Objective <p>The purpose of the current novel study is to develop dual-coated multi-particulates with a combination of time-dependent inner and pH-dependent outer coating layers to control the release of the entrapped drug from the ascending colon onwards. </p> Methods <p>Ibuprofen-loaded pellets prepared via powder layering technology were coated initially with time-dependent hydroxypropyl cellulose and ethyl cellulose-based inner polymeric layers and afterwards with the Eudragit L100 and Eudragit S100-based outer pH-dependent coating layers and evaluated. </p> Results <p>The best double-coated batch showed nominal <i>in vitro</i> release of 6.163 ± 0.23% in simulated upper GI conditions, with surface morphology collaborating with kinetics data. <i>In-vivo</i> animal X-Ray Roentgenography and plasma analysis studies revealed intact multi-particulates arriving inside the colon with maximum plasma concentration of 5.97 ± 0.41&#xa0;μg/ml (C<sub>max</sub>), retarded till 12th hr (T<sub>max</sub>). </p> Conclusion <p>Results suggest that these dual-coated multi-particulates can be more efficient for colon-specific targeting of various potent drugs.</p>

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A Novel Inner Time and Outer pH-Dependent Dual Coated Multi-Particulate Approach for Colon Specific Delivery of Ibuprofen Beyond Ileocecal Segment in Reduced Colonic Bacterial Diversity

  • Debaprasad Ghosh,
  • Nikhil Kumar Singh,
  • Ashu Mittal,
  • Deepti Katiyar,
  • Sanjeev Kumar,
  • Vinay Kumar

摘要

Objective

The purpose of the current novel study is to develop dual-coated multi-particulates with a combination of time-dependent inner and pH-dependent outer coating layers to control the release of the entrapped drug from the ascending colon onwards.

Methods

Ibuprofen-loaded pellets prepared via powder layering technology were coated initially with time-dependent hydroxypropyl cellulose and ethyl cellulose-based inner polymeric layers and afterwards with the Eudragit L100 and Eudragit S100-based outer pH-dependent coating layers and evaluated.

Results

The best double-coated batch showed nominal in vitro release of 6.163 ± 0.23% in simulated upper GI conditions, with surface morphology collaborating with kinetics data. In-vivo animal X-Ray Roentgenography and plasma analysis studies revealed intact multi-particulates arriving inside the colon with maximum plasma concentration of 5.97 ± 0.41 μg/ml (Cmax), retarded till 12th hr (Tmax).

Conclusion

Results suggest that these dual-coated multi-particulates can be more efficient for colon-specific targeting of various potent drugs.