The Influence of Nanoparticle Properties on Oral Bioavailability of Drugs

Figures & data

Figure 1 The benefits of using nanoparticles.

Abbreviation: GI, gastrointestinal.

Figure 2 (A) The nanoparticle properties including size, surface properties, and shape of nanoparticles. (B) Schematic representation illustrating the biochemical and physiological barriers of oral drug delivery. (C) The relationship of the nanoparticle properties, oral bioavailability, and barriers in oral delivery.

Table 1 Thickness of Mucus in Different Parts of the Human Gastrointestinal Tract

Mucus Membrane	Total Mucus Thickness (μm)	Ref
Gastric	30–300	[^Citation37]
Small Intestine	150–400	[^Citation37]
Ileum	400–500	[^Citation36]
Colon	30–700	[^Citation36,Citation37]

Figure 3 (A) Highly O-glycosylated mucin domains. Red, protein core; Green, oligosaccharides. (B) Schematic representation illustrating two types of mucus.

Abbreviations: Ser, serine; Thr, threonine; Pro, proline; Cys, cysteine; S-S, disulfide bonds; Ser-O-GalNAC, O-glycosylated serine.

Table 2 The Effect of Various Surface Modification Materials of Nanoparticles on the Oral Administration

Material	Influential Effect	Ref
PEG	Increasing mucus penetration (~5 KDa)	[^Citation62]
	Reduce recognition and clearance	[^Citation37,Citation71]
	Enhance plasma circulation times	[^Citation71]
	Promote drug accumulation	[^Citation37]
TA	Improve solubility of hydrophobic molecules	[^Citation75]
	Inhibitory effect of P-gp	[^Citation81]
	Avoid gastric acid degradation	[^Citation2]
Polycation	Increase solubility of hydrophobic molecules	[^Citation84]
PECs	Facilitating mucus transport	[^Citation43,Citation85]
	Increasing cellular penetration	[^Citation89]
Lipid material (log P>5)	Increase the lymphatic absorption Prevent the liver from first pass metabolizing	[^Citation84]
		[^Citation84]
Specific ligands	Increasing cellular uptake	[^Citation96]

Abbreviations: PEG, ploy(ethylene glycol); TA, tannic acid; PECs; polyelectrolyte complexes; P-gp, P-glycoprotein.

Figure 4 Structural formula of partial materials containing hydrophilic groups.

Table 3 The Different Internalization Pathways Corresponding to Different Cells and the Main Shapes Associated with Them

Cellular Mechanism	Cell Type	Nanoparticle Shape	Ref
Phagocytosis	Macrophages	Large ARs	[^Citation116]
	Monocytes
	Dendritic cells
	Natural killer cells
	Neutrophils
Macropinocytosis	Endothelial cells		[^Citation117]
	Epithelial cells
Clathrin-mediated endocytosis	Endothelial cells	Sphere-shaped particles	[^Citation118]
Caveolin-mediated endocytosis	The capillary endothelium	Large ARs	[^Citation119]
	Type I epithelial cells
	Muscle cells
	Fibroblasts

Abbreviation: AR, aspect ratio.

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