Effects on Walker 256 tumour of carmustine associated with a cholesterol-rich microemulsion (LDE)

The Journal of Pharmacy and Pharmacology
Raquel S TeixeiraR C Maranhão

Abstract

A cholesterol-rich microemulsion that binds to low-density lipoprotein (LDL) receptors (LDE), after injection into the bloodstream, concentrates in neoplastic tissues that over-express those receptors. LDE can thus serve as a vehicle for drug targeting. It was shown that carmustine side effects are pronouncedly reduced when the drug is associated with LDE in cancer patients. In this study, the therapeutic action of LDE associated with carmustine was compared with that of the non-associated drug in rats implanted with Walker 256 tumour. The toxicity and anti-tumour activity in rats treated with either free carmustine or carmustine associated with LDE and in control rats treated with saline solution were determined after a single intraperitoneal injection. The LD90 (90% lethal dose) of LDE-carmustine was 77 mg kg(-1) and of free carmustine was 44 mg kg(-1), indicating that LDE decreases toxicity. LDE-carmustine was able to decrease tumour mass at a lower dose level than free carmustine. Tumour regression time was shorter in LDE-carmustine- than in free carmustine-treated animals. Therefore, this study shows that the association of carmustine with LDE increases the therapeutic index of carmustine.

References

Mar 1, 1982·Annals of Internal Medicine·H GinsbergW V Brown
Feb 5, 1999·Biochimica Et Biophysica Acta·R D HirataR C Maranhão
Jun 28, 2001·Gynecologic Oncology·A AdesR C Maranhão
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Citations

May 10, 2012·Brazilian Journal of Medical and Biological Research = Revista Brasileira De Pesquisas Médicas E Biológicas·L A PiresR C Maranhão
Nov 11, 2011·International Journal of Nanomedicine·Elaine R TavaresRaul C Maranhão
Feb 5, 2013·International Journal of Nanomedicine·Ye JinWeiyu Zhang
Jun 1, 2006·The Journal of Pharmacy and Pharmacology·Ana C Lo PreteRaul C Maranhão
Sep 16, 2016·Cardiovascular Drugs and Therapy·Elaine N DaminelliRaul C Maranhão
Jan 1, 2012·Pharmaceutics·Marcelo L OcchiuttoVital P Costa
Mar 8, 2018·Brazilian Journal of Medical and Biological Research = Revista Brasileira De Pesquisas Médicas E Biológicas·S C M P FreitasR C Maranhão
Apr 8, 2006·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Fei XiongJiabi Zhu

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