Formulation, in-vitro and in-vivo pharmacokinetic evaluation of simvastatin nanostructured lipid carrier loaded transdermal drug delivery system

Brito Raj, S; Chandrasekhar, Kothapalli Bonnoth; Reddy, Kesavan Bhaskar

doi:10.1186/s43094-019-0008-7

Future Journal of Pharmaceutical Sciences

Table 1 Evaluation on effect of various independent and dependent variables on simvastatin NLC characteristics (n = 3), Box-Behnken—multiple linear regression method

From: Formulation, in-vitro and in-vivo pharmacokinetic evaluation of simvastatin nanostructured lipid carrier loaded transdermal drug delivery system

Std	Run	Independent variables						Dependant variables			Other variables
Std	Run	Factor A: (Compritol 188ATO : Softigen) X1 in mg	Factor B: surfactant (Span 80) X2 in mg	Factor C: Homo. speed (15,000 rpm) time X3 min	Factor A: X1 in mg	Factor B: X2 in %	Factor C: X3 min	PS Y1 nm	ZP Y2 mV	EE Y3 %	% drug content
15	1	0	0	0	8: 2	0.5	10	197.6 ± 2.64	− 26.8 ± 2.04	76.62 ± 3.62	87.24 ± 1.48
14	2	0	0	0	8: 2	0.5	10	195.2 ± 3.2	− 23.8 ± 2.06	76.82 ± 2.86	84.48 ± 2.02
1	3	− 1	− 1	0	7:3	0.25	10	145.4 ± 2.46	− 13.1 ± 2.02	90.40 ± 2.42	88.62 ± 2.24
4	4	1	1	0	9:1	1.0	10	675.9 ± 2.66	− 32.3 ± 2.16	56.28 ± 3.84	67.34 ± 2.42
11	5	0	− 1	1	8: 2	0.25	15	192.5 ± 2.56	− 19.9 ± 2.24	78.64 ± 3.26	86.54 ± 2.68
16	6	0	0	0	8: 2	0.5	10	193.2 ± 3.86	− 22.8 ± 2.22	76.28 ± 2.32	86.56 ±2.94
3	7	− 1	1	0	7:3	1.0	10	125.4 ± 2.66	− 33.6 ± 2.42	88.40 ± 2.44	89.42 ± 2.86
17	8	0	0	0	8: 2	0.5	10	203.3 ± 3.46	− 21.4 ± 2.12	76.84 ± 3.66	76.24 ± 2.48
13	9	0	0	0	8: 2	0.5	10	207.1 ± 2.36	− 22.0 ± 2.24	75.42 ± 2.86	79.86 ± 2.68
10	10	0	1	− 1	8:2	1.0	5	201.1 ± 2.26	− 30.7 ± 2.68	76.80 ± 3.44	78.56 ± 2.66
9	11	0	− 1	− 1	8: 2	0.25	5	194.8 ± 3.16	− 13.1 ± 2.10	74.50 ± 2.86	79.84 ± 2.08
8	12	1	0	1	9:1	0.5	15	511.0 ± 2.06	− 26.5 ± 2.12	58.84 ± 3.60	62.54 ± 3.42
6	13	1	0	− 1	9:1	0.5	5	695.8 ± 3.26	− 23.5 ± 2.06	54.50 ± 3.98	56.44 ± 3.42
5	14	− 1	0	− 1	7:3	0.5	5	168.7 ± 2.46	− 24.7 ± 2.54	92.20 ± 2.46	83.44 ± 3.12
12	15	0	1	1	8: 2	1.0	15	195.1 ± 2.66	− 33.4 ± 2.32	77.24 ± 3.76	78.54± 2.20
2	16	1	− 1	0	9:1	0.25	10	667.0 ± 3.86	− 17.2 ± 2.10	56.40 ± 2.66	54.34 ± 4.24
7	17	− 1	0	1	7:3	0.5	15	145.3 ± 2.66	− 21.7 ± 2.68	89.40 ± 3.64	84.52 ± 2.08

Run7, i.e., formulation F7 is the desired optimized formulation with preferred particle size of 125.4 ± 2.66 nm with good stability, based on good surface charge potential, i.e., zeta potential of − 33.6 ± 2.42 mV and good drug entrapment efficiency of 88.40 ± 2.44%.

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