Abstract
Eudragit E 100 and polycaprolactone (PCL) floating microspheres for enhanced gastric retention and drug release were successfully prepared by oil in water solvent evaporation method. Metronidazole benzoate, an anti-protozoal drug, was used as a model drug. Polyvinyl alcohol was used as an emulsifier. The prepared microspheres were observed for % recovery, % degree of hydration, % water uptake, % drug loading, % buoyancy and % drug release. The physico-chemical properties of the microspheres were studied by calculating encapsulation efficiency of microspheres and drug release kinetics. Drug release characteristics of microspheres were studied in simulated gastric fluid and simulated intestinal fluid i.e., at pH 1.2 and 7.4 respectively. Fourier transform infrared spectroscopy was used to reveal the chemical interaction between drug and polymers. Scanning electron microscopy was conducted to study the morphology of the synthesized microspheres.
Highlights
Drugs with short half are eliminated very abruptly after a brief time in the body they require multiple dosing [1,2]
In the present study, floating microspheres were prepared loaded with metronidazole benzoate (MZB) by using oil in water (o/w) solvent evaporation method
This method was selected because drug and both the polymers were soluble in dicholoromethane i.e., oil phase. 1% polyvinyl alcohol (PVA) solution was used as emulsifying agent
Summary
Drugs with short half are eliminated very abruptly after a brief time in the body they require multiple dosing [1,2]. Gastro-retentive drug delivery system which is known as FDDS is one of the most important techniques developed until now to retain the drug for a longer period of time in the stomach They increase the gastric retention time (GRT) without affecting the intrinsic rate of gastric emptying. Eudragit E 100 is pH dependent polymer, soluble in gastric fluid and swells at pH lower than 5.0 It has good adhesion, low viscosity and high pigment biding. Current work focus on the design of floating/hollow microspheres to increase the GRT and in turn sustained release of model drug i.e., metronidazole benzoate (MZB) in the stomach by using blend of E100 and PCL in the presence of polyvinyl alcohol (PVA) as an emulsifier.
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