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Zinc–leuprolide complex: preparation, physicochemical characterization and release behaviour from in situ forming implant
Author(s) -
Astaneh Reyhaneh,
NafissiVarcheh Nastaran,
Erfan Mohammad
Publication year - 2007
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.894
Subject(s) - fourier transform infrared spectroscopy , differential scanning calorimetry , chemistry , zinc , nuclear chemistry , controlled release , materials science , chemical engineering , organic chemistry , nanotechnology , physics , engineering , thermodynamics
Leuprolide acetate (LA) has been accepted as treatment for prostatic cancer and is currently also being evaluated in phase II clinical trials for the treatment of Alzheimer's disease. In this study, the zinc complex of leuprolide was prepared and its structure determined by Fourier‐transform infrared (FTIR), differential scanning calorimetry (DSC), UV, X‐ray diffraction (XRD), atomic absorption spectroscopy, elemental analysis, and compared with these parameters for leuorolide acetate. Also, the in vitro release profile of leuprolide and its complex form in situ forming implant (ISFI) in comparison to a commercial formulation (Eligard) was investigated. These studies indicate that the zinc complex can be effectively synthesized and influenced on tri‐phasic pattern after burst release of LA from the ISFI and shifts this trend to a continuous release profile. Non‐linear regression test confirmed this transformation as a zero‐order release profile as well. Copyright © 2007 European Peptide Society and John Wiley & Sons, Ltd.