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Floating Controlled Drug Delivery System of Famotidine Loaded Hollow Microspheres (Microballoons) in the Stomach

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Most of the floating systems have an inherent drawback of high variability in the GI transit time, invariably affecting the bioavailability of drug. An attempt has been made to develop floating drug delivery system for improving the drug bioavailability by prolongation of gastric residence time of famotidine in stomach. The floating microballoons were prepared using polymer Eudragit L-100 by solvent evaporation and diffusion technique. The prepared famotidine loaded microspheres were characterised for drug loading, entrapment, encapsulation efficiency, particle size distribution, surface morphology, differential scanning calorimetry, test for buoyancy, in-vitro release and in-vivo antiulcer studies. The results showed an increased drug loading, encapsulation and entrapment efficiency. The thermogram of the DSC showed that the drug was encapsulated in amorphous form and SEM studies revealed the discrete, spherical shaped spheres with rough surface and presence of holes on floating microspheres due high entrapment of PEG which are responsible for drug release and floating ability. The sizes of spheres were found between 20-120 μm which exhibited prolonged release (Invitro > 8 h) and remained buoyant for > 10 h. The mean particle size increased and the drug release rate decreased at higher Eudragit L-100 polymer concentration. The in-vivo results showed significant antiulcer property of famotidine loaded microspheres when compared to control and standard group of rats by using pyloric ligation method. The mean volume of gastric secretion, mean pH and mean total acid for formulation treated group was calculated as 3.45+0.88 ml, 5.65+ 0.74, and 114.15+1.80 mEq/L respectively.

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Keywords: Floating controlled drug delivery system; buoyancy; eudragit L-100; famotidine; hollow microspheres (microballoons)

Document Type: Research Article

Publication date: 01 January 2010

More about this publication?
  • The aim of Current Drug Delivery is to publish peer-reviewed articles, short communications, short and in-depth reviews in the rapidly developing field of drug delivery. Modern drug research aims to build in delivery properties of a drug at the design phase, however in many cases this ideal cannot be met and the development of delivery systems becomes as important as the development as the drugs themselves.

    The journal aims to cover the latest outstanding developments in drug and vaccine delivery employing physical, physico-chemical and chemical methods. The drugs include a wide range of bioactive compounds from simple pharmaceuticals to peptides, proteins, nucleotides, nucleosides and sugars. The journal will also report progress in the fields of transport routes and mechanisms including efflux proteins and multi-drug resistance.

    The journal is essential for all pharmaceutical scientists involved in drug design, development and delivery.
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