Non-ionic surfactants as novel intranasal absorption enhancers: in vitro and in vivo characterization

Figures & data

Figure 1. Effect of pH on the intranasal absorption of SMS (n = 3).

Figure 2. Effect of drug concentration on the intranasal absorption of SMS (n = 3).

Figure 3. Effect of poloxamer188 concentration on the intranasal absorption of SMS (n = 3).

Figure 4. Effect of cremophor EL concentration on the intranasal absorption of SMS (n = 3).

Figure 5. Effect of laurate SE concentration on the intranasal absorption of SMS (n = 3).

Figure 6. Comparison of different absorption enhancers on intranasal absorption of SMS (n = 3).

Figure 7. Relative inhibition rate of different absorption enhancers (n = 3).

Figure 8. Mean plasma concentration–time profiles after intranasal application of SMS containing 0.5% laurate SE, 0.5% poloxamer 188 and 0.1% cremophor EL, respectively, in rats, compared with the intranasal control group (15 mgkg⁻¹) and intravenous injection group (3 mgkg⁻¹). Indicated values are the mean of five experiments (n = 5).

Table 1. Main pharmacokinatic parameters after intranasal (i.n.) administration of SMS (15 mg kg⁻¹) with 0.5% laurate SE, 0.5% poloxamer 188 and 0.1% cremophor EL, the control group and intravenous injection group (i.v.) (mean ± SD, n = 5).

Formulation	Cmax (μg/ml)	Tmax (min)	AUC (mg/L*min)	Absolute bioavailability (%)
i.n.0.5% Laurate SE	7.40 ± 1.36	5	501.19 ± 16.95	29.99 ± 3.46*
i.n.0.5% Poloxamer 188	4.85 ± 0.74	5	353.99 ± 16.79	20.90 ± 5.45*
i.n.0.1% Cremophor EL	5.57 ± 0.50	5	395.68 ± 14.45	22.64 ± 1.34*
i.n. Control group	3.12 ± 0.98	10	288.95 ± 8.37	14.61 ± 1.12
i.v. (3 mg/kg)	8.48 ± 1.33	2	362.99 ± 46.75	_

*Significant difference compared with intranasal control group (p < 0.05).