Zinc-leuprolide complex: preparation, physicochemical characterization and release behaviour from in situ forming implant.
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.
Astaneh
Reyhaneh
R
Department of Pharmaceutics, School of Pharmacy, Shaheed Beheshti University of Medical Sciences, P.O. Box 14155-6153, Tehran, Iran. rastaneh@yahoo.com
Nafissi-Varcheh
Nastaran
N
Erfan
Mohammad
M
D002152:Calorimetry, Differential Scanning; D004343:Drug Implants / Q000378:metabolism*; D016729:Leuprolide / Q000737:chemistry* / Q000378:metabolism*; D008567:Membranes, Artificial; D017550:Spectroscopy, Fourier Transform Infrared; D014961:X-Ray Diffraction; D015032:Zinc
D004343:Drug Implants; D008567:Membranes, Artificial; D016729:Leuprolide; D015032:Zinc