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Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
Published on: August 31, 2019
Entrapment and release difference resulting from hydrogen bonding interactions in niosome
1Graduate University of Chinese Academy of Sciences, Beijing 100049, China. ymhao@gucas.ac.cn
International Journal of Pharmaceutics
|October 26, 2010
Summary
Hydrogen bonding significantly impacts drug loading and release from niosomes. Parahydroxybenzoic acid (p-BA) shows higher entrapment and slower release in intestinal fluid compared to salicylic acid (SA).
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery Systems
- Physical Chemistry
Background:
- Niosomes are non-ionic surfactant vesicles used for drug delivery.
- Drug loading and release kinetics are crucial for niosome efficacy.
- Interactions between drug molecules and the niosomal membrane influence formulation performance.
Purpose of the Study:
- To investigate the role of hydrogen bonding between niosomal membranes and model drugs (salicylic acid and p-hydroxyl benzoic acid) on drug loading and release.
- To optimize niosome formulations for maximum entrapment efficiency.
- To quantitatively analyze hydrogen bonding interactions and their impact on drug release profiles.
Main Methods:
- Niosomes were prepared using various surfactants and cholesterol via the film hydration technique.
- Entrapment efficiency (EE%) was optimized for different formulations.
- UV spectroscopy was employed to confirm hydrogen bonding interactions and calculate the entrapment equilibrium constant (K). In vitro drug release studies were conducted in simulated gastric and intestinal fluids.
Main Results:
- Entrapment efficiency followed the order: Span 60 > Span 40 > Span 20 > Span 80.
- Parahydroxybenzoic acid (p-BA) exhibited significantly higher EE% than salicylic acid (SA), attributed to hydrogen bonding.
- Drug release profiles varied: p-BA release was slower in simulated intestinal fluid (SIF) than in simulated gastric fluid (SGF), while SA release was slower in SGF than in SIF.
Conclusions:
- Hydrogen bonding plays a critical role in the entrapment efficiency of solutes within niosomes.
- The differential release rates of SA and p-BA are influenced by their interaction with the niosomal membrane and the physiological environment (SGF vs. SIF).
- This study provides a quantitative understanding of solute-niosome interactions, aiding in the rational design of niosomal drug delivery systems.
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