Montmorillonite/poly-(-caprolactone) composites as versatile layered material: Reservoirs for anticancer drug and controlled release property

Bhavesh D. Kevadiya, Rahul P. Thumbar, Mahendrapalsingh M. Rajput, Shalini Rajkumar, Harshad Brambhatt, Ghanshyam V. Joshi, Ganga P. Dangi, Haresh M. Mody, Pankaj K. Gadhia, Hari C. Bajaj

Research output: Contribution to journalArticle

36 Scopus citations

Abstract

This work evaluates intercalation of tamoxifen (Tmx) in interlayer gallery of Na +-MMT (Montmorillonite, MMT) (Tmx-MMT), which is further compounded with poly-(-caprolactone) (PCL) (Tmx-MMT/PCL, MPs), for oral chemotherapy of breast cancer. The X-ray diffraction patterns, thermal and spectroscopic analyses indicated the intercalation of Tmx into the MMT interlayer that stabilized in the longitudinal monolayer mode by electrostatic interaction. No significant change in structural and functional properties of Tmx was found in the MMT layers. In vitro study of drug release profiles showed controlled release pattern. The genotoxic effect of drug was in vitro evaluated in human lymphocyte cell culture by comet assay, and results indicated moderate reduction in DNA damage when pristine Tmx was intercalated with MMT and formulated in composites. The Tmx-MMT hybrid efficacy was also confirmed on HeLa and A549 cancer cells by in vitro cell viability assay. In vivo pharmacokinetics (PK) of formulated Tmx in rats was examined and the results showed that plasma Tmx levels were within therapeutic window as compared to pristine Tmx. Therefore, Tmx-MMT hybrid and microcomposite particles (MPs) can be of considerable value in chemotherapy of malignant neoplastic disease with reduced side effects. This study clearly indicated that MMT not only plays a role as a delivery matrix for drug, but also facilitates significant increase in the delivery proficiency.

Original languageEnglish (US)
Pages (from-to)265-272
Number of pages8
JournalEuropean Journal of Pharmaceutical Sciences
Volume47
Issue number1
DOIs
StatePublished - Aug 30 2012

Keywords

  • Cell-viability
  • Genotoxicity
  • Montmorillonite
  • Pharmacokinetics
  • Tamoxifen

ASJC Scopus subject areas

  • Pharmaceutical Science

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    Kevadiya, B. D., Thumbar, R. P., Rajput, M. M., Rajkumar, S., Brambhatt, H., Joshi, G. V., Dangi, G. P., Mody, H. M., Gadhia, P. K., & Bajaj, H. C. (2012). Montmorillonite/poly-(-caprolactone) composites as versatile layered material: Reservoirs for anticancer drug and controlled release property. European Journal of Pharmaceutical Sciences, 47(1), 265-272. https://doi.org/10.1016/j.ejps.2012.04.009