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首页> 美国卫生研究院文献>Nanomaterials >Improved In Vivo Efficacy of Anti-Hypertensive Biopeptides Encapsulated in Chitosan Nanoparticles Fabricated by Ionotropic Gelation on Spontaneously Hypertensive Rats
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Improved In Vivo Efficacy of Anti-Hypertensive Biopeptides Encapsulated in Chitosan Nanoparticles Fabricated by Ionotropic Gelation on Spontaneously Hypertensive Rats

机译：离子电凝胶法制备的壳聚糖纳米粒包裹的抗高血压生物肽对自发性高血压大鼠的体内功效的改善

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Recent biotechnological advances in the food industry have led to the enzymatic production of angiotensin I-converting enzyme (ACE)-inhibitory biopeptides with a strong blood pressure lowering effect from different food proteins. However, the safe oral administration of biopeptides is impeded by their enzymatic degradation due to gastrointestinal digestion. Consequently, nanoparticle (NP)-based delivery systems are used to overcome these gastrointestinal barriers to maintain the improved bioavailability and efficacy of the encapsulated biopeptides. In the present study, the ACE-inhibitory biopeptides were generated from stone fish (Actinopyga lecanora) protein using bromelain and stabilized by their encapsulation in chitosan (chit) nanoparticles (NPs). The nanoparticles were characterized for in vitro physicochemical properties and their antihypertensive effect was then evaluated on spontaneously hypertensive rats (SHRs). The results of a physicochemical characterization showed a small particle size of 162.70 nm, a polydispersity index (pdi) value of 0.28, a zeta potential of 48.78 mV, a high encapsulation efficiency of 75.36%, a high melting temperature of 146.78 °C and an in vitro sustained release of the biopeptides. The results of the in vivo efficacy indicated a dose-dependent blood pressure lowering effect of the biopeptide-loaded nanoparticles that was significantly higher (p < 0.05) compared with the un-encapsulated biopeptides. Moreover, the results of a morphological examination using transmission electron microscopy (TEM) demonstrated the nanoparticles as homogenous and spherical. Thus, the ACE-inhibitory biopeptides stabilized by chitosan nanoparticles can effectively reduce blood pressure for an extended period of time in hypertensive individuals.
机译：食品工业中生物技术的最新进展已导致酶促生产血管紧张素I转换酶（ACE）抑制性生物肽，这些肽具有从不同食品蛋白质中显着降低血压的作用。然而，由于胃肠道消化，生物肽的酶促降解阻碍了生物肽的安全口服给药。因此，基于纳米颗粒（NP）的递送系统用于克服这些胃肠道障碍，以维持所包封的生物肽的改善的生物利用度和功效。在本研究中，使用菠萝蛋白酶从石头鱼（Actinopyga lecanora）蛋白中生成ACE抑制生物肽，并通过将其封装在壳聚糖（chit）纳米颗粒（NPs）中使其稳定。表征纳米颗粒的体外理化特性，然后在自发性高血压大鼠（SHRs）上评估其降压作用。物理化学表征的结果表明，小粒径为162.70 nm，多分散指数（pdi）值为0.28，ζ电位为48.78 mV，高封装效率为75.36％，高熔化温度为146.78°C，且体外持续释放生物肽。体内功效的结果表明，与未包封的生物肽相比，负载生物肽的纳米颗粒的剂量依赖性降血压作用明显更高（p <0.05）。此外，使用透射电子显微镜（TEM）进行形态学检查的结果表明，纳米颗粒为均质和球形。因此，壳聚糖纳米颗粒稳定的ACE抑制生物肽可以在高血压个体中长时间有效降低血压。

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