Formulation and characterization of floating microballoons of Nizatidine for effective treatment of gastric ulcers in murine model

Figures & data

Table 1. Process variables of nizatidine-loaded microballoons.

Formulation variable	Particle size (µm)	% Entrapment efficiency	% Buoyancy (after 6 h)
Polymer ratio
1:1	268.6 ± 4.6	51.4 ± 3.2	65.6 ± 3.4
1:2	272.4 ± 6.8	56.7 ± 2.8	79.4 ± 3.8
1:3	292.8 ± 4.3	65.4 ± 4.6	81.8 ± 2.8
1:4	308.5 ± 2.4	59.3 ± 3.8	73.4 ± 4.2
Drug:Polymer ratio
1:1	266.6 ± 4.3	56.8 ± 3.6	65.2 ± 3.2
1:2	271.4 ± 6.2	60.6 ± 2.2	78.5 ± 4.5
1:3	290.5 ± 4.1	68.2 ± 4.2	85.6 ± 2.4
1:4	292.8 ± 1.4	68.2 ± 4.1	79.5 ± 2.8
Emulsifier concentration (%w/v)
0.50	292.7 ± 3.3	67.6 ± 3.5	86.6 ± 2.8
0.75	284.2 ± 4.6	61.2 ± 4.8	84.3 ± 4.1
1.00	262.4 ± 3.6	59.6 ± 3.4	81.6 ± 2.2
1.25	249.6 ± 4.2	55.6 ± 2.8	72.8 ± 4.6
Stirring speed (rpm)
300	304.4 ± 2.4	69.4 ± 1.2	80.4 ± 2.6
500	290.2 ± 5.2	64.8 ± 4.2	83.64 ± 3.2
700	274.6 ± 3.6	59.8 ± 5.2	74.8 ± 4.6

Table 2. Formula for the preparation of microballoons after optimization.

Optimized parameter	Value
Polymer ratio	1:3
Drug: polymer ratio	1:4
Emulsifier concentration (%w/v)	0.5
Stirring speed (rpm)	900
Stirring time (hour)	3

Figure 1. SEM photomicrograph of nizatidine-loaded microballoons.

Figure 2. In-vitro release profile of optimized nizatidine microballoons (n = 3).

Figure 3. X-ray photographs of microballoons in the gastric region of rat after dosing of formulations in the fasted state: (a) before dosing, (b) 3 h after dosing, (c) 6 h after dosing.

Figure 4. Evidence for the protective effect of nizatidine microballoons in rats treated with ethanol, (a) control group showing normal gastric integrity (b) nizatidine solution–treated group (100 mg/kg) (c) Nizatidine-loaded microballoons–treated group.