喷雾干燥的固体脂质纳米颗粒用于提高柏柏林的生物可用性通过口服
Van Hong Nguyen1, Khoa Nguyen Manh Le2, Mai Chau Ngoc Nguyen3
1Department of Life Sciences, Vietnam Academy of Science and Technology, University of Science and Technology of Hanoi, 18- Hoang Quoc Viet, Cau Giay, Hanoi, Vietnam.
Current pharmaceutical design
|November 14, 2023
概括
固体脂质纳米颗粒 (SLN) 增强了传统药物柏柏林 (BBR) 的口服生物可用性. 这种新型药物输送系统在治疗糖尿病和高血压等慢性疾病方面表现有前途.
科学领域:
- 制药科学 制药科学
- 纳米技术 纳米技术
- 药物输送系统 药物输送系统
背景情况:
- 柏柏林 (BBR) 对包括糖尿病,高脂血症,高血压和阿尔茨海默病在内的慢性疾病具有治疗潜力.
- BBR的低口服生物可用性限制了其治疗应用.
- 固体脂质纳米颗粒 (SLN) 提供了一种改善BBR吸收和全身循环的策略.
研究的目的:
- 准备和表征含有柏柏林的固体脂质纳米粒子 (BBR-SLNs).
- 评估BBR-SLNs作为口服药物递送系统的潜力.
- 评估BBR-SLNs的物理化学特性,体外释放和细胞毒性.
主要方法:
- 使用超声波和喷雾干燥来制备BBR-SLN.
- 使用动态光散射 (DLS) 和扫描电子显微镜 (SEM) 分析了粒子大小和形态.
- 评估了封装效率,负载能力,稳定性,体外释放和细胞毒性.
主要成果:
- BBR-SLN表现出低于200nm的均质颗粒大小,具有高封装效率 (~90%) 和负载能力 (>12%).
- 喷雾干燥的BBR-SLN粉末在30天内表现出良好的再分散性和稳定性.
- 喷雾干燥的BBR-SLNs在24小时内持续在体外释放,没有显著的细胞毒性,在HEK293细胞中增加了细胞活力.
结论:
- 固体脂质纳米颗粒 (SLN) 是一个有前途的药物输送系统,可以增强Berberine的口服.
- 开发的BBR-SLNs改善了BBR的物理化学特性和释放特征.
- 这种方法可以扩大柏柏林在各种慢性疾病的治疗应用.
相关概念视频
Factors Affecting Dissolution: Particle Size and Effective Surface Area
860
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
860
Routes of Drug Administration: Enteral
3.7K
Medications can be administered through the enteral route using liquids, capsules, or tablets.
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
Enteral administration involves drug administration via the mouth in two ways: orally or sublingually.
Unlike sublingually drugs, drugs that are taken orally pass through the gastrointestinal (GI) tract and get metabolized by the liver. Once metabolized, the drug is absorbed into the systemic circulation, reaching different body parts via the bloodstream. However, while passing through the stomach,...
3.7K
Factors Influencing Drug Absorption: Presystemic Elimination
233
The pharmacokinetic journey of oral drugs begins with a crucial first pass through the hepatic portal system, called the first-pass effect. This first pass significantly impacts bioavailability — the proportion of a drug that enters systemic circulation and is available for therapeutic action. The primary route sees the drug absorbed by intestinal membranes and then shunted to the liver via the hepatic portal vein. Here, pre-systemic elimination occurs as drugs face metabolism or biliary...
233
Drug Delivery: Enteral Route
468
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.
468
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
209
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
209
Biopharmaceutics and Pharmacokinetics: Overview
2.1K
Understanding drugs, drug products, and their performance in pharmaceutical science is pivotal. Drugs, whether simple molecules or complex compounds, are designed to interact with the body's biological systems to diagnose, treat, or prevent diseases. Drug products include various delivery systems such as tablets, capsules, injections, and inhalers. The performance of these drug products is gauged by their ability to deliver the active ingredient to the desired site of action at the...
2.1K


