Design, Synthesis and Characterization of a PEGylated Stanozolol for Potential Therapeutic Applications

Publication date: Available online 9 November 2019Source: International Journal of PharmaceuticsAuthor(s): Cristian Vergallo, Giulia Torrieri, Riccardo Provenzani, Sini Miettinen, Karina Moslova, Markku Varjosalo, Maria Chiara Cristiano, Massimo Fresta, Christian Celia, Hélder A. Santos, Felisa Cilurzo, Luisa Di MarzioAbstractStanozolol (STZ) is a drug used to treat serious disorders like aplastic anemia and hereditary angioedema. It is also indicated as an adjunct therapy for the treatment of vascular disorders and growth failures. Encouraging results obtained using animal models demonstrated that STZ increases bone formation and mineralization, thus improving both density and biomechanical properties. Like natural androgens, such as TST and 5α-dihydrotestosterone (5α-DHT), STZ binds androgen receptor (AR) to activate AR-mediated signalling. Despite its therapeutic effects, this synthetic anabolic-androgenic steroid (AAS), or 5α-DHT derivative, due to its high lipophilicity, is poor soluble in water. Thus, to increase the water solubility and stability of STZ, as well as its bioavailability and efficacy, an innovative PEGylated STZ (STZ conjugated with (MeO-PEG-NH2)10kDa, (MeO-PEG-NH)10kDa-STZ) was synthesized. As confirmed by chromatography (RP-HPLC) and spectrometry (ATR-FTIR, 1H-NMR, elemental CHNS(O) analysis, MALDI-TOF/TOF) analyses, a very pure, stable and soluble compound was obtained. Acetylcholinesterase (AChE) competitive ELISA kit demonstr...
Source: International Journal of Pharmaceutics - Category: Drugs & Pharmacology Source Type: research

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