Improving the bioaccessibility and bioavailability of carnosic acid using a lecithin-based nanoemulsion: complementary in vitro and in vivo studies.,Food & Function

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Improving the bioaccessibility and bioavailability of carnosic acid using a lecithin-based nanoemulsion: complementary in vitro and in vivo studies.
Food & Function ( IF 5.1 ) Pub Date : 2020-07-31 , DOI: 10.1039/d0fo01098g
Huijuan Zheng ₁ , Wahyu Wijaya ₂ , Hongwei Zhang ₃ , Konglong Feng ₄ , Qianru Liu ₃ , Ting Zheng ₃ , Zhiya Yin ₃ , Yong Cao ₄ , Qingrong Huang ₃

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Carnosic acid (CA) represents one of the most effective antioxidants that can be applied for the prevention of degenerative and chronic diseases. However, the intrinsic hydrophobic nature of CA results in low solubility and poor dissolution in the gastrointestinal (GI) tract, which limits its applications in a variety of functional food systems. In order to address these issues, we encapsulated CA in a lecithin-based nanoemulsion (CA-NE) to improve its bioaccessibility and bioavailability which are evaluated using in vitro and in vivo digestion models. The CA-NE demonstrated a loading capacity of 2.6–3.0%, an average particle size of 165 nm, a ζ-potential value of −57.2 mV, and good stability during 4-weeks of storage at 4, 25, and 37 °C. The in vitro static pH-stat lipolysis model and dynamic TNO gastrointestinal (TIM-1) model demonstrated a 12.6 and 5.6 fold increase in the total bioaccessibility of CA encapsulated in nanoemulsion, respectively, as opposed to CA in suspension form. Moreover, the in vivo pharmacokinetics study on a rat model (Male Sprague Dawley) confirmed that the bioavailability of CA in nanoemulsion showed a 2.2 fold increase, as compared to that of CA in suspension form. In conclusion, the bioaccessibility and bioavailability of CA were remarkably improved by encapsulation of CA in a lecithin-based nanoemulsion. Moreover, the combined in vitro and in vivo study could serve as a useful approach for the comprehensive evaluation of oral lipid-based delivery systems.

中文翻译：

使用基于卵磷脂的纳米乳剂改善肌酸的生物利用度和生物利用度：补充的体内和体外研究。

肌酸（CA）代表可用于预防退行性和慢性疾病的最有效的抗氧化剂之一。但是，CA固有的疏水性导致其在胃肠道（GI）中的溶解度低和溶解差，这限制了CA在各种功能性食品系统中的应用。为了解决这些问题，我们将CA封装在基于卵磷脂的纳米乳剂（CA-NE）中，以提高其生物利用度和生物利用度，并使用体外和体内消化模型对其进行了评估。CA-NE的负载量为2.6–3.0％，平均粒径为165 nm，ζ电位值为-57.2 mV，在4、25和37°C下储存4周期间具有良好的稳定性。在体外静态pH-stat脂解模型和动态TNO胃肠道（TIM-1）模型分别证明，与悬浮液形式的CA相比，纳米乳液中封装的CA的总生物利用度分别提高了12.6倍和5.6倍。此外，对大鼠模型（雄性Sprague Dawley）的体内药代动力学研究证实，与悬浮液形式的CA相比，纳米乳液中CA的生物利用度提高了2.2倍。总之，通过将CA包封在基于卵磷脂的纳米乳液中，CA的生物可利用性和生物利用度得到显着改善。此外，结合的体外和体内研究可以作为有用的方法，用于基于口服脂质的递送系统的综合评估。

更新日期：2020-09-23

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