Oral drug delivery with nanoparticles into the gastrointestinal mucosa

Abstract

The oral route of protein and peptide drugs has been a popular method of drug delivery in recent years, although it is often a challenge to achieve effective drug release and minimize the barrier functions of the gastrointestinal tract. Gastrointestinal mucosa can capture and remove harmful substances; similarly, it can limit the absorption of drugs. Many drugs are effectively captured by the mucus and rapidly removed, making it difficult to control the release of drugs in the gastrointestinal tract. The use of drug carrier systems can overcome the mucosal barrier and significantly improve bioavailability. Nanoparticle drug carriers can protect the drug from degradation, transporting it to a predetermined location in the gastrointestinal tract to achieve more efficient and sustained drug delivery. It is becoming clearer that the characteristics of nanoparticles, such as particle size, charge, and hydrophobicity, are related to permeability of the mucosal barrier. This review focuses on the latest research progress of nanoparticles to penetrate the mucosal barrier, including the delivery methods of nanoparticles on the surface of gastrointestinal mucosa, and aims to summarize how successful oral nanoparticle delivery systems can overcome this biological barrier in the human body. In addition, the in vitro model based on gastrointestinal mucus is an important tool for drug research and development. Here, we discuss different types of drug delivery systems and their advantages and disadvantages in design and potential applications. Similarly, we reviewed and summarized various methods for evaluating oral nanoparticles in in vitro and in vivo models.

Oromucosal Alginate Films with Zein Nanoparticles as a Novel Delivery System for Digoxin

“…The mean size of the zein nanoparticles without digoxin was 85.72 ± 0.360 nm, which increase when the digoxin concentration also augmented (Table 4). However, all produced nanoparticles displayed a mean diameter inferior to 200 nm, which is ideal for escaping recognition by the reticuloendothelial system and, consequently, prolong their half-life in the blood system [74]. Nevertheless, other authors described the particle size reduction of nanosuspensions as determinant for the increase in the surface area and enhancement in dissolution velocity of the drug [75,76].…”

“…Nanoparticle drug carriers aim to achieve more efficient and sustained drug delivery. Their characteristics, such as particle size, charge, and hydrophobicity, are determinants of the permeability of the mucosal barrier [74]. The mean size of the zein nanoparticles without digoxin was 85.72 ± 0.360 nm, which increase when the digoxin concentration also augmented (Table 4).…”

Options to Improve the Action of PROTACs in Cancer: Development of Controlled Delivery Nanoparticles

“…Thus, parenteral route administration of nanoPROTACs would be expected for rapid translation to the clinic. However, oral administration would be desirable to guarantee patient endorsement (Liu et al, 2021b). Polymer-based nanoPROTACs formulation would be obtained in suspension to preserve aggregation phenomena after lyophilization.…”

Safety and Toxicity Issues of Therapeutically Used Nanoparticles from the Oral Route

“…In recent years, NPs have increasingly been explored to overcome GI tract barriers and improve the oral bioavailability by taking the excellent features of the GI tract and overcoming the problems like low oral solubility and bioavailability of drugs [18]. NPs are ultrafine colloidal particles that range from about 1 to 1000 nm in diameter and show different properties compared to their source materials.…”