Anticancer research · 2009
Role of the pharmaceutical excipients in the tamoxifen activity on MCF-7 and vero cell cultures.
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Rossi Tiziana, Iannuccelli Valentina, Coppi Gilberto, Bruni Elisa, Baggio Giosué
Аннотация
BACKGROUND: Microparticles are used for controlled drug delivery. With the aim of improving both bioavailability and tamoxifen selective toxicity, the activity of tamoxifen embedded in calcium alginate/chitosan microparticles was studied.
MATERIALS AND METHODS: Tamoxifen alone and embedded in microparticles prepared with sodium alginate from Kelco (62% mannuronic acid and 38% guluronic acid) and from Fluka (30% mannuronic acid and 70% guluronic acid) was added to MCF-7 and Vero cultures and evaluated for antiproliferative activity by the MTT test.
RESULTS: The use of Kelco or Fluka alginate resulted in different LD(50) values on Vero and MCF-7 cultures, showing a higher cytotoxicity toward Vero cells treated with tamoxifen embedded in Kelco microparticles (25 microM vs. 48 microM on MCF-7 cells) but a selective toxicity with Fluka microparticles (25 microM and 10 microM on Vero and MCF-7 cells respectively).
CONCLUSION: Microparticle formulation may improve selective toxicity according to the alginate employed: differences in the chemical alginate composition can dramatically change both drug activity and toxicity.
MATERIALS AND METHODS: Tamoxifen alone and embedded in microparticles prepared with sodium alginate from Kelco (62% mannuronic acid and 38% guluronic acid) and from Fluka (30% mannuronic acid and 70% guluronic acid) was added to MCF-7 and Vero cultures and evaluated for antiproliferative activity by the MTT test.
RESULTS: The use of Kelco or Fluka alginate resulted in different LD(50) values on Vero and MCF-7 cultures, showing a higher cytotoxicity toward Vero cells treated with tamoxifen embedded in Kelco microparticles (25 microM vs. 48 microM on MCF-7 cells) but a selective toxicity with Fluka microparticles (25 microM and 10 microM on Vero and MCF-7 cells respectively).
CONCLUSION: Microparticle formulation may improve selective toxicity according to the alginate employed: differences in the chemical alginate composition can dramatically change both drug activity and toxicity.