Development of ibuprofen nanoliposome for transdermal delivery: Physical characterization, in vitro/in vivo studies, and anti-inflammatory activity

Figures & data

Table I. Composition of formulations (Drug lipid ratio = 1:3).

S.No.	Formulation Code	Composition	Molar ratio (% w/w)
1.	IG	Dispersion of drug (1%) in Carbopol gel	–
2.	ILG-1	PC: Chol: DCP	7/1/1
3.	ILG-2	PC: Chol: DCP	7/1/2
4.	ILG-3	PC: Chol: DCP	7/2/1
5.	ILG-4	PC: Chol: DCP	7/2/2
6.	ILG-5	PC: Chol: DCP	7/3/1
7.	ILG-6	PC: Chol: DCP	7/3/2

IG = Ibuprofen gel (1% in carbopol).

ILG = Ibuprofen liposomal gel (liposomal gel containing 1% drug, suspended in carbopol).

Figure 1. Transmission electron micrograph of ILG-5.

Table II. Physicochemical parameters of various formulations.

Formulation Code	Size(nm)	PDI	ζ potential	Entrapment efficiency	Viscosity (Cps)
IG	–	–	–	–	9035
ILG-1	162 ± 3.3	0.413	− 71 ± 1.1	33 ± 2.4	10121
ILG-2	161 ± 3.1	0.422	− 74 ± 1.2	35 ± 2.3	10115
ILG-3	174 ± 3.8	0.429	− 73 ± 1	41 ± 2.8	10211
ILG-4	166 ± 2.6	0.392	− 76 ± 1.3	44 ± 2.5	10192
ILG-5	159 ± 3.6	0.331	− 70 ± 0.9	49 ± 2.6	10201
ILG-6	173 ± 3.9	0.461	− 73 ± 1.1	48 ± 2.8	10175

Size, PDI, Zeta potential, Entrapment efficiency for vesicular formulation; viscosity for corresponding gel (1% carbopol 934).

Figure 2. Pattern of in vitro drug release in 24 h for different formulations.

Figure 3. Pattern of ex vivo drug permeation in 24 h for different formulations.

Table III. Different permeation parameters for nanoliposome formulations.

Formulation code	Flux (μg/cm^2/h)	Lag time (Hrs.)	Permeability coefficient (cm/h × 10^−2)	Distribution Parameter (cm^2/h)
IG	0	0	0	0
ILG-1	0.527	0.643	0.0527	2.332
ILG-2	0.489	0.697	0.0489	2.152
ILG-3	0.417	0.901	0.0417	1.664
ILG-4	0.461	0.75	0.0461	2
ILG-5	0.635	0.613	0.0635	2.446
ILG-6	0.462	0.863	0.0462	1.738

Figure 4. In vivo drug permeation study.

Table IV. In vivo study data of the IG, IOS, and ILG-5.

Formulation code	Cmax (μg/ml)	Tmax (hrs)	AUC (μg.hr/ml)
IG	0.68 ± 0.01	6	7.395
IOS	2.8 ± 0.08	2	19.98
ILG-5	7.35 ± 0.59	6	110.1

All data are expressed as mean ± S.D.; n = 6; (p ≤ 0.05).

Figure 5. Anti-inflammatory activity.