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Pentoxifylline Loaded Floating Microballoons: Design, Development and Characterization

DOI: 10.1155/2013/107291

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Abstract:

The floating microballoons have been utilized to obtain prolonged and uniform release in the stomach. The objective of the present study involves design, development, and characterization of pentoxifylline loaded floating microballoons to prolong their gastric residence time. Pentoxifylline (trisubstituted xanthine derivative) loaded microballoons were prepared by the solvent evaporation technique using different concentrations of polymers like HPMC K4M and ethyl cellulose (EC) in ethyl alcohol and dichloromethane organic solvent system. Microballoons were characterized for their particle size, surface morphology, production yield, loading efficiency, buoyancy percentage, and in vitro drug release studies. From the characterization it was observed that increases in amount of polymers (HPMC K4M and EC) led to increased particle size, loading efficiency, and buoyancy percentage, and retarded drug release. The particle size, particle yield, loading efficiency, buoyancy percentage and in vitro drug release for optimized formulation (F3) were found to be ?μm, %, %, %, and %, respectively. The data was fitted to different kinetic models to illustrate its anomalous (non-Fickian) diffusion. The in vitro result showed that formulations comprised of varying concentrations of ethyl cellulose in higher proportion exhibited much retarded drug release as compared to formulations comprised of higher proportion of varying concentrations of HPMC K4M. 1. Introduction Oral drug delivery systems are essential to optimize both the residence time of the system within the gastrointestinal tract and the release rate of the drug from the system. Various attempts have been made to prolong the residence time of the dosage forms within the stomach [1]. Rapid gastrointestinal transit could result in incomplete drug release from the drug delivery system to absorption window leading to diminished efficacy of the administered dose. Prolonged gastric retention is important in achieving control over the gastric residence time because it helps to maintain the controlled release system in the stomach for a longer time in an expected manner [2]. Floating systems (hydrodynamically controlled systems) are low-density systems which means they are less dense than gastric fluid. These systems have sufficient buoyancy to float over the gastric contents and remain buoyant in the stomach for a prolonged period of time without disturbing the gastric emptying rate. While the formulation is floating on the gastric contents, drug is released slowly from it at a desired rate [3, 4]. For oral sustained

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