Long term multiple sclerosis drug delivery using dendritic polyglycerol flower-like microspheres.
J Biomater Sci Polym Ed. 2019 Oct 14;:1-13
Authors: Veloso da Silva P, Alencar de Queiroz AA
The purpose of this study was to produce and characterize the dendritic polyglycerol microspheres (DPGlyM) carrier with potential for use in treatment of multiple sclerosis (MS). This novel drug delivery system is comprised of DPGlyM as carrier for dimethyl fumarate (DMF) and curcumin (CUR). Molecular docking (MD) was used as in-silico tool to guide the drug entrapment and indicates a spontaneous interactions of DPGlyM with DMF (ΔGo= -11.3 kJ.mol-1) and CUR (ΔGo= -23.8 kJ.mol-1). The DPGlyM morphology and size distribution was determined using a scanning electron microscopy (SEM). The average size of the microspheres was 30-40 μm. The highest encapsulation efficiency and loading efficiency for CUR and DMF were 94.1% and 65.3%, respectively. The zeta potential indicates that CUR and DMF loaded DPGlyM form stable suspension in phosphate buffer solution (PBS) at pH 7.4. Cytotoxicity and hemocompatibility studies suggests that CUR and DMF loaded DPGlyM not influence cell viability and are well tolerated in hemolysis assays without any damaging effects even at high concentrations up to 50 mg/mL. The in-vitro release of DMF and CUR in phosphate buffer of pH 7.4 followed a kinetics type super case II transport. The activation energy for CUR and DMF release from DPGlyM was found to be 56.95 kJ/mol and 13.87 kJ/mol for CUR and DMF, respectively. The in-vitro release assays show that the DPGlyM have good sustained release of CUR and DMF for 5 days. CUR and DMF loaded DPGlyM has shown promising results for a sustained release during enhanced time duration.
PMID: 31609679 [PubMed – as supplied by publisher]