Development and biological evaluation of vesicles containing bile salt of telmisartan for the treatment of diabetic nephropathy

Figures & data

Figure 1. Effect of formulation compositions on (A) vesicles size, (B) polydispersity index, (C) zeta potential, (D) entrapment efficiency of TS-loaded vesicles containing bile salt. Formulations F1, F2, F3, F4, F5, F6 contained SoyPC/ NaDC in 9/1, 7/1, 6/1, 5/1, 4/1, 3/1 ratio, respectively. NaDC: sodium deoxycholate; SoyPC: soybean phosphatidylcholine; TS: telmisartan.

Figure 2. Transmission electron microscopy of TS-loaded optimized formulation F4 contained SoyPC and NaDC in 5/1 ratio. Abbreviations: NaDC, sodium deoxycholate; SoyPC, soybean phosphatidylcholine; TS, telmisartan.

Table 1. Effects of TS suspension and formulation F4 on kidney function test in streptozotocin-induced diabetic nephropathy rats (mean ± SEM).

Variables	Normal control	Diabetic nephropathy	TS suspension	Formulation F4
Creatinine (mg/dl)	0.456 ± 0.016	1.138 ± 0.042	0.630 ± 0.030	0.502 ± 0.020
Urea (mg/dl)	24.350 ± 0.882	55.723 ± 1.234	34.127 ± 1.714	24.650 ± 0.716
LDH (U/l)	61.731 ± 0.990	227.584 ± 6.314	125.679 ± 1.638	90.999 ± 3.990
Urinary total protein (g/l)	6.373 ± 0.227	32.661 ± 0.723	18.095 ± 0.906	11.156 ± 0.693

TS: telmisartan; LDH: lactate dehydrogenase.

Table 2. Effects of TS suspension and formulation F4 on antioxidant enzymes and oxidative stress markers in streptozotocin-induced diabetic nephropathy rats (mean ± SEM).

Variables	Normal control	Diabetic nephropathy	TS suspension	Formulation F4
CAT (U/mg protein)	11.742 ± 0.516	5.205 ± 0.257	7.541 ± 0.496	10.814 ± 0.431
NP-SH (nmol/g)	7.957 ± 0.340	1.979 ± 0.075	4.711 ± 0.231	6.305 ± 0.184
MDA (nmol/mg)	29.840 ± 1.410	54.863 ± 1.174	44.875 ± 2.329	36.860 ± 2.041
NO (nM/mg protein)	29.898 ± 0.768	52.682 ± 1.327	41.347 ± 0.839	33.260 ± 0.758

TS: telmisartan; CAT: catalase; NP-SH: non-protein sulfhydryl; MDA: malondialdehyde; NO: nitric oxide.

Figure 3. Effect of TS suspension and formulation F4 on (A) MPO, (B) TNF-α, (C) IL-6 in streptozotocin-induced diabetic nephropathy rats (mean ± SEM). IL-6: interleukin 6; MPO: myeloperoxidase; TNF-α: tumour necrosis factor-α; TS: telmisartan.

Figure 4. Effect of TS suspension and formulation F4 on protein expression by immunoblotting of (A) iNOS, (B) AT₁R in streptozotocin-induced diabetic nephropathy rats (mean ± SEM). Abbreviation: AT₁R, angiotensin II type 1 receptor; iNOS, inducible nitric oxide synthase; TS: telmisartan.

Figure 5. Effect of TS suspension and formulation F4 on histopathological changes in kidney tissue of streptozotocin-induced diabetic nephropathy rats. Representative section of (A) control, (B) diabetic nephropathy, (C) treated with TS suspension, (D) treated with formulation F4. TS: telmisartan.