液，用蒸馏水配制1mg/mL多聚磷酸盐，取壳聚糖溶液10mL，加入0.67mL磁流体和0.1g苦参碱，在1000r/min搅拌下，将5mL多聚磷酸盐注入到壳聚糖溶液中，搅拌、分离、干燥即得载药苦参碱磁性微球。
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810154879A CN101756904A (zh) | 2008-10-27 | 2008-10-27 | 壳聚糖微球制备工艺 |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN200810154879A CN101756904A (zh) | 2008-10-27 | 2008-10-27 | 壳聚糖微球制备工艺 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101756904A true CN101756904A (zh) | 2010-06-30 |
Family
ID=42488390
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN200810154879A Pending CN101756904A (zh) | 2008-10-27 | 2008-10-27 | 壳聚糖微球制备工艺 |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101756904A (zh) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104004744A (zh) * | 2014-06-12 | 2014-08-27 | 江南大学 | 一种制备具有缓释效果的固定化葡萄糖氧化酶的方法 |
| CN104689374A (zh) * | 2015-03-26 | 2015-06-10 | 福州大学 | 一种有机/无机双相杂化靶磁性载中药复合微球 |
| CN104689375A (zh) * | 2015-03-26 | 2015-06-10 | 福州大学 | 一种双重原位杂化制备的具有磁响应性多重梯度载药微球 |
-
2008
- 2008-10-27 CN CN200810154879A patent/CN101756904A/zh active Pending
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104004744A (zh) * | 2014-06-12 | 2014-08-27 | 江南大学 | 一种制备具有缓释效果的固定化葡萄糖氧化酶的方法 |
| CN104689374A (zh) * | 2015-03-26 | 2015-06-10 | 福州大学 | 一种有机/无机双相杂化靶磁性载中药复合微球 |
| CN104689375A (zh) * | 2015-03-26 | 2015-06-10 | 福州大学 | 一种双重原位杂化制备的具有磁响应性多重梯度载药微球 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| Zhang et al. | Metal–organic-framework-supported immunostimulatory oligonucleotides for enhanced immune response and imaging | |
| Gao et al. | Preparation of anti-CD40 antibody modified magnetic PCL-PEG-PCL microspheres | |
| Ma et al. | Cancer theranostic nanoparticles self-assembled from amphiphilic small molecules with equilibrium shift-induced renal clearance | |
| García-Jimeno et al. | Magnetoliposomes prepared by reverse-phase followed by sequential extrusion: Characterization and possibilities in the treatment of inflammation | |
| Liang et al. | pH‐responsive nanoparticles loaded with graphene quantum dots and doxorubicin for intracellular imaging, drug delivery and efficient cancer therapy | |
| Tang et al. | The effect of cryoprotection on the use of PLGA encapsulated iron oxide nanoparticles for magnetic cell labeling | |
| CN103980506B (zh) | 一种基于聚乳酸–聚乙二醇嵌段共聚物的磁性微球的制备方法 | |
| Zhou et al. | Magnetic tumor targeting of β-glucosidase immobilized iron oxide nanoparticles | |
| Chen et al. | Study of Fe3O4–PLLA–PEG–PLLA magnetic microspheres based on supercritical CO2: Preparation, physicochemical characterization, and drug loading investigation | |
| Bian et al. | Preparation and study on anti-tumor effect of chitosan-coated oleanolic acid liposomes | |
| Tian et al. | Paclitaxel-loaded magnetic nanoparticles: synthesis, characterization, and application in targeting | |
| Shen et al. | Polyphosphoester-based cationic nanoparticles serendipitously release integral biologically-active components to serve as novel degradable inducible nitric oxide synthase inhibitors | |
| CN101756904A (zh) | 壳聚糖微球制备工艺 | |
| Sivakumar et al. | Chitosan capped nanoscale Fe-MIL-88B-NH2 metal-organic framework as drug carrier material for the pH responsive delivery of doxorubicin | |
| Israel et al. | Ultrasound-mediated surface engineering of theranostic magnetic nanoparticles: an effective one-pot functionalization process using mixed polymers for siRNA delivery | |
| Zhu et al. | Targeted therapeutic effects of oral magnetically driven pectin nanoparticles containing chlorogenic acid on colon cancer | |
| Nagura et al. | Preparation of Robust Metal‐Free Magnetic Nanoemulsions Encapsulating Low‐Molecular‐Weight Nitroxide Radicals and Hydrophobic Drugs Directed Toward MRI‐Visible Targeted Delivery | |
| Chen et al. | Preparation and antitumor effect evaluation of composite microparticles co-loaded with siRNA and paclitaxel by a supercritical process | |
| CN101697962A (zh) | 苦参碱磁性壳聚糖微球制备工艺 | |
| CN100386080C (zh) | 汉防己甲素固体脂质纳米粒及其制备方法 | |
| CN100362984C (zh) | 一种苦参碱磁性微球的制备方法 | |
| Alpdemir et al. | Magnetically responsive, sorafenib loaded alginate microspheres for hepatocellular carcinoma treatment | |
| CN105434355B (zh) | 一种Fe3O4磁性尼莫地平脂质体及其制备方法 | |
| Liu et al. | Physiochemical properties and paclitaxel release behaviors of dual-stimuli responsive copolymer-magnetite superparamagnetic nanocomposites | |
| Li et al. | Micellization of antineoplastic agent to significantly upregulate efficacy and security |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C06 | Publication | ||
| PB01 | Publication | ||
| DD01 | Delivery of document by public notice |
Addressee: Cao Cuizhen Document name: Notification of Publication of the Application for Invention |
|
| DD01 | Delivery of document by public notice |
Addressee: Cao Cuizhen Document name: Notification of before Expiration of Request of Examination as to Substance |
|
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20100630 |