Quality by Design Based Fabrication of Iron Oxide Induced Mucoadhesive Microspheres for Enhanced Bioavalibility of Cinnarizine

Author(s): Inderbir Singh, Sunil Kamboj, Vikas Rana*.

Journal Name: Current Drug Delivery

Volume 14 , Issue 8 , 2017

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Graphical Abstract:


Background: The study was aimed to enhance the mucoadhesive potential of Eudragit RS 100 and RL 100 using iron oxide.

Methods: Microspheres of Eudragit RS/RL100, containing cinnarizine, were prepared by emulsification solvent evaporation technique employing 32 full factorial design. Eudragit RS or RL (X1) and iron oxide (X2) concentrations were the independent variables. Particle size, entrapment efficiency, mucoadhesion, zeta potential and t90% were the response variables. Microspheres when characterized by FTIR-ATR and DSC confirm entrapment of drug.

Results: SEM analysis of microspheres exhibits roughness/micropores responsible for drug release. Particle size of Eudragit RS and Eudragit RL microspheres was found to increase from 275.60±2.68 to 438.72±22.73 nm and 283.14±1.95 to 475.55±29.66 nm. Incorporation of iron oxide increases zeta potential from 0.88±0.18 to 10.74±1.78 mV and 1.12±0.11 to 14.44±2.44 mV for Eudragit RS and RL microspheres, respectively. Highest mucoadhesion and zeta potential were obtained when 4.5% w/v of X1 and 20% w/v of X2 were used in the formulation of microspheres.

Conclusion: The r2 values were significantly higher (P < 0.01) for the Langmuir equation as compared to Freundlich equation, indicating the involvement of electrostatic forces in the specific adsorption of mucin on to Eudragit microspheres. In vivo study indicates 2.5 to 3 times increased bioavailabity of cinnarizine through mucoadhesive microspheres.

Keywords: Cinnarizine, Eudragit RS, Eudragit RL, 32 full factorial design, mucoadhesive microspheres, zeta potential.

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Article Details

Year: 2017
Page: [1154 - 1169]
Pages: 16
DOI: 10.2174/1567201813666161018152836
Price: $58

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