. 2019 Jan 10;9(5):902–922. doi: 10.1016/j.apsb.2019.01.004

Table 5.

Summary of lipid-based particles in oral delivery of therapeutic peptides/proteins.

Formulation composition	Model drug	Main transport mechanisms	Characterization (size, ZP, EE)	PK		PD	Ref.
Formulation composition	Model drug	Main transport mechanisms	Characterization (size, ZP, EE)	Dose	F (%)	PD	Ref.
GCTE-liposomes	Vancomycin	N/A	Size: 134.0±9.7 nm;	N/A	N/A	N/A	6
			ZP: −4.43±0.81 mV;
			EE: 58.53±1.76%
GCTE-liposomes	Myrcludex B	N/A	Size: 140.7±4.3 nm;	N/A	N/A	3.5-Fold increase compared to the free peptide	7
			ZP: –4.20±0.48 mV;
			EE: 65.67±2.91%
Liposomes containing bio-enhancers and tetraether lipids	hGH	N/A	Size: 229.7±12.8 nm;	8 mg	3.4	N/A	8
			ZP: 41.0±1.2 mV;
			EE: 31.2±0.5%
Liposomes with 25% TELs	Octreotide	N/A	Size: 130–207 nm;	N/A	N/A	4-Fold the hypoglycemic effect compared with free octreotide	9
Liposomes with 25% TELs	Octreotide	N/A	EE: 13.0%	N/A	N/A		9
Octreotide-DOCA SEDDS	Octreotide	N/A	Size: 152 nm;	50 mg (pig)	5.21	N/A	10
Octreotide-DOCA SEDDS	Octreotide	N/A	ZP: –3.7 mV	50 mg (pig)	5.21	N/A	10
CS–TGA–MNA-coated liposomes	sCT	TJs opening	Size: 604.8±29.6 nm;	40 μg	4.04	A minimum of 65% of PGL value after 6 h	14
CS–TGA–MNA-coated liposomes	sCT	TJs opening	ZP: 27.9±1.1 mV	40 μg	4.04	A minimum of 65% of PGL value after 6 h	14
Exenatide/DOC SNEDDS	Exendin-4	N/A	Size: 45.87±2.9 nm;	150 μg	14.62±3.07	20.6% decrease of PGL in 5 h	38
Exenatide/DOC SNEDDS	Exendin-4	N/A	ZP: 0.7±0.1 mV	150 μg	14.62±3.07	20.6% decrease of PGL in 5 h	38
Liposomes containing SGC, STC, STC respectively	Ins	Transcellular way	Size: 157±19 nm;	20 IU/kg	8.5±2.1 (the optimal formulation)	60% decrease of PGL in 20 h with peak time around 8–12 h	52., 81.
			EE: 29.8±1.7%
			(the optimal formulation)
Biotinylated liposomes (BLPs)	Ins	Biotin receptor mediated transport	Size: ~150 nm;	20 IU/kg	12.09	64% reduction of the PGL in 24 h with peak time around 5–12 h	55
Biotinylated liposomes (BLPs)	Ins	Biotin receptor mediated transport	EE: 35%–42%	20 IU/kg	12.09		55
Proliposomes encased in Eudragit S100	Ins	Paracellular way	Size: 583.2±10.2 nm;	N/A	N/A	N/A	98
			ZP: 28.3±3.7 mV;
			EE: 17.6±2.4%
VA incorporated SLN nanoparticles	Ins	N/A	Size: 172~281 nm;	50 IU/kg	5.1	~50% decrease of PGL in 4 h	103
			ZP: –40 mV;
			EE: 54.5%
Ins–phospholipid complex loaded SNEDDS	Ins	TJs opening	Size: multi-dispersed peaks;	50 IU/kg	0.43±0.13	38% decrease of PGL in 10 h	106
			ZP: –4.1±0.3 mV ;
			EE: 73.1%

ZP, zeta potential; EE, encapsulation efficiency; F, relative bioavailability; PGL, plasma glucose levels; TGA, thioglycolic acid; MNA, 6-mercaptonicotinamide-conjugate; Pt, protamine; TELs, tetraether lipids; GCTE, glycerylcaldityltetraether lipids; VA, viscosity-enhancing agent; SNEDDS, self-nanoemulsifying drug delivery systems; DOC, sodium docusate; DOCA, deoxycholate