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A Novel Three-Dimensional Large-Pore Mesoporous Carbon Matrix as a Potential Nanovehicle for the Fast Release of the Poorly Water-soluble Drug, Celecoxib

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Abstract

Purpose

A novel mesocellular carbon foam (MSU-FC) with a large pore size and a three-dimensional porous structure for the oral delivery of poorly water-soluble drugs was prepared. The goal of this study was to improve in vitro dissolution and in vivo absorption of celecoxib (CEB), a model drug, by means of novel carbon-based nanoparticles prepared from the MSU-FC matrix.

Methods

The MSU-FC matrix was synthesized by an inverse replica templating method using mesocellular silica template. A solvent immersion/evaporation method was used to load the drug molecules. The drug-loaded nanoparticles were characterized for morphology, surface area, particle size, mesoporous structure, crystallinity, solubility and dissolution. The effect of MSU-FC on cell viability was measured using the MTT conversion assay. Furthermore, the oral bioavailability of CEB-loaded MSU-FC in fasted rats was compared with that of the marketed product.

Results

Our results demonstrate that CEB incorporation into the prepared MSU-FC resulted in an approximately 9-fold increase in aqueous solubility in comparison with crystalline CEB. MSU-FC produced accelerated immediate release of CEB in comparison with crystalline CEB (pure CEB powder or marketed formulation) and the drug-loaded conventional mesoporous carbon particles. The relative bioavailability of CEB for CEB-loaded MSU-FC was 172%. In addition, MSU-FC nanoparticles exhibited very low toxicity.

Conclusions

The MSU-FC nanomatrix has been shown to be a promising drug delivery vehicle for improving the dissolution and biopharmaceutical characteristics of poorly water-soluble drugs.

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Acknowledgments and disclosures

This work was generously supported by the National Basic Research Program of China (973 Program) (No.2009CB930300). Dr. David B. Jack is gratefully thanked for correcting English of the manuscript.

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Authors and Affiliations

  1. Department of Pharmaceutics,, Xuzhou Medical College, P.O. Box 62, No. 209, Tongshan Road, Xuzhou, 221004, China

    Yanzhuo Zhang & Yu Wang

  2. Department of Pharmaceutics, School of Pharmacy, Shenyang Pharmaceutical University, No. 103, Wenhua Road, Shenyang, 110016, China

    Hong Wang & Siling Wang

  3. Jiangsu Hengrui Medicine Co. Ltd., No. 11 Changjiang Road,, Lianyungang, 222047, China

    Chuanjun Li, Baoxiang Sun & Cunqiang Gao

Authors
  1. Yanzhuo Zhang
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  2. Hong Wang
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  5. Yu Wang
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  6. Siling Wang
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Correspondence to Yanzhuo Zhang.

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Zhang, Y., Wang, H., Li, C. et al. A Novel Three-Dimensional Large-Pore Mesoporous Carbon Matrix as a Potential Nanovehicle for the Fast Release of the Poorly Water-soluble Drug, Celecoxib. Pharm Res 31, 1059–1070 (2014). https://doi.org/10.1007/s11095-013-1227-9

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  • DOI: https://doi.org/10.1007/s11095-013-1227-9

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