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. 2017 Dec 2;7(12):421.
doi: 10.3390/nano7120421.

Improved In Vivo Efficacy of Anti-Hypertensive Biopeptides Encapsulated in Chitosan Nanoparticles Fabricated by Ionotropic Gelation on Spontaneously Hypertensive Rats

Shehu Muhammad Auwal  1   2 , Mohammad Zarei  3   4 , Chin Ping Tan  5 , Mahiran Basri  6 , Nazamid Saari  7
Affiliations

Improved In Vivo Efficacy of Anti-Hypertensive Biopeptides Encapsulated in Chitosan Nanoparticles Fabricated by Ionotropic Gelation on Spontaneously Hypertensive Rats

Shehu Muhammad Auwal et al. Nanomaterials (Basel). .

Abstract

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.

Keywords: ACE-inhibitory biopeptides; angiotensin I-converting enzyme; bioavailability; blood pressure; chitosan nanoparticles; efficacy; enzymatic degradation; oral administration; physicochemical properties; spontaneously hypertensive rats.

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Conflict of interest statement

The authors have no conflict of interest. Moreover, the funding sponsors had no role in the design of the study; in the collection, analyses, or interpretation of data; in the writing of the manuscript, and in the decision to publish the results.

Figures

Figure 1
Figure 1
Effect of formulation parameters on the particle size (nm) and entrapment efficiency (EE, %) of Chit-AntBiop-NPs (a) AntBiop:Chitosan mass ratio; (b) stirring speed; (c) and stirring time.
Figure 2
Figure 2
Physical properties of Chit-AntBiop-NPs; (a) particle size and pdi, (b) zeta potential.
Figure 3
Figure 3
Physical appearance, in vitro release profiles and differential scanning calorimetry (DSC) of the Chit-AntBiop-NPs; (a) transmission electron microscopy (TEM) images of Chit-AntBiop-NPs, (b) In vitro release profiles of AntBiop from Chit-AntBiop-NPs in PBS pH 7.4 (c) DSC curve of the blank chitosan nanoparticles and (d) DSC curve of the Chit-AntBiop-NPs.
Figure 4
Figure 4
Systolic blood-pressure-lowering effect of unencapsulated biopeptides, captopril and three doses of Chitosan-AntBiop-NPs within 24 h of single oral administration on SHRs.
See this image and copyright information in PMC

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