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The Thai Journal of Pharmaceutical Sciences

Abstract

Objectives: Methotrexate (MTX) is a biopharmaceutics classification system Class IV drug having potential cytotoxic action against cancer cells. However, short half-life and poor bioavailability have limited its application. The object of this work was to entrap MTX and an herbal bioenhancer in a nanoparticle system to improve its bioavailability. Methods: We prepared the nanoparticles (NPs) by emulsion solvent evaporation method with Eudragit RLPO (ERLPO) polymer. Results: The result revealed good in vitro properties with 110 to 228 nm particle size range. The percentage of drugs released from all the batches in 72 h was within the range of 82.71 to 95.47%. The release kinetics data were best fitted to Higuchi’s model and was following Fick’s law of diffusion. Surprisingly, a formulation with higher bioenhancer loading (NPF 6) showed a higher antiproliferative effect on A549 cells. Conclusion: From this result, it can be predicted that the incorporation of the drug into ERLPO NPs helped to sustain the release profile of the formulations which may further reduce the dosage frequency of the MTX. Finally, it can be concluded that the addition of bioenhancer with antitumor drug can enhance its proliferative effect.

Publisher

Faculty of Pharmaceutical Sciences, Chulalongkorn University

First Page

406

Last Page

412

Included in

Pharmacology Commons

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