Abstract
The objective of the current investigation is to reduce dosing frequency and improve patient compliance by designing and systematically evaluating sustained release microspheres of Glipizide. An anti-diabetic drug, Glipizide, is delivered through the microparticulate system using ethyl cellulose as the controlled release polymer. Microspheres were developed by the emulsion solvent diffusion-evaporation technique by using the modified ethanol,-dichloromethane co-solvent system. The polymer mixture of ethyl cellulose and Eudragit® S100 was used in different ratios (1:0, 1:1, 2:3, 1:4 and 0:1) to formulate batches F1 to F5. The resulting microspheres were evaluated for particle size, densities, flow properties, morphology, recovery yield, drug content, and in vitro drug release behavior. The formulated microspheres were discrete, spherical with relatively smooth surface, and with good flow properties. Among different formulations, the fabricated microspheres of batch F3 had shown the optimum percent drug encapsulation of microspheres and the sustained release of the Glipizide for about 12 h. Release pattern of Glipizide from microspheres of batch F3 followed Korsmeyers-peppas model and zero-order release kinetic model. The value of ‘n’ was found to be 0.960, which indicates that the drug release was followed by anomalous (non-fickian) diffusion. The data obtained thus suggest that a microparticulate system can be successfully designed for sustained delivery of Glipizide and to improve dosage form characteristics for easy formulation.
Highlights
The limitations of the most obvious and trusted drug delivery techniques, such as conventional drug delivery system (DDS), have been recognized for some time the most important limitation of them being the patient incompliance due to frequent medication
An accurately weighed quantity of Glipizide (50 mg) and enteric polymer Eudragit® S100 along with ethyl cellulose was codissolved at room temperature in a solvent mixture
This solution was introduced into 1000 ml of 0.4% Polyvinyl alcohol (PVA) aqueous solution at room temperature and dispersed to form emulsion at stirring rates of 200 rpm using a mechanical stirrer equipped with 4-blade propeller
Summary
The limitations of the most obvious and trusted drug delivery techniques, such as conventional drug delivery system (DDS), have been recognized for some time the most important limitation of them being the patient incompliance due to frequent medication. This limitation can be overcome by modifying existing DDS. SR dosage forms, based on multiparticulate systems have attracted much attention due to their several benefits in reducing risk of dose dumping, and local irritation as the individual units can pass randomly through the pylorus and distribute widely in the GI tract[4] producing more predictable drug release profiles
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