Proniosomal gel-mediated transdermal delivery of bromocriptine: in vitro and ex vivo evaluation

Figures & data

Table 1. Entrapment efficiency and vesicle size of different proniosomal formulations.

Code	Drug (mg)	Span 20 (mg)	Span 40 (mg)	Span 60 (mg)	Span 80 (mg)	Tween 20 (mg)	Tween 60 (mg)	Tween 80 (mg)	Lecithin (mg)	Cholesterol (mg)	Vesicle size (µm)	Polydispersity index	Entrapment efficiency (%)
F1S20	5	90	−	−	−	−	−	−	90	10	1.2 ± 0.049	0.409 ± 0.021	94.9 ± 0.23
F2S40	5	−	90	−	−	−	−	−	90	10	1.1 ± 0.045	0.910 ± 0.091	97.8 ± 0.27
F3S60	5	−	−	90	−	−	−	−	90	10	1.3 ± 0.034	0.044 ± 0.020	98.9± 0.19
F4S80	5	−	−	−	90	−	−	−	90	10	1.0 ± 0.052	0.523 ± 0.071	96.8 ± 0.35
F5T20	5	−	−	−	−	90	−	−	90	10	1.2 ± 0.055	0.566 ± 0.063	93.3 ± 0.41
F6T60	5	−	−	−	−	−	90	−	90	10	2.6 ± 0.070	0.088 ± 0.013	91.8 ± 0.38
F7T80	5	−	−	−	−	−	−	90	90	10	1.6 ± 0.055	0.409 ± 0.012	94.4 ± 0.43
F8SSL	5	−	−	45	−	−	−	−	90	10	2.0 ± 0.061	1.0 ± 0.063	87.9 ± 0.35
F9SSH	5	−	−	135	−	−	−	−	90	10	2.6 ± 0.096	0.02 ± 0.013	97.01 ± 0.27
F10SCL	5	−	−	90	−	−	−	−	90	5	2.3 ± 0.045	0.56 ± 0.061	85.2 ± 0.35
F11SCH	5	−	−	90	−	−	−	−	90	15	1.2 ± 0.078	0.018 ± 0.029	87.17 ± 0.72
F12SLL	5	−	−	90	−	−	−	−	45	10	1.0 ± 0.034	0.046 ± 0.038	85.0 ± 0.72
F13SLH	5	−	−	90	−	−	−	−	135	10	2.6 ± 0.068	0.96 ± 0.071	99.0 ± 1.45
F14SDL	3	−	−	90	−	−	−	−	90	10	0.7 ± 0.024	0.66 ± 0.063	99.1 ± 0.72
F15SDH	7	−	−	90	−	−	−	−	90	10	3.5 ± 0.068	0.18 ± 0.025	90.9 ± 0.55

Figure 1. Photomicrograph of proniosomal formulation F₃S₆₀ (A). SEM image of niosomes formed after hydration of F₃S₆₀ (B), F₁₀S_CL (C) and F₁₁S_CH (D).

Figure 2. DSC thermograms of bromocriptine proniosomes (A), blank proniosomes (B), span 60 (C) and bromocriptine (D).

Figure 3. In vitro drug release from proniosomes prepared using different cholesterol (A) and drug (B) content (n = 3). Amount of cholesterol was 5 mg (F₁₀S_CL), 10 mg (F₃S₆₀) and 15 mg (F₁₁S_CH), and the amount of bromocriptine was 3 mg (F₁₄S_DL), 5 mg (F₃S₆₀) and 7 mg (F₁₅S_DH).

Figure 4. Ex vivo release of bromocriptine from proniosomes and drug dispersion (n = 3).

Table 2. Permeation parameters of drug dispersion and proniosomal formulation.

Formulation	Transdermal flux (Jss) (µg/cm^2/h)	Permeation coefficient (cm^2/h)	Enhancement ratio
Drug dispersion	3.67 ± 0. 18	0.0048 ± 0.0004	4.40 ± 0.23
Proniosomal gel	16.15 ± 0.832	0.00734 ± 0.00012

Note: All values are expressed as mean ± SD; n = 3.

Table 3. Stability study of the optimised proniosomal formulation (F₃S₆₀).

	4 ± 2 °C		25 ± 2 °C/60 ± 5% RH		40 ± 2 °C/75 ± 5% RH
Storage time (days)	Vesicle size (µm)	EE (%)	Vesicle size (µm)	EE (%)	Vesicle size (µm)	EE (%)
0	1.3 ± 0.049	98.9 ± 0.19	1.3 ± 0.049	98.9 ± 0.19	1.3 ± 0.049	98.9 ± 0.19
30	1.3 ±0.048	98.9 ± 0.38	1.3 ± 0.052	98.1 ± 0.33	1.3 ± 0.047	97.9 ± 0.40
60	1.3 ± 0.041	98.7 ± 0.45	1.3 ± 0.071	98.0 ± 0.41	1.4 ± 0.050	95.0 ± 0.56
90	1.3 ± 0.042	98.6 ± 0.50	1.3 ± 0.069	97.7 ± 0.38	1.8 ± 0.051	93.9 ± 0.58

Note: All values are expressed as mean ± SD; n = 3.

EE: entrapment efficiency.