Novel tamarind seed polysaccharide-alginate mucoadhesive microspheres for oral gliclazide delivery:in vitro–in vivoevaluation

Abstract

Novel tamarind seed polysaccharide (TSP)-alginate mucoadhesive microspheres were prepared using TSP and alginate as blend in different ratios with different calcium chloride (CaCl 2 ) concentration as a cross linker by ionotropic gelation. The prepared microspheres were of spherical shape having rough surfaces, and average particle sizes within the range of 752.12 ± 6.42 to 948.49 ± 20.92 µm. The drug entrapment efficiency of these microspheres were within the range between 58.12 ± 2.42 to 82.78 ± 3.43% w/w. Fourier transform infrared (FTIR) studies indicated that there were no reactions between gliclazide, and polymers (TSP, and sodium alginate) used. Different formulations of gliclazide loaded TSP-alginate microspheres showed prolonged in vitro release profiles of gliclazide over 12 hours in both stomach pH (pH 1.2), and intestinal pH (pH 7.4). It was found that the gliclazide release in gastric pH was comparatively slow and sustained than intestinal pH. These TSP-alginate microspheres also exhibited good mucoadhesivity. The in vivo studies on alloxan-induced diabetic rats (Animal Ethical Committee registration number: IFTM/837ac/0160) demonstrated the significant hypoglycemic effect of selected formulation of TSP-alginate mucoadhesive microspheres containing gliclazide on oral administration. This developed gliclazide loaded new TSPalginate mucoadhesive microspheres may be very much useful for prolonged systemic absorption of gliclazide for proper maintaining blood glucose level and advanced patient compliance.

Probucol Release from Novel Multicompartmental Microcapsules for the Oral Targeted Delivery in Type 2 Diabetes

“…All experiments were done in triplicate (n=3). The swelling index of the microcapsules was calculated from the following formula (16,17):…”

Antihyperglycemic Activity of Phenyl and Ortho-Hydroxy Phenyl Linked Imidazolyl Triazolo Hydroxamic Acid Derivatives

“…The capability of FP1-FP12 is to protect the body from weight loss as a result of to reduce hyperglycemia. The outcomes of this study showed that synthesized hydroxamic acid derivatives (FP1-FP12) have a hypoglycemic effect in streptozotocin-induced diabetic rats [28][29][30][31][32][33][34][35][36][37][38]. The antihyperglycemic effects of FP1-FP12 may be mediated through an increase in insulin secretion, the inhibition of gluconeogenesis and glycogenolysis and/or protection of pancreatic β-cells from streptozotocin and glucose-induced oxidative stress.…”

Tamarind Seed Polysaccharide: An Emerging Excipient for Pharmaceutical Use

“…In another investigation, the same group developed and evaluated tamarind seed polysaccharide-alginate mucoadhesive microspheres containing gliclazide by varying ratios of polymer-blends and calcium chloride concentrations in cross-linking solution through ionotropicgelation. 96 The drug entrapment efficiencies in these microspheres were 58.12 ± 2.42 to 82.78 ± 3.43% w/w; whereas microparticle sizes were 752.12 ± 6.42 to 948.49 ± 20.92 μm. These microspheres showed prolonged in-vitro release of gliclazide over 12 h. Both the metformin HCl-loaded beads and gliclazide-loaded microspheres made of tamarind seed polysaccharidealginate blends showed good ex-vivo mucoadhesivity with the biological membrane in wash-off test.…”

“…93,94 The same research group has developed also tamarind seed polysaccharide-blended alginate mucoadhesive beads and microspheres through ionotropic-gelation. 95,96 Mucoadhesive beadscomposed of tamarind seed polysaccharide-alginate blends for oral delivery of metformin HCl were developed and optimized. 95 The optimized beads exhibited 94.86 ± 3.92% drug encapsulation efficiency and average diameter of 1.24 ± 0.07 mm.…”

“…[93][94][95][96] Mucoadhesive beads containing metformin HCl made of low methoxy pectintamarind seed polysaccharide polymer-blends were developed through ionotropic-gelation technique and optimized. 93 The optimized calcium pectinate-tamarind seed polysaccharide beads containing metformin HCl showed drug encapsulation efficiency of 95.12 ± 4.26% and mean diameter of 1.93 ± 0.26 mm.…”