控制尺寸和形状的生物降解聚合物刷基于l-氨基酸用于细胞内药物输送和深层组织透
Utreshwar Arjun Gavhane1, Dheeraj Chandra Joshi1, Manickam Jayakannan1
1Department of Chemistry, Indian Institute of Science Education and Research (IISER Pune), Dr. Homi Bhabha Road, Pune 411008, Maharashtra, India.
Biomacromolecules
|May 7, 2024
概括
来自氨基酸的可生物降解聚合物刷显示了增强的深层组织透和更快的细胞吸收. 棒形刷子在药物输送方面优于球形刷子,展示了作为先进药物载体的潜力.
科学领域:
- 生物材料科学 生物材料科学
- 聚合物化学 聚合物化学
- 纳米技术纳米技术
背景情况:
- 开发先进的药物输送系统对于提高治疗疗效至关重要.
- 可生物降解和生物相容的材料在生物医学应用中非常受欢迎.
- 控制聚合物架构是优化材料性能的关键.
研究的目的:
- 从l-氨基酸生物资源合成和表征大小和形状控制的聚合物刷.
- 研究聚合物拓对酶生物降解和深层组织透的影响.
- 评估这些聚合物刷子作为药物输送支架的潜力.
主要方法:
- 基于l-tyrosine的甲基功能化单体的定制合成.
- 没有溶剂的融化聚凝和后聚合点击化学.
- 制造1D棒形和3D球形两型聚合物刷.
- 在体外和体内研究,包括细胞成像和动物生物成像 (IVIS).
主要成果:
- 合成的无毒,无血溶性聚合物刷,能够装载多克索鲁比和IR-780.
- 与球形刷子相比,棒状的聚合物刷子在内分泌体区内表现出优异的细胞吸收和更快的生物降解.
- 在体内研究证实了IR-780装载的棒状聚合物刷的高效深层组织透.
- 聚合物刷在血中表现出良好的稳定性,并在消化器官中优先积累,对重要器官的毒性低.
结论:
- 聚合物刷子拓显著影响生物活动,包括生物降解和组织透.
- 生物衍生和可生物降解的聚合物刷子为下一代智能药物输送提供了一个有前途的平台.
- 聚合物刷的受控合成使其能够为特定的生物医学应用提供量身定制的特性.
相关概念视频
Bioavailability Enhancement: Drug Permeability Enhancement
314
After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt secretion,...
314
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
313
Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
313
Modified-Release Drug Delivery Systems: Stimuli-Activated
140
Stimuli-activated drug delivery systems are designed to release drugs in response to specific physical, chemical, or biological stimuli. These systems often utilize hydrogels—three-dimensional, hydrophilic polymer networks capable of swelling in aqueous environments and retaining significant fluid volumes. Upon exposure to particular stimuli, these hydrogels undergo structural transitions that allow the embedded drug to be released. Due to this adaptive behavior, such systems are also...
140
Modified-Release Drug Delivery Systems: Site-Targeted
141
Site-targeted drug delivery systems enhance therapeutic efficacy while minimizing systemic toxicity and treatment costs. Unlike conventional methods, these systems ensure precise drug delivery, improving bioavailability and reducing side effects. Targeted drug delivery is classified into three levels. First-order targeting directs drugs to the capillary beds of specific organs or tissues. Second-order targets specific cell types, such as tumor cells, using receptor-mediated interactions.
141
Site-Targeted Drug Delivery Systems: Polymeric Carriers
127
Polymeric carriers enhance targeted drug delivery by increasing efficacy while minimizing off-target effects. These carriers comprise a biodegradable polymeric backbone integrated with functional elements that enable targeting, improve physicochemical properties, and regulate drug release.Targeting MechanismsThe targeting ability of polymeric carriers is mediated by a homing device, which is a molecular recognition component designed to selectively bind to specific tissues or cells. Monoclonal...
127
Oral Drug Delivery Systems: Delayed-Release Systems
180
Delayed-release drug delivery systems are specialized pharmaceutical formulations designed to postpone the release of active compounds until the drug reaches a specific region of the gastrointestinal (GI) tract, typically the intestine. These systems are essential for drugs that may cause gastric irritation, are unstable in acidic environments, or need to exert therapeutic effects locally in the intestinal or colonic regions.The core feature of delayed-release systems is the use of enteric...
180


