RSC Advances
·
2014
·Vol. 4
·期 82
·43392-43398
·
IF 3.708
Ying Cao,Lina Wang,Mingli He,Yanhua Zhang,Huajie Wang
Punicic acid belongs to one of conjugated linolenic acids isomers (CLnAs) and contains many outstanding functions related to human health such as anti-carcinogenic, anti-diabetes, anti-hyperlipidemia, anti-obesity and anti-atherosclerotic properties; moreover, interest in the punicic acid is growing. Note that since punicic acid is extremely susceptible to oxidation, antioxidants were often added to increase its stability. However, sometimes such method resulted in the great decrease of its antitumor activity. In addition, punicic acid is quite insoluble in water and only a minor fraction of it can be absorbed. Therefore, the present study aims to identify a method, which can maintain the cytotoxicity when there is an increase in the oxidative stability and solubility of punicic acid. In brief, free punicic acid was modified with glycerol and the amphiphilic monoglycerides of punicic acid were obtained, which were further dispersed to nanodispersions. Oxidative stability, cytotoxicity to NIH3T3 cells and digestion in intestinal juice of such nanodispersions under different conditions were studied. It was found that such nanodispersions showed higher oxidative stability, higher solubility in water. Most importantly, its cytotoxicity to NIH3T3 cells was also as strong as that of free punicic acid. Furthermore, since it can be hydrolyzed by pancreatin in intestinal juice, the nanodispersions formed by monoglycerides of punicic acid can be used as nutrient precursor of free punicic acid.
研究领域:
营养学
·
食品科学
·
生物化学
✓ 已验证
产品关联
DOI
高影响因子
International Journal of Nanomedicine
·
2025
·
IF 6.5
Dongyan Duan,Hua Xie,Jiayi Jiang,Ping Yang,Zhiyuan Guo,Xiaoqiang Guo,Xingyu Chen,Qian Yao
Purpose Most absorption enhancers boost the oral absorption of drugs via increasing intestinal permeability. However, they often damage intestinal mucosa and induce inflammatory reactions. The aim of this study is to synthesize a new absorption enhancer, punicic acid ethyl ester (PAEE), with excellent absorption-prompting effect and low toxicity.Methods The structure of PAEE was confirmed by NMR, MS, IR and UV. Setting oleic acid (OA) as the control, the three forms of punicic acid (PA), ie, free PA, PAEE, and pomegranate seed oil, in which PA exists in the form of triglyceride, were formulated into nanoemulsions (NE). The stability, physiochemical properties of the oils and NE were compared. The permeation-enhancing effect was estimated by phenol red intestinal transport experiments. The potential damage on small intestines was assessed by biochemical assay and pathological section.Results Though the three forms of PA had various strength in enhancing intestinal permeability, the difference was not significant (p > 0.05). Moreover, the effect was notably stronger than that of OA (p < 0.05) and was inversely related to the density and required HLB value of the oils. Compared to the corresponding oils, the NE exhibited much weaker effect in prompting intestinal permeability. Oral administration of OA and OA NE for 10 d impaired intestinal mucosa and villi along with strong inflammatory reactions in the small intestines. In contrast, the oils from PA series and their NE did not induce obvious intestinal inflammation. PAEE and its NE hindered the release of cytokines and increased the ratio of intestinal villus length to crypt depth.Conclusion PAEE is a promising absorption enhancer with a strong permeability-prompting effect and mucosa-protecting capacity against intestinal inflammation. It provides a practical strategy to enhance the bioavailability of the drugs with poor biological membrane penetration.
研究领域:
药学
·
生物医学
✓ 已验证
产品关联
DOI
PubMed
高影响因子
DRUG DEVELOPMENT RESEARCH
·
2018
·Vol. 80
·期 2
·230-245
·
IF 2.646
Michael Adu-Frimpong,Caleb Kesse Firempong,Emmanuel Omari-Siaw,Qilong Wang,Yusif Mohammed Mukhtar,Wenwen Deng,Qingtong Yu,Ximing Xu,Jiangnan Yu
Punicic acid of pomegranate oil (PAP) has gained heightened interest due to several health benefits, such as anticarcinogenic, antidiabetic, and antiatherosclerotic properties. However, these bioactivities have been hampered by chemical instability, poor water solubility, rapid metabolism, and low bioavailability of PAP. Therefore, this study was aimed at optimizing the liposomal formulation of Triacylglycerol-bound punicic acid with its regioisomers (TPAR) for improved oral bioavailability and increased hepatoprotection through antioxidation and anti-inflammation. Herein, the optimized TPAR nanoliposome (TPAR-NL) was developed using thin-film dispersion method and subsequently characterized with appropriate indices. The optimized TPAR-NL produced fairly stable spherical nanoparticles (˂ 200 nm) with encapsulation efficiency (%EE) of 85.77%, as well as enhanced in vitro release and improved oral bioavailability. The TPAR-NL exhibited profound antihepatotoxic effect in mice pretreated with carbon tetrachloride (CCl 4 ) via reduction of serum alanine aminotransferase, aspartate aminotransferase, and total bilirubin levels compared with free TPAR. The TPAR-loaded liposome also significantly reduced oxidative stress by increasing superoxide dismutase and glutathione levels while lowering malonaldehyde concentration compared with the free TPAR. The TPAR-LNF further exhibited remarkable anti-inflammatory activity compared with the free drug via inhibition of interleukin-6 and tumor necrosis factor-alpha generation. Thus, the developed nanoliposomes potentiated the antihepatotoxic activity of TPAR via antioxidation and anti-inflammation.
研究领域:
药剂学
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生物化学
·
肝脏病学
✓ 已验证
DOI
PubMed
高影响因子
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