聚乙二醇羟基乙酸—壳聚糖微粒共传递蒿甲醚和胡椒碱增强缓释
发布时间：2021-08-31 22:48
疟疾是一种恶性寄生虫病,通过疟原虫这一特殊种类的生物进行传播,其中恶性疟原虫（PF）是主要的传播疟疾的单细胞寄生虫,而蚊子能够将PF快速带入血液,进而感染肝细胞和血细胞。由于这种传染性,致使人引发多种病症甚至死亡。因此,疟疾是一种严重的疾病。蒿甲醚,一种高效的抗疟疾药物,具有治愈感染P.F.患者的潜力。然而,它的治疗功效和临床应用受其生物利用度差,半衰期短和快速降解等因素的限制。这些限制可以通过与天然生物增强剂如胡椒碱的组合来解决。本文中,我们通过将胡椒碱与聚乙二醇-共-羟基乙酸（PLGA）和基于壳聚糖的核-壳微粒包封在一起来克服蒿甲醚药物的局限性。本研究使用同轴电喷雾（CES）系统,该系统已被确立为开发核-壳微粒的有效策略,来制备微粒。通过优化的工艺参数,以高封装效率（75.6%和78.8%）制备蒿甲醚-胡椒碱负载的PLGA-壳聚糖微粒（AP-PLGA-C5）和蒿甲醚-胡椒碱负载的PLGA微粒（AP-PLGA）,平均尺寸为2.2和1.7μm,其中载药量（LE）分别9.7%和9.4%,且能够持续释放。此外,XRD和DSC结果表明,当通过CES方法包封在微粒中时,蒿甲醚和胡椒碱转变为无定...
【文章来源】：中国科学技术大学安徽省 211工程院校 985工程院校
【文章页数】：114 页
【学位级别】：硕士
【文章目录】：
Abstract
摘要
Glossary of Abbreviations
Chapter 1. Introduction
1.1 Malaria
1.2 History
1.3 Transmission and Life Cycle of Malaria
1.4 Symptoms and Complications
1.5 Malaria Diagnosis
1.5.1 Clinical Diagnosis
1.5.2 Laboratory Diagnosis
1.6 Conventional Treatment for Malaria
1.7 Nanomedicine Treatment for Malaria
1.8 Artemisinin and its derivatives
1.8.1 Artemether
1.8.2 Chemistry and Structure of Artemether and Fast Facts
1.8.3 Mechanism of Artemether Action
1.8.4 Pharmacokinetics of Drug
1.8.5 Recommended Dosage and Side Effects
1.8.6 Artemether Interaction in Human Body
1.8.7 Available Forms and Restrictions/Disadvantages
Chapter 2. Bioenhancer
2.1 Introduction
2.2 The concept of Bioavailability Enhancers
2.3 History of Bioenhancers
2.4 Piperine
2.4.1 Properties of Piperine
2.4.2 Antioxidant activity
2.4.3 Bioenhancing Ability
2.5 Advantages of Using Piperine as Bioenhancer
2.5.1 Proposed Mechanism for Bio enhancing Effect
2.6 Biodegradable Polymer
2.6.1 Poly lactic-co-glycolic Acid (PLGA)
2.6.2 Pharmacokinetic of PLGA
2.6.3 Chitosan
2.6.4 General properties of chitosan
Chapter 3. Electrospray System
3.2 Introduction
3.3 Principle of Electrospray
3.3.1 Single Axial Electrospray
3.3.2 Coaxial Electrospray System
3.4 Electrospray Modes
3.5 The Taylor Cone jet Mode Stability
3.6 Process Parameters of Coaxial Electrospray System
3.7 Effect of Applied Voltages on Stable Cone-Jet
3.8 Effect of Flow Rates on Stable Cone jet
3.9 Components of the Electrospray System
3.10 Electrified Droplet Concept & Identification of Morphology
3.11 Properties of Liquids
3.11.1 Electrokinetics of Liquids
3.11.2 Electrical Permittivity
3.11.3 Interfacial Tension and Surface Tension
3.11.4 Viscosity
3.11.5 Liquid concentration
3.11.6 Scaling law
Chapter 4. Experimental Study
4.1 Introduction
4.2 Materials and Methods
4.2.1 Materials
4.2.2 Experimental Setup
4.3 Morphological characterization
4.3.1 Morphology and Size Distribution Analysis
4.3.2 Core-Shell Structured Evaluation
4.3.3 Thermal Analysis
4.3.4 Crystallinity using X-ray diffractometer
4.3.5 UPLC Analysis
4.3.6 Drug Encapsulation Efficiency (EE%)and Loading Rate (LR%)
4.3.7 In Vitro Drug Release
4.3.8 Cell Culture and Maintenance
4.3.9 Evaluation of Cytotoxicity
4.4 RESULTS AND DISCUSSION
4.4.1 Fabrication of AP-PLGA and AP-PLGA-CS Microparticles
4.4.2 Preparation of Inner and Outer solutions
4.4.3 Characterization of AP-PC Microparticles and AP-P Microparticles
4.4.4 Core-shell structure formation and verification of AP-PLGA and AP-PLGA-CSMicroparticles
4.4.5 XRD Analysis of AP-PC and AP-P Microparticles
4.4.6 DSC measurements on AP-PLGA and AP-PLGA-CS microparticles
4.4.7 Encapsulation Efficiency and Cytotoxicity
4.4.8 In Vitro Release profile of AP-PLGA and AP-PLGA-CS Microparticles
Chapter 5. Conclusion and Future Work
5.1 Summary
List of References
Acknowledgements
【参考文献】：
期刊论文
[1]胡椒碱抗实验性胃溃疡的作用(英文)[J]. 白音夫,旭红. Acta Pharmacologica Sinica. 2000(04)
[2]THE INFECTIVITY OF GAMETOCYTES OF PLASMODIUM FALCIPARUM FROM PATIENTS TREATED WITH ARTEMISININ[J]. 陈沛泉,李国桥,郭兴伯,何坤荣,符永新,符林春,宋玉宗. Chinese Medical Journal. 1994(09)
本文编号：3375762
【文章来源】：中国科学技术大学安徽省 211工程院校 985工程院校
【文章页数】：114 页
【学位级别】：硕士
【文章目录】：
Abstract
摘要
Glossary of Abbreviations
Chapter 1. Introduction
1.1 Malaria
1.2 History
1.3 Transmission and Life Cycle of Malaria
1.4 Symptoms and Complications
1.5 Malaria Diagnosis
1.5.1 Clinical Diagnosis
1.5.2 Laboratory Diagnosis
1.6 Conventional Treatment for Malaria
1.7 Nanomedicine Treatment for Malaria
1.8 Artemisinin and its derivatives
1.8.1 Artemether
1.8.2 Chemistry and Structure of Artemether and Fast Facts
1.8.3 Mechanism of Artemether Action
1.8.4 Pharmacokinetics of Drug
1.8.5 Recommended Dosage and Side Effects
1.8.6 Artemether Interaction in Human Body
1.8.7 Available Forms and Restrictions/Disadvantages
Chapter 2. Bioenhancer
2.1 Introduction
2.2 The concept of Bioavailability Enhancers
2.3 History of Bioenhancers
2.4 Piperine
2.4.1 Properties of Piperine
2.4.2 Antioxidant activity
2.4.3 Bioenhancing Ability
2.5 Advantages of Using Piperine as Bioenhancer
2.5.1 Proposed Mechanism for Bio enhancing Effect
2.6 Biodegradable Polymer
2.6.1 Poly lactic-co-glycolic Acid (PLGA)
2.6.2 Pharmacokinetic of PLGA
2.6.3 Chitosan
2.6.4 General properties of chitosan
Chapter 3. Electrospray System
3.2 Introduction
3.3 Principle of Electrospray
3.3.1 Single Axial Electrospray
3.3.2 Coaxial Electrospray System
3.4 Electrospray Modes
3.5 The Taylor Cone jet Mode Stability
3.6 Process Parameters of Coaxial Electrospray System
3.7 Effect of Applied Voltages on Stable Cone-Jet
3.8 Effect of Flow Rates on Stable Cone jet
3.9 Components of the Electrospray System
3.10 Electrified Droplet Concept & Identification of Morphology
3.11 Properties of Liquids
3.11.1 Electrokinetics of Liquids
3.11.2 Electrical Permittivity
3.11.3 Interfacial Tension and Surface Tension
3.11.4 Viscosity
3.11.5 Liquid concentration
3.11.6 Scaling law
Chapter 4. Experimental Study
4.1 Introduction
4.2 Materials and Methods
4.2.1 Materials
4.2.2 Experimental Setup
4.3 Morphological characterization
4.3.1 Morphology and Size Distribution Analysis
4.3.2 Core-Shell Structured Evaluation
4.3.3 Thermal Analysis
4.3.4 Crystallinity using X-ray diffractometer
4.3.5 UPLC Analysis
4.3.6 Drug Encapsulation Efficiency (EE%)and Loading Rate (LR%)
4.3.7 In Vitro Drug Release
4.3.8 Cell Culture and Maintenance
4.3.9 Evaluation of Cytotoxicity
4.4 RESULTS AND DISCUSSION
4.4.1 Fabrication of AP-PLGA and AP-PLGA-CS Microparticles
4.4.2 Preparation of Inner and Outer solutions
4.4.3 Characterization of AP-PC Microparticles and AP-P Microparticles
4.4.4 Core-shell structure formation and verification of AP-PLGA and AP-PLGA-CSMicroparticles
4.4.5 XRD Analysis of AP-PC and AP-P Microparticles
4.4.6 DSC measurements on AP-PLGA and AP-PLGA-CS microparticles
4.4.7 Encapsulation Efficiency and Cytotoxicity
4.4.8 In Vitro Release profile of AP-PLGA and AP-PLGA-CS Microparticles
Chapter 5. Conclusion and Future Work
5.1 Summary
List of References
Acknowledgements
【参考文献】：
期刊论文
[1]胡椒碱抗实验性胃溃疡的作用(英文)[J]. 白音夫,旭红. Acta Pharmacologica Sinica. 2000(04)
[2]THE INFECTIVITY OF GAMETOCYTES OF PLASMODIUM FALCIPARUM FROM PATIENTS TREATED WITH ARTEMISININ[J]. 陈沛泉,李国桥,郭兴伯,何坤荣,符永新,符林春,宋玉宗. Chinese Medical Journal. 1994(09)
本文编号：3375762
本文链接：https://www.wllwen.com/yixuelunwen/yiyaoxuelunwen/3375762.html
最近更新
教材专著
