热敏聚氨基水凝作为梅洛西卡姆输送的潜在载体
Ioana-Alexandra Plugariu1, Luiza Madalina Gradinaru1, Mihaela Avadanei1
1"Petru Poni" Institute of Macromolecular Chemistry, 41-A Grigore Ghica Voda Alley, 700487 Iasi, Romania.
Pharmaceuticals (Basel, Switzerland)
|November 25, 2023
概括
新的聚氨水凝有效地提供非类固醇抗炎药物 (NSAID) 梅洛西卡姆 (MX). 这些先进的药物载体显示出对疼痛和炎症的控制释放有希望.
科学领域:
- 材料科学 材料科学 材料科学
- 聚合物化学 聚合物化学
- 制药科学 制药科学
背景情况:
- 梅洛西卡姆 (MX) 是一种广泛使用的非类固醇抗炎药物 (NSAID),用于治疗疼痛,炎症和发烧.
- 目前的NSAID药物输送系统在控制和持续释放方面面临挑战.
- 基于聚氨 (PU) 的水凝由于其可调节的特性,具有作为新型药物输送平台的潜力.
研究的目的:
- 开发和描述含有梅洛西卡姆 (MX) 的热敏聚氨 (PU) 基水凝.
- 为了研究准备的水凝配方的风学和粘弹性特性.
- 评估PU水凝中的梅洛西卡姆体外药物释放动力学和机制.
主要方法:
- 制备含有各种辅料 (PEG,PVP,HPC,精油) 的热敏PU水凝.
- 液凝性质的表征,包括小胞体大小,泽塔潜力和风湿学.
- 在24-48小时和长达2周的时间内,在pH6和37°C的水凝中进行了体药物释放研究.
- 使用运输现象模型分析药物释放机制.
主要成果:
- 在37°C时,PU水凝的微粒大小约为35.8nm,随着MX负载而略微增加.
- 泽塔电位值在-10mV至-11.5mV之间,表明配方的稳定性.
- 在24-48小时内观察到显著的梅洛西卡姆释放 (60-80%),在2周内超过90%.
- 异常运输现象被确定为PU网络释放MX的主要机制.
结论:
- 以热敏PU为基础的水凝显示出有效的载荷和可控释放的 meloxicam.
- 开发的水凝显示了作为NSAIDs的替代载体的潜力,改善了药物输送.
- 需要进一步的研究来探索这些水凝用于先进的制药应用.
相关概念视频
01:19Modified-Release Drug Delivery Systems: Rate-Programmed II
Rate-programmed drug delivery systems release drugs in a controlled manner to maintain therapeutic levels. Three main designs include reservoir, matrix, and hybrid systems.Reservoir systems consist of a drug core enclosed within a membrane that controls drug release. In non-swelling reservoir systems, polymers like ethyl cellulose or polymethacrylates are used. These do not hydrate in aqueous media and control release through membrane thickness, porosity, or insolubility. This type includes...
01:23Modified-Release Drug Delivery Systems: Classification
Modified-release drug delivery systems improve drug efficacy and minimize side effects by controlling the rate and location of drug release. These systems fall into three categories: rate-programmed, stimuli-activated, and site-targeted.Rate-programmed systems release drugs at a predetermined rate, maintaining consistent therapeutic levels and reducing fluctuations that could lead to toxicity or subtherapeutic effects. These systems use polymeric matrices, reservoir-based designs, or osmotic...
01:30Modified-Release Drug Delivery Systems: Stimuli-Activated
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 called...
01:24Site-Targeted Drug Delivery Systems: Polymeric Carriers
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...
01:11Oral Drug Delivery Systems: Delayed-Release Systems
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...