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DEVELOPMENT OF MESOPOROUS SILICATE NANOPARTICLES AS DRUG CARRIER FOR MAGNOLOL
Abstract
The goal of the present study is to evaluate the use of mesoporous silicate nanoparticles MCM-41 for the loading and release of the magnolol. MCM-41 has a hexagonal arrangement of mesopores, with diameters ranging from 2 to 10 nm. The homogeneity of the cylindrical pores, high surface area with uniform porosity, and good thermal stability, which make them an attractive molecular sieve for applications in sorption of large organic molecules, as well as host for quantum confinement of guest molecules. Also, the biocompatibility, in vivo biodegradability, and the possibility to has its surface modified by functionalization with various organic groups, thereby allowing drug loading and release control. Magnolol (MGN) is a small-molecule neolignan polyphenolic compound isolated from the genus Magnolia. The anti-inflammatory, anti-oxidative, anti-diabetic, antitumorgenic, anti-neurodegenerative, anti-depressant and anti-microbial properties of MGN are well documented in recent literature. The oral bioavailability of magnolol is reported to be only 5% due to extensive first-pass metabolism and low absorption. The study followed the evolution of in-vitro dissolution profile of magnolol from the silica matrix, kinetics of drug release. The products were characterized by X-ray diffraction (XRD), scanning electron microscopy (SEM) and nitrogen adsorption-desorption isotherms before and after drug nanoencapsulation. The hexagonal ordering is very well preserved after encapsulation of drug molecules within its mesopores. A kinetic study was performed for nanoencapsulation of magnolol within MCM-41 mesopores and results revealed that the adsorption equilibrium is reached in 15 minutes under ultrasonic irradiation, and the maximum amount of MGN adsorbed is of 145 mg per 1 g of silica matrix. Also, a 34% reduction of the pore volume was obtained after drug loading, while the pore size diminishes accordingly. The in vitro release of magnolol into simulated body fluid (pH = 7.4) at 37o C was investigated. MGN loading degree in the nanoporous matrix was determined by UV-VIS spectrophotometry at ? = 290 nm. The results of the in vitro dissolution test show that MCM-41 act as matrix for sustained-release of MGN for over 12 hours. Taken together, these results suggest that inorganic silica of MCM-41 is suitable to be used as host and prolonged delivery system of magnolol.
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