Untitled

Abstract

ABSTRACT:The objective of the present investigation is to study the possibilities to improve the aqueous solubility and dissolution rate of Tamoxifen citrate (TC) -an oral anticancer drug, based on inclusion complexes with -cyclodextrin (α -CD). The inclusion processes are discussed based on absorption, emission, FT-IR, 1 H-NMR, SEM and phase solubility study. The α -CD study shows that the drug form 1:1 inclusion complexes. The solubility and dissolution results revealed that there was a considerable increase in solubility and dissolution of all inclusion complexes. Scanning Electron Microscopy (SEM) to analyze physicochemical interaction between drug and carrier and evaluation of the crystal morphology and their approximate size. The inclusion complex appears as tiny aggrigates of amorphous pieces of irregular sizes. In both absorption and emission the intensity increase with increase in concentration of α -CD. The aromatic ring is encapsulated in the non-popular α -CD cavity. The formation constant value reveals a hydrogen bonding interaction is present between the drug and α -CD cavity. The presence of aliphatic chains has not significantly changed the absorption and emission spectral behaviour and inclusion process. INTRODUCTION:Tamoxifen Citrate is an antagonist of the estrogen receptor in breast tissue via its active metabolite. In other tissues such as the endometrium, it characterized as a mixed agonist/ antagonist. Tamoxifen citrate is the usual endocrine (anti-estrogen) therapy for hormone receptor positive breast cancer in pre-menopausal women and is also a standard in post-menopausal women although aromators, inhibitors are also frequently used in that setting.