Entrapment and release difference resulting from hydrogen bonding interactions in niosome.
In this study the influence of hydrogen bonding interaction between niosomal membrane and solutes on the drug loading and release was investigated. Salicylic acid (SA) and p-hydroxyl benzoic acid (p-BA) were selected as models. Niosomes were prepared with 1:1 molar ratios of various surfactants and cholesterol by film hydration technique, and the corresponding formulation variables were optimized to achieve the maximum entrapment efficiencies (EE%). The EE% of different formulations followed the trend Span 60>Span 40>Span 20>Span 80. Additionally, it was also found that the EE% of p-BA was much higher than that of SA. This difference may be due to the formation of hydrogen bond between p-BA and niosomal membrane, and the corresponding interaction diagram has been proposed and confirmed indirectly by UV spectroscopy method. The quantitative analysis of hydrogen binding interaction between solutes and niosome has been finished firstly, and the corresponding entrapment equilibrium constant K has been calculated as well. Moreover, in vitro the release of both drugs from niosomes was examined in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF), respectively. The results indicated that the release of p-BA in SIF was much slower than that in SGF, and the release rate of SA in SGF is apparently slower than that in SIF. The possible mechanism was given as well.
Graduate University of Chinese Academy of Sciences, Beijing 100049, China. ymhao@gucas.ac.cn
Yong-Mei
YM
Hao
Ke'an
K
Li
D000042:Absorption; D002626:Chemistry, Pharmaceutical; D002784:Cholesterol / Q000737:chemistry*; D005750:Gastric Juice / Q000737:chemistry; D006860:Hydrogen Bonding; D008081:Liposomes; D046529:Microscopy, Electron, Transmission; D008954:Models, Biological; D015394:Molecular Structure; D010226:Parabens / Q000008:administration & dosage* / Q000737:chemistry; D010316:Particle Size; D004364:Pharmaceutical Preparations / Q000008:administration & dosage* / Q000737:chemistry; D020156:Salicylic Acid / Q000008:administration & dosage* / Q000737:chemistry; D012995:Solubility; D013056:Spectrophotometry, Ultraviolet; D013499:Surface Properties; D013501:Surface-Active Agents / Q000737:chemistry*
D008081:Liposomes; D010226:Parabens; D004364:Pharmaceutical Preparations; D013501:Surface-Active Agents; D002784:Cholesterol; C038193:4-hydroxybenzoic acid; D020156:Salicylic Acid