通过超可变形膀载荷补丁增强皮肤间传递西利尼德:统计优化,表征和药物动力学评估
D Maheswara Reddy1, Mothilal M2
1SRM College of Pharmacy, SRM Institute of Science and Technology, Kattankulathur - 603203, Tamilnadu, India.
Pharmaceutical nanotechnology
|November 6, 2024
概括
这项研究开发了Cilnidipine (CND) 转基因补丁,以改善口服输送的限制. 通过皮肤贴片显示了增强的生物可用性和受控释放,为高血压管理提供了一个有希望的替代方案.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 纳米技术 纳米技术
背景情况:
- 奇利尼迪平 (CND) 是一种抗高血压药物,在口服中存在局限性,包括低生物可用性和不良反应.
- 通过皮肤递送药物提供了一种替代途径,以克服口服的挑战.
研究的目的:
- 开发和评估超可变形转基因组封装西利尼迪平 (CND) 的超可变形转基因组,用于通过皮肤补丁的配方.
- 通过一种新的通过皮肤递送系统,增强CND的生物可用性和治疗疗效.
主要方法:
- 通过薄膜水化方法,CND被封装在转基因组中.
- 使用Box Behnken设计优化了17种配方,评估了囊泡大小,PDI和EE%.
- 优化的配方被纳入了透皮贴片,随后进行了物理化学,体外/活体透,皮肤刺激和大鼠的药理动力学研究.
主要成果:
- 转基因组合表现出囊泡大小从185-401nm,EE%为63%-92%,以及-52到-20mV的泽塔潜力.
- 通过皮肤贴片显示,与普通贴片相比,CND透率显著改善,药物释放率更高 (85.7±1.5%) 并且没有皮肤刺激.
- 药理动力学研究显示,转移体补丁 (CTP-17) 的Cmax和AUC高于口服CND.
结论:
- 转移体补丁的CND代表了一个可行的和有效的策略,通过皮肤递送药物.
- 这种方法有可能改善,控制和长期管理高血压.
相关概念视频
Drug Delivery: Overview
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The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
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Drug Delivery: Miscellaneous Routes
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Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection, and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
329
Drug Delivery: Enteral Route
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The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
384
Factors Influencing Drug Absorption: Drug Dissolution
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The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
423
Non-Oral Extravascular Drug Absorption Routes
199
Non-oral extravascular routes, which encompass sublingual, buccal, topical, intramuscular, and inhalation methods, primarily utilize passive diffusion to transport drugs into the systemic circulation. The absorption rates and effectiveness of these routes depend on the drug's physicochemical properties, as well as the patient's anatomical and pathophysiological state.
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
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Methods for Studying Drug Absorption: In vitro
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In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
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