Micellar emulsions composed of mPEG-PCL/MCT as novel nanocarriers for systemic delivery of genistein: a comparative study with micelles

Figures & data

Figure 1 Chemical structure of genistein.

Figure 2 Schematic illustration of structures of micelles, micellar emulsions, and emulsions.

Figure 3 Quantification of Gen by UPLC-QTOF/MS.

Notes: (A) Representative chromatograms for quantification of Gen by UPLC-QTOF/MS. (B) The extracted ion chromatogram of Gen in plasma.

Abbreviations: Gen, genistein; MS, mass spectroscopy; QTOF, quadrupole time of flight; UPLC, ultra performance liquid chromatography.

Figure 4 Formulation screening of Gen-MEs.

Notes: The effects of MCT/mPEG-PCL ratio (A), drug/mPEG-PCL ratio (B), and organic/aqueous phase volume ratio upon injection (C) on particle size as well as PDI of Gen-MEs (n=3, mean ± SD).

Abbreviations: Gen-MEs, genistein-loaded micellar emulsions; MCT, medium-chain triglycerides; mPEG-PCL, methoxy poly(ethylene glycol)-block-(ε-caprolactone); PDI, polydispersity index.

Figure 5 Characterization of Gen-MEs.

Notes: (A) Particle size distribution; (B) morphology of Gen-MEs observed by TEM.

Abbreviations: Gen-MEs, genistein-loaded micellar emulsions; TEM, transmission electron microscopy.

Figure 6 Release curves of Gen-MEs and Gen-micelles performed in pH 7.4 medium based on an equilibrium dialysis method (n=3, mean ± SD).

Abbreviations: Gen, genistein; Gen-MEs, Gen-loaded micellar emulsions.

Figure 7 The stability of Gen-MEs characterized by particle size distribution.

Notes: A short-term (1 week) stability investigation on storage performed at 4°C (A) and 25°C (B); physical changes in appearance for Gen-MEs and Gen-micelles after 1 week of preparation (C); the physiological stability in the blood estimated with pH 7.4 SBF (D).

Abbreviations: Gen, genistein; Gen-MEs, Gen-loaded micellar emulsions; SBF, simulated body fluid.

Table 1 List of pharmacokinetic parameters derived by fitting the conventional two-compartment model to the plasma data

Parameter	Unit	Gen-MEs	Gen-micelles	Gen solution
k10	1/h	3.22±1.27**	4.61±1.54**	7.68±2.32
t1/2α	h	0.10±0.04	0.11±0.03	0.07±0.03
t1/2β	h	9.96±3.27**	7.5±3.39*	2.15±2.35
CL	L/h	1.28±0.37**	1.33±0.36**	2.57±0.43
CL2	L/h	0.73±0.21**,##	1.53±0.15**	2.94±0.29
AUC0−t	µM*h	8.48±1.33**,##	5.55±0.59**	2.97±0.73
AUC0−inf	µM*h	9.44±1.93**,#	6.52±1.53**	3.99±0.77
AUMC	µM*h^Citation2	38.27±5.21**,##	27.93±3.99**	5.14±1.63
MRT	h	8.27±1.28**,#	5.27±1.56**	1.12±1.26
Vss	L	6.98±1.51**	7.03±3.11*	2.52±2.41

Notes: Student’s t-test,

* P<0.05,

** P<0.01, compared with Gen solution;

# P<0.05,

## P<0.01, compared with Gen-micelles. Data are presented as mean ± standard deviation.

Abbreviations: Gen, genistein; Gen-MEs, Gen-loaded micellar emulsions; h, hour; k₁₀, elimination rate constant from the central compartment; t_1/2α, redistribution half-life; t_1/2β, elimination half-life; CL, clearance of central compartment; CL₂, clearance of peripheral compartment; AUC, area under the plasma concentration–time curve; AUMC, area under the first moment of the plasma concentration–time curve; MRT, mean retention time; V_ss, steady-state volume of distribution.

Figure 8 Plasma Gen concentration vs time profiles after intravenous administration of Gen-MEs, Gen-micelles, and Gen solution to rats (mean ± SD, n=5).

Abbreviations: Gen, genistein; Gen-MEs, Gen-loaded micellar emulsions.

Figure 9 Tissue distribution of Gen after intravenous administration of Gen-MEs and Gen-micelles at 2, 10, and 24 hours.

Notes: Student’s t-test, **P<0.01, compared with Gen-micelles.

Abbreviations: Gen, genistein; Gen-MEs, Gen-loaded micellar emulsions.

TaylorCKLevyRMElliottJCBurnettBPThe effect of genistein aglycone on cancer and cancer risk: a review of in vitro, preclinical, and clinical studiesNutr Rev200967739841519566600

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