Preparation and Evaluation of SBA-16, ZSM-5 and MCM-41 Mesoporous Silica Nanoparticles as Drug Delivery System for Carvedilol

Abstract

Carvedilol is a non-selective beta/alpha1 blocker that is broadly used in treatment of arrhythmia, congestive heart failure, hypertension, and myocardial infarction. Enhancing carvedilol low solubility and dissolution rate would help in improving the efficiency of the tablet dosage form. In this study, different types of silica nanoparticle (NPs) (SBA-16, MCM-41 and ZSM-5) were synthesized. Coupling of SBA-16 with 3-Aminopropyl-triethoxysilane (APTES) was performed to improve surface characteristics of SBA-16. Different methods to load carvedilol on these carriers were used with high-performance liquid chromatography (HPLC) as a method of analysis for carvedilol. For the characterization of the loaded NPs Fourier -transform infrared spectroscopy (FT-IR), X ray crystallography (XRD) and Therapeutic goods administration (TGA) were used. MCM-41 loaded with Carvedilol was decided to be formulated as tablet dosage and compared with tablets contain carvedilol without carrier. The results showed that SBA-16, SBA-16 coupled, ZSM-5 and MCM-41 carriers were used successfully to load carvedilol in a good drug load percent of 64.5, 69.3, 82 and 90%, respectively. MCM-41 gave highest loading efficiency of carvedilol using solvent evaporation method and the dissolution of carvedilol from powder was superior to the pure carvedilol where it gave 100% release of the drug at 15 minutes compared to 30% of pure carvedilol. MCM-41 loaded with carvedilol was successfully formulated as tablet dosage form according to the specifications of USP and the release of carvedilol from the prepared tablet was 99% at 15 min compared to the carvedilol released from tablets prepared using carvedilol powder which gave 38% which indicates the efficiency of the carrier in increasing the solubility and dissolution of carvedilol, a class II BCS drugs.