Multivesicular Liposomes for the Sustained Release of Angiotensin I-Converting Enzyme (ACE) Inhibitory Peptides from Peanuts: Design, Characterization, and In Vitro Evaluation.

Ning Li,Guoquan Zhang,Aimin Shi,Qiang Wang

doi:10.3390/molecules24091746

Abstract

The multivesicular liposome (MVL) provides a potential delivery approach to avoid the destruction of the structure of drugs by digestive enzymes of the oral cavity and gastrointestinal system. It also serves as a sustained-release drug delivery system. In this study, we aimed to incorporate a water-soluble substance into MVLs to enhance sustained release, prevent the destruction of drugs, and to expound the function of different components and their mechanism. MVLs were prepared using the spherical packing model. The morphology, structure, size distribution, and zeta potential of MVLs were examined using an optical microscope (OM), confocal microscopy (CLSM), transmission electron cryomicroscope (cryo-EM) micrograph, a Master Sizer 2000, and a zeta sizer, respectively. The digestion experiment was conducted using a bionic mouse digestive system model in vitro. An in vitro release and releasing mechanism were investigated using a dialysis method. The average particle size, polydispersity index, zeta potential, and encapsulation efficiency are 47.6 nm, 1.880, −70.5 ± 2.88 mV, and 82.00 ± 0.25%, respectively. The studies on the controlled release in vitro shows that MVLs have excellent controlled release and outstanding thermal stability. The angiotensin I-converting enzyme (ACE) inhibitory activity of ACE-inhibitory peptide (AP)-MVLs decreased only 2.84% after oral administration, and ACE inhibitory activity decreased by 5.03% after passing through the stomach. Therefore, it could serve as a promising sustained-release drug delivery system.

Highlights

High blood pressure is one of the leading risk factors for global mortality and is estimated to have caused 9.4 million deaths and 7% of disease burden, as measured in disability-adjusted life years (DALYs) [1]
The enzymatic hydrolysis of protein by-products leads to value-added hydrolysates with improved biological activity, which can be used as a functional ingredient in food, nutraceuticals, and pharmacological formulations
multivesicular liposome (MVL) could encapsulate water-soluble substances. They can provide speculate that the peanut peptide obtained in this experiment is a substrate angiotensin I-converting enzyme (ACE) inhibitor. a new strategy for poorly soluble drugs, and ACE-inhibitory peptide (AP)-MVLs may serve as a promising sustained-release drug delivery system

Summary

Introduction

High blood pressure is one of the leading risk factors for global mortality and is estimated to have caused 9.4 million deaths and 7% of disease burden, as measured in disability-adjusted life years (DALYs) [1]. The proportion of the world’s population with high blood pressure or uncontrolled hypertension fell modestly between 1980 and 2010. Because of population growth and ageing, the number of people with uncontrolled hypertension has risen over the years. Hypertension causes stroke, myocardial infarction, cardiac failure, dementia, renal failure, and blindness. These disease conditions cause human suffering and impose severe financial and service burdens on health systems [4]

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