Preparation and evaluation of ibuprofen-loaded microemulsion for improvement of oral bioavailability

Figures & data

Table 1.  Solubility of ibuprofen in various vehicles at 25°C (mean ± SD, n = 3).

	Vehicle	Solubility of ibuprofen (mg/ml)
Surfactant	Tween80	250.51 ± 17.10
	Labrasol	265.65 ± 16.97
	Cremophor RH40	259.33 ± 13.78
	span80	144.70 ± 14.15
Oil	peanut oil	66.30 ± 7.90
	Labrafac Lipophile WL1349	98.86 ± 15.10
	Labrafil M 1944CS	87.64 ± 11.90
Co-surfactant	Transcutol P	389.91 ± 19.40
	Propylene glycol	162.68 ± 12.25
	Ethanol	408.39 ± 17.09

Figure 1.  The pseudo-ternary phase diagrams of the oil-surfactant-water system at 1:1 (a), 2:1 (b), and 3:1 (c) weight ratios of Cremophor RH40 to Transcutol P at room temperature. E, emulsion; G, gel; L, isotropic region; shaded region, microemulsion.

Table 2.  Compositions, droplet size, and ibuprofen content of the selected formulations (mean ± SD, n = 3).

Formulation	Oil:Sm:water	Droplet size (nm)	Drug content (mg/mL)
F1	8:32:60	53.2 ± 1.36	36.6 ± 1.66
F2	12:30:58	55.6 ± 2.81	50.9 ± 1.75
F3	17:28:55	56.9 ± 2.46	60.3 ± 1.37

Figure 2.  Transmission electron microphotography of ibuprofen-loaded microemulsions.

Figure 3.  Release profiles of drug from microemulsion in PH 6.8 PBS, 0.1 N HCl, and distilled water (mean ± SD, n = 3).

Table 3.  Comparison of pharmacokinetic parameters between ibuprofen microemulsion and ibuprofen granule (mean ± SD, n = 5).

Group	Microemulsion	Granule
T1/2 (h)	2.14 ± 0.63	2.16 ± 0.27
Cmax (mg/L)	69.02 ± 9.88	37.14 ± 9.59
tmax (h)	0.65 ± 0.34	0.50 ± 0.31
AUC (h·mg/L)	183.19 ± 11.82	95.31 ± 15.14
MRT (h)	2.70 ± 0.24	2.77 ± 0.17

Figure 4.  The blood concentration-time profile of ibuprofen after oral administration of granule and microemulsion to rats (mean ± SD, n = 5).