Abstract
Purpose: The goal of this study was to improve the solubility and dissolution behavior of Raloxifene Hydrochloride (RH) using Spray Freeze Drying (SFD) technique.Methods: For achieving this goal, series of samples containing RH with polyvinylpyrrolidone (PVP) or hydroxypropyl beta cyclodextrin (HPβCD) used as solubility enhancers were prepared and microparticles were formed via SFD. The resultant microparticles were physicochemically characterized. Morphology of the microparticles were observed using Scanning Electron Microscopy (SEM). High Performance Liquid Chromatography (HPLC) was used for analyzing the solubility and dissolution profile of the samples.Results: Fourier Transmission Infrared (FTIR) spectra showed that SFD processed compositions did not affect chemical structure of RH. SEM and Thermal Gravimetric Analysis (TGA) revealed that the fabricated spherical and highly porous microparticles were in amorphous state. SFD processed powders showed superior solubility and dissolution behavior; where, 80% of the drug was dissolved within 5 minutes.Conclusion: SFD method can be a promising alternative for enhancing the solubility of poorly water soluble compounds.
Highlights
Raloxifene Hydrochloride (RH) is a Selective Estrogen Receptor Modulator (SERM) acts as an agonist on bone and liver
In order to increase the solubility of RH, different methods have been investigated to date
The effect of Spray freeze drying (SFD) method on dissolution rate of RH was studied in the presence of PVP and HPβCD as solubility enhancers
Summary
Raloxifene Hydrochloride (RH) is a Selective Estrogen Receptor Modulator (SERM) acts as an agonist on bone and liver. Raloxifene has been approved for the prevention of osteoporosis as well as reducing the risk of invasive breast cancer in postmenopausal women.[1] RH shows very low oral bioavailability (c.a. 2% of the given dose) which is mostly due to its extensive first pass hepatic metabolism via glucuronide conjugation as well as incomplete dissolution as the drug is poorly water-soluble.[2,3] This drug is categorized as class II of Biopharmaceutical Classification System (BCS).[4] its low bioavailability seems to be enhanced by increasing its solubility.[5,6] Several techniques can be used to improve solubility of drugs such as co-grinding, salt formation, spray drying, and supercritical fluid processing.[7,8,9,10] In order to increase the solubility of RH, different methods have been investigated to date. In comparison to other particle engineering processes, SFD grants better control on different aspects of particle properties This method can produce highly porous and low density particles. PVP has been widely used for solubility improvement of waterinsoluble drugs such as piroxicam, furosemide, praziquantel, and celecoxib.[17,18,19,20] Cyclodextrin (CD) derivatives are cyclic oligosaccharides comprise
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
