Abstract
Purpose: To develop modified release microcapsules of flurbiprofen for sustained release and reduced gastrointestinal side effects.Method: A co-polymer containing Eudragit RS 100 and hydroxypropyl methylcellulose (HPMC) in different drug/co-polymer ratios was used for microencapsulation of flurbiprofen by modified emulsion solvent evaporation (MESE) technique. The microcapsules were evaluated by x-ray diffraction (XRD), differential scanning calorimetry (DSC), Fourier transform infra-red spectroscopy (FTIR) and scanning electron microscopy (SEM). Dissolution study was conducted in 0.1 M HCl for 2 h and phosphate buffer (pH 7.4) for 8 h, and the resulting data were analyzed by various pharmacokinetic models.Results: The data obtained from pre-formulation confirmed the purity of flurbiprofen. Particle size, flow rate and angle of repose showed good flow properties. FTIR and DSC confirmed the absence of incompatibilities among the drug and polymers. XRD of flurbiprofen showed characteristic sharp peaks confirming the crystalline nature of the drug which, however, decreased slightly in the formulation. SEM revealed that microencapsules of spherical shape and rough surface were produced at lower drug to copolymer ratio in contrast to the higher ratio which produced irregular microcapsules. Encapsulation efficiency was 65 - 85 % while regression coefficient (R2) values from kinetic analysis showed thatrelease followed Korsmeyer-Peppas model with “n” > 1 indicating release mechanism followed super case II transport.Conclusion: MESE technique using Eudragit RS 100/HPMC polymer blend is a suitable approach to development of modified release flurbiprofen microcapsules.Keywords: Microcapsules, Eudragit RS-100, Hydroxypropyl methylcellulose, Emulsion solvent evaporation, Flurbiprofen, Sustained drug release
Highlights
A well designed modified drug delivery system can overcome many of the problems of conventional dosage forms and enhance the therapeutic efficacy of the administered drug [1]
Eudragit RS 100 is a polymethacrylate, with a chemical names such as poly, having low amount of quaternary ammonium attached which gives pHindependent permeability and renders the film form by RS 100 less permeable to water [3]. It is a versatile polymer with a wide range of applications in development of transdermal delivery system, modified release dosage forms, ocular formulations, oral delivery system and Nano particles formulation [4]
The in vitro release of flurbiprofen was determined using USP dissolution apparatus type I with basket assembly
Summary
A well designed modified drug delivery system can overcome many of the problems of conventional dosage forms and enhance the therapeutic efficacy of the administered drug [1]. Eudragit RS 100 is a polymethacrylate, with a chemical names such as poly (ethyl acrylate, methyl methacrylate, trimethylammonioethyl methacrylate chloride), having low amount of quaternary ammonium attached which gives pHindependent permeability and renders the film form by RS 100 less permeable to water [3] It is a versatile polymer with a wide range of applications in development of transdermal delivery system, modified release dosage forms, ocular formulations, oral delivery system and Nano particles formulation [4]. For this purpose the weighed amount of polymer was dissolved in 25 ml acetone; by stirring the mixture at 600 rpm for 15 min, using magnetic stirrer. The analysis was performed at nitrogen flow of 40 ml/min and scanning was done at the heating rate of 10 oC/min from 25 oC
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