Current Science

Sunil K. Jain ¹, Ashok K. Sahoo ¹, Mukesh Gupta ¹, Aditya Nath Pandey ¹, Amrish Kumar ¹, Akhlesh K. Jain ¹

Affiliations
1 Department of Pharmaceutics, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (a Central University), Bilaspur 495 009, IN

Abstract

The main aim of this work is to develop and thoroughly evaluate resin-based multiparticles of repaglinide for effective management of type-2 diabetes mellitus. Repaglinide was complexed with cholestyramine resin; later the resin complexed drug was encapsulated in ethylcellulose microspheres. The microspheres were characterized for micromeritic properties, SEM analysis, entrapment efficiency, percentage yield, IR spectroscopy, buoyancy behaviour and in vitro drug release in simulated gastric fluid. Microparticles showed regular shape and spherical morphology with entrapment efficiency in the range 51-69%. Differential scanning calorimetry confirmed that there was no chemical interaction between the polymer and the drug. Resin-based microspheres showed good buoyancy behaviour (P < 0.05) due to the presence of bicarbonate ions and sustained release compared to plain drug microspheres (P < 0.05). Finally, the effectiveness of the formulations was evaluated in vivo for blood glucose lowering effect in both normal and streptozotocin-induced diabetic rats. Blood glucose lowering effect induced in diabetic rats by the repaglinide- loaded microspheres was significantly greater (P < 0.05) and prolonged (∼8 h) compared to plain drug microspheres. In a nutshell, floating microspheres containing drug resin complex were able to sustain the drug release in an effective manner for prolonged periods of time and proven in vivo effectiveness by reducing blood glucose level for a longer duration.

Keywords

Cholestyramine, Diabetes Mellitus, Ethylcellulose, Microspheres, Repaglinide.

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Sunil K. Jain ¹, Mukesh Gupta ¹, Ashok K. Sahoo ¹, Aditya N. Pandey ¹, Akhlesh K. Jain ¹

Affiliations
1 Department of Pharmaceutics, SLT Institute of Pharmaceutical Sciences, Guru Ghasidas Vishwavidyalaya (A Central University), Bilaspur 495 009, IN

Abstract

Helicobacter pylori mainly exists deep inside the gastric mucosae and adheres to epithelial cells of the stomach. In the present work, concanavalin-A (Con-A) conjugated gastro-retentive microspheres of amoxicillin trihydrate (AMT) were formulated and thoroughly evaluated. Eudragit S100 microspheres were prepared by emulsion solvent diffusion method and characterized for micromeritic properties, per cent drug entrapment, per cent yield, surface morphology, buoyancy behaviour and in vitro drug release in simulated gastric fluid. The microspheres were then conjugated with Con-A and conjugation was verified by IR spectroscopy and differential scanning calorimetry. Moreover, Con-A conjugated microspheres were further characterized for zeta potential, mucoadhesiveness to gastric mucosae and Con-A conjugation efficiency. The microparticles were found to be regular and spherical in shape with a size range 106.4-192.4 μm depending on drug to polymer ratio (1:1 to 1:3). All the microsphere formulations showed noteworthy drug entrapment from 62.3% to 70.2%. In vitro floating test clearly showed that most of the microspheres were floating even after 12 h of testing period. Zeta potential of optimized formulation and Con-A conjugated microspheres was found to be 5.6 and 18.7 mV respectively. Attachment of lectin to the Eudragit microspheres significantly increases the muco-adhesiveness (83.7%) compared to non-conjugated microspheres (16.7%) and also controlled the release of drug in simulated GI fluids. The results suggest that these carriers can be used to incorporate other antibiotic agents and could provide better therapeutic effect against H. pylori infection.

Keywords

Amoxicillin, Concanavalin-A, Helicobacter pylori, Microspheres.

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