Design of chimeric GLP-1A using oligomeric bile acids to utilize transporter-mediated endocytosis for oral delivery

Table 1 Pharmacokinetic parameters of GLP-1A-Cys and oligomeric DOCA-G1As

	GLP-1A-Cys	GLP-1A-Cys	mD-G1A	bD-G1A	tD-G1A
Administration route	IV	PO	PO	PO	PO
Dose (μg/kg)	10	100	100	100	100
T_max (h)		2.0	0.5	1.5	0.5
C_max (ng/mL)		0.56 ± 0.08	5.01 ± 2.37	7.63 ± 0.90	13.39 ± 5.54
AUC_0-last (ng·h/mL)	17.38 ± 0.70	2.88 ± 0.21	13.27 ± 0.91	24.43 ± 4.97	22.14 ± 2.03
MRT (h)	11.2 ± 1.7	27.3 ± 22.8	7.6 ± 3.8	7.9 ± 1.3	6.6 ± 2.6
BA (%)	100	1.0 ± 0.1	4.7 ± 0.3	8.6 ± 1.7	7.6 ± 0.7

Abbreviations: IV intravenous, PO per oral, T_max time of maximum concentration, C_max maximum concentration, AUC area under the curve, MRT mean residence time, BA bioavailability compared with IV route
Data are presented as mean ± standard deviation (n = 4 for each group). T_max represents the median

ISSN: 2055-7124