Abstract
Raloxifene HCl is a drug with poor bioavailability and poor water solubility. Furthermore nο pharmaceutically acceptable organic solvent has been reported before to dilute the drug. It was observed that Raloxifene HCl can be diluted in a solvent mixture of acetone/water or ethanol/water. The aim of this study was to use biodegradable polymers in order to prepare Raloxifene HCl nanoparticles. For this purpose a series of novel biodegradable poly(ethylene succinate-co-propylene adipate) P(ESu-co-PAd) polyesters were synthesized following the polycondensation method and further, poly(ethylene succinate) (PESu) and poly(propylene adipate) (PPAd) were used. The prepared polyesters were characterized by intrinsic viscosity measurements, end group analysis, enzymatic hydrolysis, Nuclear Magnetic Resonance Spectroscopy (1Η-NMR and 13C-NMR) and Wide-angle X-ray Diffractometry (WAXD). The drug nanoparticles have been prepared by a variation of the co-precipitation method and were studied by Wide-angle X-ray Diffractometry (WAXD), FTIR spectrometry, light scattering size distribution, Scanning Electron Microscopy (SEM) and release behavior measurements. The interactions between the polymers and the drug seem to be limited, so the drug occurs in crystalline form in all nanoparticles. The size of the nanoparticles seems to be in the range of 150-350 nm, depending on the polymer that was used. The drug release depends on the melting point and degree of crystallinity of the polyesters used. An initial high release rate was recorded followed by very slow rates of controlled release.
Highlights
IntroductionDue to their favorable features of biodegradability and biocompatibility, constitute one of the most important classes of synthetic biodegradable polymers and are nowadays available commercially in a variety of types
Aliphatic polyesters, due to their favorable features of biodegradability and biocompatibility, constitute one of the most important classes of synthetic biodegradable polymers and are nowadays available commercially in a variety of types
The prepared P(ESu-co-PAd) copolyesters that were used as drug carriers in the present work were studied by 1H-Nuclear Magnetic Resonance (NMR), 13C-NMR, intrinsic viscosity measurements, Wide-angle X-ray Diffractometry (WAXD) and enzymatic hydrolysis
Summary
Due to their favorable features of biodegradability and biocompatibility, constitute one of the most important classes of synthetic biodegradable polymers and are nowadays available commercially in a variety of types. Some examples of aliphatic polyesters one may mention are polycaprolactone (PCL), poly(hydroxybutyrate) (PHB), poly(3-hydroxybutyrate-co-3-hydroxyvalerate) (Biopol®), poly(L-lactide), etc., [1,2,3,4]. Most of these polyesters have been studied for their biocompatibility, bioresorbability and their cytocompatibility as well [5, 6]. It was found that they are biocompatible materials with higher hydrolysability into human body and they can be used as drug carriers for controlled release devices and for biomedical applications. Targeting drug delivery systems have been studied widely in cancer therapeutic applications [7,8,9,10,11]. In the last years poly(alkylene dicarboxylates) such as poly(propylene succinate) (PPSu) and poly(propylene adipate)
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