Development of enteric-coated microspheres of embelin for their beneficial pharmacological potential in ulcerative colitis

Figures & data

Figure 1. Scanning electron microscopic (SEM) image of polymeric microparticle.

Table 1. Effect of formulation parameters on particle size and entrapment efficiency.

Formulation	Parameters	Values	Particle size	Entrapmentefficiency
F1	EC:ES 100:drug	1:1:0.3	13.5 μm ± 1.2	81.2 ± 3.4%
F2		2:1:0.3	21.3 μm ± 1.6	75.5 ± 1.2%
F3		1:2:0.3	17.5 μm ± 3.9	53.5 ± 3.9%
F4		0:1:0.3	8.7 μm ± 4.3	54.9 ± 4.34%
F5	Crosslinking agent	0.1 ml	5.08 μm ± 0.8	73.6 ± 4.4%
F6		0.2 ml	11.7 μm ± 1.7	79.5 ± 3.1%
F7		0.3 ml	26.1 μm ± 2.4	81.2 ± 3.4%
F8	Span 80	0.5%	28.5 μm ± 1.4	84.8 ± 1.5%
F9		1%	23.2 μm ± 1.5	83.5 ± 2.3%
F10		1.5%	19.9 μm ± 3.8	80.8 ± 1.8%
F11		2%	12.6 μm ± 2.1	79.5 ± 2.3%
F12		2.5%	17.4 μm ± 0.8	60.1 ± 2.8%

Bold values indicate the optimized values also have been considered as the best values of size, concentration of crosslinking agent and span to avail maximum entrapment efficiency of formulation.

Figure 2. % Drug release with respect to time. Values expressed as mean ± SD (n = 3).

Table 2. Drug release kinetics of different formulations.

S.no.	Formulation	Zeroorder (R^2)	Firstorder (R^2)	Peppasmodel (R^2)	Higuchimodel (R^2)
1	F1 (1:1)	0.9588	0.9961	0.7947	0.8594
2	F2 (1:2)	0.7176	0.8253	0.5947	0.9427
3	F3 (2:1)	0.7129	0.8817	0.6108	0.9279
4	F4 (0:1)	0.5283	0.7957	0.4974	0.8508

Table 3. Macroscopic scoring for evaluation of disease in different treatment groups.

Treatment	Scores (% weight loss)	Stool consistency	Lesion scores	Macroscopic scores
Group I (normal control)	0.0 ± 0	0.0 ± 0	0.0 ± 0	0
Group II (colitis control)	3 ± 0.02^a	4 ± 0.05^a	4 ± 0.01^a	4 ± 0.01^a
Group III (acetic acid + plain embelin (50 mg/kg)	2 ± 0.04^b	2 ± 0.03^b	3 ± 0.02^b	3 ± 0.02^b
Group IV (acetic acid + embelin-loaded microparticles)	2 ± 0.03^b	1 ± 0.05^b	2 ± 0.05^b	2 ± 0.03^b
Group V (acetic acid + mesalamine)	1 ± 0.05^b	1 ± 0.05^b	1 ± 0.01^b	1 ± 0.03^b

Values are given as mean ± SEM; values are statistically significant at ^ap < 0.05 as compared to normal and ^bp < 0.05 as compared to colitis control rats.

Table 4: Scoring chart for the evaluation of disease.

For weight change	Stool consistency	Lesion score
0 score – 0%	0 score – well-formed pellets	0 score – no
1 score – 1–5%	1 score – hard	1 score – hyperemia at sites
2 score – 5–10%	2 score – semisolid	2 score – lesion having diameter less than 1 mm
3 score – 10–20%	3 score – pasty	3 score – lesion having diameter less than 2 mm
4 score – above 20%	4 score – liquid diameter	4 score – lesion having diameter less than 3

Figure 3. Effect of embelin on MPO level of acetic acid induced colitis in female wistar rats. Values are given as mean ± SEM; values are statistically significant at ^ap < 0.05 as compared to normal and ^bp < 0.05 as compared to colitis control rats.

Figure 4. Effect of embelin on LPO level of acetic acid induced colitis in female wistar rats. Values are given as mean ± SEM; values are statistically significant at ^ap < 0.05 as compared to normal and ^bp < 0.05 as compared to colitis control rats.

Figure 5. Effect of embelin on GSH level of acetic acid induced colitis in female wistar rats. Values are given as mean ± SEM; values are statistically significant at ^ap < 0.05 as compared to normal and ^bp < 0.05 as compared to colitis control rats.

Figure 6. (A) Normal control. (B) Colitis control. (C) Plain embelin (50 mg/kg)+acetic acid. (D) Embelin-loaded microspheres + acetic acid. (E) Standard drug, i.e., mesalamine (100 mg/kg)+acetic acid.