Abstract
Background: Categorized as a Biopharmaceutics Classification System (BCS) Class II drugs, statin exhibit low aqueous solubility and bioavailability thus presenting an obstacle and great challenge to formulation researchers. This paper describes a de novo approach to enhance the aqueous solubility of one of the most commonly prescribed statins i.e., simvastatin (SMV) by forming a complex (SMV-ARG) with cosolute arginine (ARG).
Methods: The complex has been characterized for its apparent solubility and in vitro dissolution. The solid state characterization has been carried out using Fourier Transform Infra-Red (FTIR) Spectroscopy, Elemental Analysis, X-Ray Powder Diffraction (XRD), Differential Scanning Calorimetry (DSC) analysis, Thermal Gravimetric Analysis (TGA) and Scanning Electron Microscopy (SEM).
Results: Simvastatin-Arginine (SMV-ARG) complex exhibited massive solubility enhancement by 12,000 fold and significant improvement in both acidic and alkaline dissolution media. A conversion of coherent crystalline to non-coherent pattern, and certain extent of amorphization in SMV-ARG complex, fully justifies the enhanced solubility, and hence the dissolution profile.
Conclusion: The present study provides a significant evidence that ARG molecules are capable to form a complex with small molecules and increase their aqueous solubility which prove to be beneficial in drug formulation and development.
Keywords: Solubility, dissolution, solid state, X-Ray powder defractometric, arginine complexes, simvastatin.
Graphical Abstract
Related Books
Localized Micro/Nanocarriers for Programmed and On-Demand Controlled Drug Release
Mixed Polymeric Micelles for Osteosarcoma Therapy: Development and Characterization
A Comprehensive Text Book on Self-emulsifying Drug Delivery Systems
Nanomaterials: Evolution and Advancement towards Therapeutic Drug Delivery (Part II)
Nanomaterials: Evolution and Advancement Towards Therapeutic Drug Delivery (Part I)
29
2
1