Click
here to close Hello! We notice that
you are using Internet Explorer, which is not supported by Echinobase
and may cause the site to display incorrectly. We suggest using a
current version of Chrome,
FireFox,
or Safari.
Nanomaterials (Basel)
2017 Dec 02;712:. doi: 10.3390/nano7120421.
Show Gene links
Show Anatomy links
Improved In Vivo Efficacy of Anti-Hypertensive Biopeptides Encapsulated in Chitosan Nanoparticles Fabricated by Ionotropic Gelation on Spontaneously Hypertensive Rats.
Auwal SM
,
Zarei M
,
Tan CP
,
Basri M
,
Saari N
.
???displayArticle.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.
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. Physical properties of Chit-AntBiop-NPs; (a) particle size and pdi, (b) zeta potential.
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. 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.
Ahmed,
Preparation, characterization, and potential application of chitosan, chitosan derivatives, and chitosan metal nanoparticles in pharmaceutical drug delivery.
2016, Pubmed
Ahmed,
Preparation, characterization, and potential application of chitosan, chitosan derivatives, and chitosan metal nanoparticles in pharmaceutical drug delivery.
2016,
Pubmed
Alam,
Nanocarriers as treatment modalities for hypertension.
2017,
Pubmed
Auwal,
Response Surface Optimisation for the Production of Antioxidant Hydrolysates from Stone Fish Protein Using Bromelain.
2017,
Pubmed
Beltrán-Barrientos,
Invited review: Fermented milk as antihypertensive functional food.
2016,
Pubmed
GBD 2013 Mortality and Causes of Death Collaborators,
Global, regional, and national age-sex specific all-cause and cause-specific mortality for 240 causes of death, 1990-2013: a systematic analysis for the Global Burden of Disease Study 2013.
2015,
Pubmed
Geng,
A Tricholoma matsutake Peptide with Angiotensin Converting Enzyme Inhibitory and Antioxidative Activities and Antihypertensive Effects in Spontaneously Hypertensive Rats.
2016,
Pubmed
He,
Size-dependent absorption mechanism of polymeric nanoparticles for oral delivery of protein drugs.
2012,
Pubmed
Khdair,
Modified-chitosan nanoparticles: Novel drug delivery systems improve oral bioavailability of doxorubicin.
2016,
Pubmed
Kontis,
Contribution of six risk factors to achieving the 25×25 non-communicable disease mortality reduction target: a modelling study.
2014,
Pubmed
Luo,
A review of biodegradable polymeric systems for oral insulin delivery.
2016,
Pubmed
Muhammad Auwal,
Optimization of Bromelain-Aided Production of Angiotensin I-Converting Enzyme Inhibitory Hydrolysates from Stone Fish Using Response Surface Methodology.
2017,
Pubmed
,
Echinobase
Niu,
Lipid-based nanocarriers for oral peptide delivery.
2016,
Pubmed
Patel,
Development of oral sustained release rifampicin loaded chitosan nanoparticles by design of experiment.
2013,
Pubmed
Patel,
Cardiovascular mortality associated with 5 leading risk factors: national and state preventable fractions estimated from survey data.
2015,
Pubmed
Renukuntla,
Approaches for enhancing oral bioavailability of peptides and proteins.
2013,
Pubmed
Rizwan,
pH Sensitive Hydrogels in Drug Delivery: Brief History, Properties, Swelling, and Release Mechanism, Material Selection and Applications.
2017,
Pubmed
Roth,
Demographic and epidemiologic drivers of global cardiovascular mortality.
2015,
Pubmed
Shegokar,
Nanocrystals: industrially feasible multifunctional formulation technology for poorly soluble actives.
2010,
Pubmed
Soltani,
The impacts of obesity on the cardiovascular and renal systems: cascade of events and therapeutic approaches.
2015,
Pubmed
Sun,
Preparation and in vitro/in vivo characterization of enteric-coated nanoparticles loaded with the antihypertensive peptide VLPVPR.
2014,
Pubmed
Yang,
Release of Doxorubicin by a Folate-Grafted, Chitosan-Coated Magnetic Nanoparticle.
2017,
Pubmed
Yu,
Enhanced and Extended Anti-Hypertensive Effect of VP5 Nanoparticles.
2016,
Pubmed
Zhang,
Chitosan-based nanoparticles for improved anticancer efficacy and bioavailability of mifepristone.
2016,
Pubmed
