抗癌薬の溶解強化のための単一および混合ミセラ環境におけるポリオキシエチレン (POE) ベースの非離子表面活性剤の物理化学的特徴付け
Virendra Prajapati1, Yashika Tomar2, Gautam Singhvi2
1Department of Chemistry, Sardar Vallabhbhai National Institute of Technology (SVNIT), Ichchhanath Dumas Road, Keval Chowk, Surat-395007, Gujarat, India. ketankuperkar@gmail.com.
Physical chemistry chemical physics : PCCP
|September 5, 2025
まとめ
この研究では,Soluplus®と他の表面活性物質を用いてナノスケールのミセル形成を調査し,薬物溶解と制御された放出を促進するシナージ効果を明らかにしました. Soluplus®を研究した結果
科学分野:
- コロイドと表面科学
- 材料科学
- 医薬品科学
背景:
- Soluplus®のようなアンフィフィリック・グラフト・コポリマーは 溶解性の低い薬剤の製剤に不可欠です
- 単一および混合サーファクタントのシステムにおけるミセラ行動を理解することは,薬物投与アプリケーションの鍵です.
- ポリオキシエチレン (POE) ベースの非離子表面活性剤は,濃度と温度によって異なる溶液特性を示します.
研究 の 目的:
- 様々なPOEベースの非イオン表面活性剤と組み合わせたSoluplus®のナノスケールミセラ形成と溶液の振る舞いを調査する.
- 表面活性剤の混合がミセル形態学,安定性,薬剤溶解能力に与える影響を特徴づける.
- これらのナノスケールシステムからクエルセチン (QCT) の薬物放出運動を*in vitro*で評価する.
主な方法:
- 溶液の粘度および粘弾性特性を決定するレオロギー測定.
- ダイナミック・ライト・スキャタリング (DLS) とスモール・アングル・ニュートロン・スキャタリング (SANS) を用いてミセルサイズと形状の分析を行う.
- クエルセチンの溶解度 (QCT) を定量化するための紫外線可視 (UV-vis) スペクトロスコーピー.
主要な成果:
- Soluplus®は大きな球状のミセルを形成し,P123は熱可逆の凝結と形態学的移行を示しています.
- 混合 Soluplus® システムは,シネジスティックな相互作用を示し,雲点を大幅に増加させ,QCT の溶解性を高めます.
- ヒグチモデルは,拡散制御メカニズムを示し,薬物の放出を*in vitro*で最もよく記述した.
結論:
- Soluplus®ベースの混合ミセラーシステムは,QCTのような水性薬の優れた溶解と制御された放出を提供します.
- 特定のSoluplus®混合物における相乗効果は,製薬剤の開発に有利である.
- これらのナノスケールアセンブリは,遠水性活性薬剤の配送を強化するための有望なプラットフォームを提供します.
関連する概念動画
01:21Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.9K
Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.9K
01:23Factors Affecting Dissolution: Particle Size and Effective Surface Area
1.0K
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...
1.0K
03:22Colloids
17.9K
Children at play often make suspensions such as mixtures of mud and water, flour and water, or a suspension of solid pigments in water known as tempera paint. These suspensions are heterogeneous mixtures composed of relatively large particles that are visible to the naked eye or can be seen with a magnifying glass. They are cloudy, and the suspended particles settle out after mixing. On the other hand, a solution is a homogeneous mixture in which no settling occurs and in which the dissolved...
17.9K
03:00Solubility
18.2K
Solution, Solubility, and Solubility Equilibrium
A solution is a homogeneous mixture composed of a solvent, the major component, and a solute, the minor component. The physical state of a solution—solid, liquid, or gas—is typically the same as that of the solvent. Solute concentrations are often described with qualitative terms such as dilute (of relatively low concentration) and concentrated (of relatively high concentration).
In a solution, the solute particles (molecules,...
A solution is a homogeneous mixture composed of a solvent, the major component, and a solute, the minor component. The physical state of a solution—solid, liquid, or gas—is typically the same as that of the solvent. Solute concentrations are often described with qualitative terms such as dilute (of relatively low concentration) and concentrated (of relatively high concentration).
In a solution, the solute particles (molecules,...
18.2K
01:22Factors Influencing Drug Absorption: Physicochemical Parameters
425
The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
425
01:20Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
258
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...
258