. 2023 Apr 19;24(8):7548. doi: 10.3390/ijms24087548

Table 5.

Preclinical animal studies investigating the therapeutic applicability of larazotide acetate.

Model	Species	Administration	Daily Dose	Results	Ref.
celiac disease	gliadin-sensitized HLA-HCD4/DQ8 transgenic mouse	p.o. gavage	0.25 mg	reduced intestinal permeability and macrophage infiltration	[213]
celiac disease	gliadin-sensitized HLA-HCD4/DQ8 transgenic mouse	p.o. gavage	0.3 mg	reduced intestinal permeability	[214]
intestinal permeability	Il10^−/− mouse	p.o. gavage	5 mg	reduced intestinal permeability and inflammation	[215]
spontaneous colitis	Il10^−/− mouse	p.o. in drinking water	0.1 or 1 mg/mL	reduced intestinal permeability and inflammation	[216]
DSS induced colitis	zonulin transgenic mouse	p.o. in drinking water	1 mg/mL	reduced intestinal permeability	[217]
radiation-induced enteropathy	mouse	i.p.	0.25 mg	improved clinical state and histological scores, inhibited bacterial translocation, elevated TJ protein levels	[218]
healthy (pharmacokinetics)	pig	p.o. capsule	0.05 mg/kg	determining pharmacokinetics of larazotide acetate in the small intestine	[219]
Ruminococcus blautia gnavus colonization	germ-free mouse	p.o. in drinking water	0.15 mg/mL	reduced intestinal permeability	[102]
spontaneous T1D	BB diabetic-prone rat	p.o. in drinking water	0.01 mg/mL	inhibited development of diabetes	[138]
rheumatoid arthritis	mouse	p.o. in drinking water	0.15 mg/mL	attenuated arthritis	[153]
rheumatoid arthritis	Il10ra^−/− mouse, Cldn8^−/− mouse	p.o. gavage	2 × 0.05 mg	reduced intestinal permeability, inflammation, and joint swelling	[220]
vasculitis	mouse	i.p.	0.5 mg	reduced intestinal permeability and LPS translocation, prevented cardiovascular lesions	[221]
LPS-induced acute lung injury		i.t.	0.05 mg	reduced severity, decreased inflammatory markers	[12]
LPS-induced acute lung injury		i.v.	0.01 or 0.025 or 0.05 mg	reduced severity, decreased inflammatory markers	[12]
influenza		i.v.	0.15 mg	reduced severity of acute lung injury	[222]
salivary gland fibrosis		i.p.	5 mg/kg	improved epithelial barrier function, ameliorated fibrosis	[223]
NAFLD		p.o. in drinking water	0.1 or 1 mg/mL	reduced intestinal permeability	[224]
NAFLD		p.o. gavage	2 × 0.03 or 2 × 0.3 mg	reduced intestinal permeability	[224]
acute liver failure	rat	p.o. in drinking water	0.01 mg/mL	decreased intestinal damage	[225]
acute liver failure	rat	p.o. gavage	2 × 0.03 mg	decreased intestinal damage	[225]

Abbreviations: Ref.: reference; p.o.: per os; i.p.: intraperitoneal; i.v. intravenous; DSS: dextran sulphate sodium; TJ: tight junction; T1D: type 1 diabetes; LPS: lipopolysaccharide; NAFLD: non-alcoholic fatty liver disease.