Improved oral bioavailability of 20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol using nanoemulsion based on phospholipid complex: design, characterization, and in vivo pharmacokinetics in rats

Figures & data

Figure 1 Chemical structure of 20(R)-25-methoxyl-dammarane-3β, 12β, 20-triol.

Figure 2 Differential scanning calorimetry thermograms of 25-OCH₃-PPD (A), phospholipid (B), physical mixture (C), and complex (D).

Figure 3 Scanning electron microscopic pictures of 25-OCH₃-PPD (A), 25-OCH₃-PPD-phospholipid complex (B), physical mixture (C), and phospholipid (D) at ×500 magnification.

Figure 4 Infrared radiation of 25-OCH₃-PPD (A), phospholipid (B), physical mixture (C), and complex (D).

Table 1 Apparent solubility of 25-OCH₃-PPD, physical mixture and complex in water and in n-octanol at room temperature

Samples	Solubility (μg/mL)
	Water	n-octanol
25-OCH3-PPD	9.44±0.11	518.87
Physical mixture	22.59±1.13	454.11
25-OCH3-PPD-phospholipid complex	46.87±1.17	715.95

Note: n=3, mean ± SD.

Abbreviation: SD, standard deviation.

Figure 5 Product ion mass spectra of [M+H]⁺ ions. Product ion mass spectra of 25-OCH₃-PPD (m/z 493.5 → 425.4) (A) and mifepristone (m/z 430.3 → 372.1) (B).

Table 2 Pharmacokinetic parameters of 25-OCH₃-PPD and complex in rats after oral administration

Parameters	25-OCH3-PPD	25-OCH3-PPD-phospholipid
t1/2 (hours)	2.51±0.74	3.58±0.34
Tmax (hours)	2.25±2.47	2.10±0.55
Cmax (ng/mL)	7.18±3.39	28.07±19.52*
AUC(0–24 h) (ng/mL hours)	26.65±7.11	97.24±40.17*
AUC(0–∞) (ng/mL hours)	44.52±16.40	114.02±44.84

Notes: Data are presented as mean ± SD (n=5),

* P<0.05.

Abbreviations: AUC, area under the curve; SD, standard deviation.

Figure 6 The plasma concentration–time curve of 25-OCH₃-PPD in rats after the oral administration of 25-OCH₃-PPD in Carboxyl methyl Cellulose (CMC) and the complex (20 mg/kg, 25-OCH₃-PPD).

Note: Data are presented as mean ± SD, (n=5).
Abbreviation: SD, standard deviation.