Development and evaluation of crystalline inclusion complex of finasteride using electrospraying as a novel approach

Abstract

Solid form of drug plays the central role in optimizing its physicochemical properties, thus discovery of new solid forms always provides more options to achieve the desirable pharmaceutical profiles of drugs. Recently, certain drugs have been found to form crystalline inclusion complexes (ICs) with multiple types of linear polymers, representing a new sub-category of pharmaceutical solids. In this study, Finasteride (FNS) was used as the model host and poly (ethylene glycol) (PEG) as the guest, to form ICs of drug with the purpose of offering solubility advantage. Electrospraying as a novel approach was used for production of micro-particles of crystalline ICs of FNS, as it gave narrow particle size distribution and dry powder as end product. The obtained dry powder was characterized using powder X-ray diffraction, NMR spectroscopy and other characterization methods. The results revealed that FNS formed ICs with the biodegradable hydrophilic polymer (PEG), thus offering a FNS-PEG ICs as a potential new solid form. Compared with pure FNS crystals the FNS-PEG ICs crystals showed significantly higher solubility and faster dissolution rates; making it more suitable to achieve higher drug release profiles. Results demonstrated the possibility of using drug-polymer ICs microparticles as solid forms, providing a new approach to design formulations with enhanced drug release. In a nutshell developed formulation was found to be suitable for enhancing water solubility of poorly soluble actives.