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

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.

A Proposed Methodology for a Risk Assessment-Based Liposome Development Process

“…The critical ones have to be selected and labelled as CMAs and CPPs. To make this figure and the tables of QTPP and CQAs, prior knowledge, previous experimental experience, and a thorough literature background survey of the field [31,[41][42][43][44][45][46][47][48] were necessary. Although, the main points of the tables and figures are shreds of evidence from the literature mixed with practical experiences, the systemic collection of all the relevant factors and data in one paper is the novelty of the work.…”

Screening and Molecular Modeling Evaluation of Food Peptides to Inhibit Key Targets of COVID-19 Virus

“…The peptides were collected from the latest reviews on ACE-inhibitory peptides derived from the natural food resources including plant, animal, marine, and mushroom [ 23 , 24 , 25 , 26 , 27 , 28 , 29 ]. All the peptides were drawn using Chem3D software (Version 15.0, Cambridge Software Inc., Cambridge, MA, USA, 2018), and then, one step of optimization was employed to get the effective structure.…”

“…The inhibition mechanism of peptides against human angiotensin-converting enzyme 2 (ACE2, the COVID-19 coronavirus spike protein binding receptor), COVID-19 coronavirus main protease (COVID-19 virus M pro ), and RNA-dependent RNA polymerase (RdRp) were conducted through the molecular docking and dynamic test using Discovery studio client software (v16.1.0.15350) (BIOVIA, San Diego, CA, USA) based on our previous methods [ 15 , 23 , 24 ]. MLN-4760, inhibitor N3, and Remdesivir were set as positive controls [ 18 , 20 , 21 ].…”

Nanomedicine for Drug Delivery throughout the Alimentary Canal

“…The formulation reduced blood glucose levels for 16 h in a Type I diabetes model. The oral bioavailability was 34%, and the time at which the C max occurred ( T max ) was 9 h. Another study used multivesicular liposomes to create a sustained release formulation of angiotensin I-converting enzyme inhibitory peptides from peanuts . Multivesicular liposomes were used to prevent the degradation of drugs in gastric enzymes and sustain drug release.…”