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Design and Evaluation of Floating Micro-Carriers for Effective Delivery of a Hydrophobic Drug.

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PURPOSE Gastro-retentive drug delivery systems plays a significant role in delivery of drugs with narrow absorption window by following plethora of versatile approaches such as high-density system, muco-adhesive system, low… Click to show full abstract

PURPOSE Gastro-retentive drug delivery systems plays a significant role in delivery of drugs with narrow absorption window by following plethora of versatile approaches such as high-density system, muco-adhesive system, low density system, super-porous hydrogels, and floating systems to enhance the bioavailability in upper part of stomach. The recent research work was focused on floating system in which different combination of polymers and lipids were used to synthesize the floating microparticles that remain buoyant over the gastric fluid for 24 hrs. METHODS Solvent diffusion evaporation method was adopted by using various polymers such as ethyl cellulose, stearyl alcohol, gelucire 43/01, Eudragit E100 and tween 80 as surfactant. Eudragit E100 was used in different concentrations to modulate the release pattern. Furosemide was selected as a model drug due to has narrow absorption window in GIT. Furthermore, characterization was carried out by analysis the percent recovery of microparticles, furosemide loading, in-vitro release studies, SEM, DSC, XRD, FTIR, particles size analysis, optical microscopy. RESULTS Around 88% encapsulation efficiency of microparticles were obtained which was free flowing. Particle size of microparticles containing stearyl alcohol was from 363.3±120 to 400±204.41 µm and containing gelucire 43/01 was from 216±106 to 296.7±106 µm. CONCLUSION Controlled drug release was accomplished by the addition of hydrophilic polymer Eudragit E100 which forms the pores on the surface of microparticles. In addition, pores on the surface of microparticles due to Eudragit E100 were assessed by SEM. DSC, XRD and FTIR confirmed the absence of drug polymer interaction and amorphous form of drug after encapsulation. Drug release kinetics was determined by applying the different models such zero-order model, first order model, higuchi and korsemeyer-pappas model. All formulations followed the korsemeyer-peppas model at 1.2 pH. FUTURE PROSPECTS In vivo study will be performed in future to accomplish better results regarding bioavailability of drug loaded microparticles.

Keywords: eudragit e100; system; release; model; drug; delivery

Journal Title: Current drug delivery
Year Published: 2022

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