Development and characterization of enteric-coated microparticles of biochanin A for their beneficial pharmacological potential in estrogen deficient-hypertension

Figures & data

Figure 1. (a) Zetasizer and PDI of drug-loaded biochanin A microparticle (BAMP). (b) Zeta-sizer and PDI of ECMPs of biochanin A.

Figure 2. (a) FTIR spectrum of BAMP and (b) FTIR spectrum of ECMP.

Table 1. Optimization of drug, BAMP and ECMP.

F. No.	Drug (biochanin A)	Pectin (%)	Sodium alginate (%)	Calcium chloride (%)	Ethyl cellulose (%)	Diameter (µm)	PDI	% Entrapment
F1	–	1	2	6	–	4.407 ± 0.22	0.290	–
F2	–	2	2	6	–	4.52 ± 0.27	0.288	–
F3	–	3	2	6	–	8.949 ± 0.35	0.274	–
F4	–	4	2	6	–	2.719 ± 0.12	0.324	–
F5	–	6	2	6	–	3.092 ± 0.16	0.252	–
F6	–	7	2	6	–	5.254 ± 0.33	0.518	–
F7	1	1	2	6	–	3.36 ± 0.17	0.290	98.94 ± 0.45
F8	2	2	2	6	–	3.94 ± 0.29	0.288	92.3 ± 1.32
F9	1	6	2	6	3	4.96 ± 0.47	0.25	94 ± 0.96
F10	1	4	2	6	3	5.14 ± 0.49	0.45	93.1 ± 2.42

F7 represents optimized Pectin Microparticulate formulation

F9 represents optimized ethyl cellulose coated formulation (ECMP)

Table 2. FTIR frequency of observed peaks of biochanin A-loaded pectin microparticles (BAMP) and its interpretation.

Biochanin A peaks (cm^−1)	Frequency range (cm^−1)	Interpretation
3426.82	3600–3200	Phenolic OH stretch
1647.5	1716 and 1675	Stretching vibration of C = O
1019.06	1000–1300	C–O stretch

Table 3. FTIR frequency of observed peaks of ethyl cellulose-coated pectin microparticles of biochanin A (ECMP) and its interpretation.

Biochanin A peaks (cm^−1)	Frequency range (cm^−1)	Interpretation
3482.06	3600–3200	Phenolic OH stretch
1734.92	1716 and 1675	Stretching vibration of C = O
1111.10	1000–1300	C–O stretch

Figure 3. In vitro drug release versus time.

Figure 4. In vivo pharmacokinetic studies.

Table 4. Pharmacokinetic parameters of ECMP of biochanin A and pure drug (biochanin A) calculated by using plasma concentration time data using Thermo Kinetica, Version 5.0 (Thermo Fisher Scientific, Waltham, MA).

Pharmacokinetic parameters	Biochanin A	ECMP
Cmax (µg/ml)	80.2 ± 5.92	110.9 ± 7.85
Tmax (h)	2.88 ± 0.27	3.88 ± 0.47
AUC total (h µg/ml)	80.24 ± 7.05	120.65 ± 9.75
t1/2 (h)	6.16 ± 0.45	8.12 ± 0.42
Dose (mg/kg)	2.4	10

Figure 5. Effect of pharmacological interventions on systolic blood pressure in ovariectomized hypertensive rats.

Figure 6. Effect of pharmacological interventions on diastolic blood pressure in ovariectomized hypertensive rats.

Figure 7. Effect of pharmacological interventions on mean arterial pressure in ovariectomized hypertensive rats.

Figure 8. Effect of pharmacological intervention on lipid peroxidation in ovariectomized hypertensive rats.

Figure 9. Effect of pharmacological intervention on reduced GSH in ovariectomized hypertensive rats.

Figure 10. Effect of pharmacological intervention on serum nitrite in ovariectomized hypertensive rats.

Figure 11. Effect of pharmacological intervention on TNF-α in ovariectomized hypertensive rats.

Figure 12. (a) Histology slides of Group A: Sham Control, Group B: Ovx-HT, Group C: Ovx-HT+BCA, Group D: Ovx-HT + BCA + L-NAME. (b) Histology slides of Group E: Ovx-HT + ECMP, Group F: Ovx-HT + ECMP + L-NAME, Group G: Ovx-HT + Lisinopril.