Physicochemical Characterization of Finasteride Nanosystem for Enhanced Topical Delivery

Figures & data

Table 1 Microstructure and Composition of Various Developed Formulations of Finasteride Nanosystems

Formulation	Microstructure	Composition (% w/w)
		Drug	Oleic Acid	Span 80	Acetone	Tween 80	Chitosan	Water
F0 (blank)	Oil in water	–	0.77	0.154	0.05	0.154	–	98.872
F1	Oil in water	0.05	0.77	0.154	0.05	0.154	–	98.822
F2	Oil in water	0.05	0.77	0.154	0.05	0.154	0.125	98.697
F3	Oil in water	0.05	0.77	0.154	0.05	0.154	0.25	98.572
F4	Oil in water	0.05	0.77	0.154	0.05	0.154	0.5	98.322
F5	Oil in water	0.05	0.77	0.154	0.05	0.154	1	97.822

Figure 1 Solubility of finasteride in oils and emulgents. Experiments were carried out in triplicate (n=3). Error bar shows standard deviation. Level of significance was determined using Student’s t-test (p<0.05).

Table 2 Physicochemical Characteristics of Finasteride Nanosystems

Formulation	Droplet Size (nm)	Size Distribution (PDI)	Surface Charge (mV)	pH	Specific Viscosity
F0	18 ± 0.2	0.329 ± 0.02	−10.16 ± 0.002	5.4 ± 0.06	0.002 ± 0.06
F1	41.6 ± 0.4	0.480 ± 0.009	−12.89 ± 0.226	5.1 ± 0.05	0.009 ± 0.01
F2	242 ± 8.42	0.316 ± 0.05	56.35 ± 0.63	5.5 ± 0.07	0.266 ± 0.02
F3	344 ± 1.41	0.269 ± 0.006	59.50 ± 1.27	5.6 ± 0.03	0.723 ± 0.01
F4	512± 44.54	0.338 ± 0.03	61.65 ± 1.48	5.4 ± 0.09	6.628 ± 0.06
F5	864 ± 82.23	0.278 ± 0.07	56.10 ± 0.00	5.5 ± 0.02	22.73 ± 0.02

All the experiments were done in triplicate (n=3). Level of significance was determined by employing Student’s t-test (p<0.05).

Figure 2 TEM images of nanosystems. (I) Blank nanosystem (F0). (II) Undecorated finasteride nanosystem (FNS-NS) (F1). (III) 0.125% FNS-NS (F2). (IV) 0.25% FNS-NS (F3). (V) 0.5% FNS-NS (F4). (VI) 1% FNS-NS (F5).

Figure 3 In vitro release profile of finasteride nanosystems. Experiments were performed in triplicate (n=3). Error bar shows standard deviation. Level of significance was determined by one-way ANOVA (p<0.05).

Table 3 Drug Release Kinetics

Formulation	Zero Order (R^2)	First Order (R^2)	Higuchi Model (R^2)	Korsmeyer–Peppas (R^2) (N)		Mechanism of Drug Release
F1	0.652	0.959	0.862	0.833	0.606	Non-Fickian diffusion
F2	0.836	0.964	0.978	0.961	0.699	Non-Fickian diffusion
F3	0.881	0.984	0.980	0.979	0.808	Non-Fickian diffusion
F4	0.913	0.988	0.990	0.948	0.725	Non-Fickian diffusion
F5	0.909	0.968	0.974	0.968	0.731	Non-Fickian diffusion

Figure 4 Ex vivo permeation of finasteride through rat skin. Experiments were performed in triplicate (n=3). Error bar shows standard deviation. Level of significance was determined by one-way ANOVA (p<0.05).

Table 4 Finasteride Nanosystem Patterns of Drug Release, Permeation, Flux and Drug Retention

Formulation	Cumulative Drug Release (%)	Cumulative Drug Permeation (µg/cm^2)	Flux (µg/cm^2/h)	Average Drug Retention (%)
F1	100 ± 2.28	45.18 ± 1.03	1.34 ± 0.005	6.38 ± 0.18
F2	97.31 ± 2.03	31.70 ± 2.01	0.89 ± 0.015	6.89 ± 0.32
F3	93.62 ± 4.26	25.65 ± 1.84	0.74 ± 0.01	8.17 ± 0.06
F4	86.08 ± 3.49	22.26 ± 1.06	0.70 ± 0.02	8.45 ± 1.04
F5	78.73 ± 3.35	16.35 ± 1.25	0.59 ± 0.026	10.81 ± 0.37

Analyses were carried out in triplicate (n=3 ± SD).

Figure 5 Finasteride skin deposition profile. Experiments was performed in triplicate (n=3). Error bar shows standard deviation. Level of significance was determined using Student’s t-test (p<0.05).