Desenvolvimento da forma farmacÃutica injetÃvel a partir da β-lapachona e ensaios preliminares in vivo

AUTOR(ES)

Youssef Conrado Haun

DATA DE PUBLICAÇÃO

2006

RESUMO

The β-lapachone (C15H14O3, MM 242,3), chemically named as 3,4-dihydro-2,2-dimethyl-2H-naphtol[1,2-b]pyran-5,6-dione, is a natural o-naphtoquinone derived from the lapacho tree (Tabebuia avellandae Lor), from the Bigoneaceae family. β-lapachone has been objective of many researches, many of them aiming to explore its elevated antineoplasic potential. Acting against many types of human cancers, specially the ones of very slow cellular cycle, as the case of some prostate lineages resistant to the conventional treatments, itâs believed that its action is by some sort of peculiar apoptosis mechanism. The main barrier on the development of an acceptable pharmaceutical form has been its poor aqueous solubility, what possibly leads to an equally poor bioavailability. This work intended to execute solubility studies with β-lapachone in different pharmaceutical solvents, and promote its complexation with cyclodextrins intending to reach a series of formulations that could be used in pre-clinical assays. Although the complexation process had been very long, the use of cyclodextrins shown itself as an viable pharmacotechnical option, because once the aqueous solubility problem is solved, there is a possible improvement of β-lapachone bioavailability. The formulations achieved were quantified by high performance liquid chromatography (HPLC), using a pre-validated methodology, and two of them were elected to be used in the in vivo assays: β-lapachone cyclodextrin complexes in aqueous solution and free β-lapachone in super refined sesame oil, administered orally and by intramuscular injection. The results had shown that the pharmacological answer to complexed β-lapachone is very meaningful; however, the formulations still need to be optimized

ASSUNTO(S)

cyclodextrins -lapachona injetÃvel solubility β intramuscular injection solubilidade complexaÃÃo in vivo assays farmacia complexation -lapachone ciclodextrina β estudos in vivo

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