A novel drug delivery gel of terbinafine hydrochloride with high penetration for external use

Figures & data

Table 1. The entrapment efficiency and particle size of transfersomes under different preparation degree.

Temperature (°C)	Entrapment efficiency (%)	Particle size
40	93.5 ± 0.35	67.5 ± 0.68
45	95.2 ± 0.26	68.0 ± 0.92
50	90.5 ± 0.39	69.5 ± 0.86
55	86.7 ± 0.40	69.6 ± 0.67

Table 2. The entrapment efficiency of transfersomes containing different kinds of surfactants.

Surfactant	Surfactant dosage (mg)	Drug content (mg/mL)	Entrapment efficiency (%)
NaDC	50	9.64 ± 0.32	96.8 ± 0.30
SDS	50	9.74 ± 0.15	97.5 ± 0.21
SC	50	9.61 ± 0.30	98.8 ± 0.62
TW-80	150	9.81 ± 0.27	95.4 ± 0.51
BrijS20	150	9.75 ± 0.29	94.2 ± 0.47
AEO-9	150	9.70 ± 0.41	97.7 ± 0.39
RH-40	150	9.90 ± 0.26	98.1 ± 0.35
EL-35	150	9.62 ± 0.28	96.3 ± 0.33

Figure 1. (A) Accumulative amount of drug permeated in 12 h under different pH of the PBS buffer and (B) the amount of drug remained in the skin under different pH of the PBS buffer. Data represents mean with standard deviation at n = 3.

Figure 2. (A) Accumulative amount of drug permeated in 12 h under different drug loading and (B) the amount of drug remained in the skin under different drug loading. Data represents mean with standard deviation at n = 3.

Figure 3. (A) Accumulative amount of drug permeated in 12 h under different surfactants and (B) the amount of drug remained in the skin under different surfactants. Data represents mean with standard deviation at n = 3.

Table 3. The entrapment efficiency and particle size of transfersomes containing different amount of drug.

Drug dosage (mg)	Entrapment efficiency (%)	Particle size (nm)
100	95.2 ± 0.43	60.7 ± 1.88
150	90.4 ± 0.39	69.8 ± 1.96
200	80.2 ± 0.37	70.06 ± 1.67

Table 4. The optimized formulation of terbinafine hydrochloride transforsomes.

Type of excipients	Dosage of excipients
Terbinafine hydrochloride	100 mg (1%,w/v)
Phospholipids	450 mg (4.5%,w/v)
Tween-80	150 mg (1.5%,w/v)
Sodium cholesteryl sulfate	100 mg (1%,w/v)
Anhydrous ethanol	2 mL (20%,v/v)
Sodium benzoate	50 mg (0.5%,w/v)
Sodium pyrosulfate	20 mg (0.2%,w/v)
pH 5.00 phosphate buffer	10 mL

Figure 4. (A) Accumulative amount of drug permeated in 12 h and (B) the amount of drug remained in the skin of the transfersomes gel and the Lamisil cream. Data represents mean with standard deviation at n = 3.

Table 5. The stability of the transfersomes gel in one month.

Time (d)	Appearance	pH	Drug content (mg/mL)	Entrapment efficiency (%)
0	Smooth white gel, no stratification	4.38 ± 0.01	4.45 ± 0.15	94.5 ± 0.53
5	Smooth white gel, no stratification	4.33 ± 0.02	4.41 ± 0.12	94.2 ± 0.39
10	Smooth white gel, no stratification	4.35 ± 0.01	4.46 ± 0.20	94.6 ± 0.44
30	Smooth white gel, no stratification	4.31 ± 0.01	4.44 ± 0.17	94.0 ± 0.30
120	Smooth white gel, no stratification	4.16 ± 0.01	4.45 ± 0.20	94.2 ± 0.43

Table 6. The in vitro relative recovery of the probe.

	Dialysis	Reverse dialysis
Flow rate (µL/min)
1.0	75.09 ± 2.13	77.63 ± 3.50
1.5	71.32 ± 4.00	72.08 ± 3.83
2.0	63.04 ± 2.90	68.75 ± 1.35
Concentration (µg/mL)
1	71.75 ± 4.42	73.10 ± 4.00
5	70.53 ± 2.59	73.32 ± 5.11
10	71.32 ± 4.00	72.08 ± 3.83

Figure 5. (A) In vivo recovery of the probe in reverse dialysis during 10 h and (B) the drug concentration-time curves of the transfersomes gel and the Lamisil cream. Data represents mean with standard deviation at n = 3.

Table 7. The pharmacokinetic parameters.

Parameters	Unit	Transfersomes gel	Lamisil cream
t1/2	h	8.6	6.03
K	1/h	0.08	0.12
Cmax	µg/L	869.67	313.12
Tmax	h	1	0.5
AUC0→t	µg/L × h	5096.57	1738.60
AUC0→∞	µg/L × h	7422.96	2489.69

Figure 6. Electron microscopy figure of terbinafine transfersomes (× 50 000).