Nanoparticles: Oral Delivery for Protein and Peptide Drugs

Abstract

Protein and peptide drugs have many advantages, such as high bioactivity and specificity, strong solubility, and low toxicity. Therefore, the strategies for improving the bioavailability of protein peptides are reviewed, including chemical modification of nanocarriers, absorption enhancers, and mucous adhesion systems. The status, advantages, and disadvantages of various strategies are systematically analyzed. The systematic and personalized design of various factors affecting the release and absorption of drugs based on nanoparticles is pointed out. It is expected to design a protein peptide oral delivery system that can be applied in the clinic.

Nanoparticles Modified with Cell-Penetrating Peptides: Conjugation Mechanisms, Physicochemical Properties, and Application in Cancer Diagnosis and Therapy

“…Interestingly, a lot of research has been invested in the development of strategies for oral administration since this is meant as the ideal mode of drug administration [113]. In this respect, Tan et al recently presented CPP-PEG-modified mesostructured silica NPs that greatly enhanced the bioavailability of therapeutic peptides and proteins.…”

Recent Advances in Encapsulation, Protection, and Oral Delivery of Bioactive Proteins and Peptides using Colloidal Systems

“…Nevertheless, they may be dissociated or degraded within the GIT, thereby releasing the BPPs, which can then diffuse through the mucus layer. Once they reach the surface of the epithelium cells the BPPs may be absorbed through numerous mechanisms, such as active or passive transcellular routes, paracellular (tight-junctions) routes, or endocytosis [11,33]. Moreover, the BPPs may be absorbed by different kinds of epithelium cells (such as enterocytes or M-cells) depending on their size and surface chemistry.…”

“…Moreover, the BPPs may be absorbed by different kinds of epithelium cells (such as enterocytes or M-cells) depending on their size and surface chemistry. M-cells, which are located in the Peyer's patches, are typically much more effective at absorbing colloidal particles (d < 500 nm) than enterocytes, but they are much less prevalent in the GIT, which limits their effectiveness for this purpose [11]. Many kinds of proteins and BPP-loaded colloidal particles are too large or too hydrophilic to be absorbed by the mechanisms typically used for smaller pharmaceuticals or nutraceuticals.…”

“…While these two challenges are not specific to oral delivery, they are complicated by the harsh chemical environments present within the human gastrointestinal tract (GIT), such as the strongly acidic and enzymatically active gastric fluids within the human stomach [8]. For these reasons, BPPs may need to be administered using some kind of colloidal delivery system (CDS) to protect them from degradation during storage and passage through the GIT, but then release them at the required location inside the human body [3,[9][10][11]. Many kinds of CDS have been created that may be suitable for this purpose, including microemulsion droplets, emulsion droplets, solid fat particles, liposomes, and microgels ( Figure 1).…”

Nanoparticle modification in biological media: implications for oral nanomedicines

“…3,4 Targeting of biological transport is thought to be essential as most particulates themselves show poor permeability across the GI mucosa. 5 Nanoparticle biocorona formation, which arises as a result of interaction of nanoparticles with a range of biomolecules present in biological milieus (e.g. proteins, lipids, nucleic acids, metabolites), is a critical phenomenon that determines the biological fate (therapeutic activity or toxicity) of nanoparticles.…”