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Solubility Enhancement of Aripiprazole via Mesoporous Silica: Preparation, Characterization, In vitro Drug Release, and Solubility Determination
PawanDevangan,AakashSaini,DigeshwariPatel,UjwalKolhe
Journal of Pharmaceutical Innovation Pub Date : 03/20/2023 00:00:00 , DOI:10.1007/s12247-023-09722-9
Abstract
PurposeHollow types of mesoporous silica have been extensively used as drug delivery carriers owing to their excessive drug loading competence in the interior void cavity as well as enhancement of solubility. The main aim of this study was to improve the solubility and dissolution rate of ARPZ, a class II drug, upon incorporation into mesoporous silica (SBA-15).MethodsARPZ was loaded in mesoporous silica using specific SBA-15 to solubilize by the wet impregnation method. The optimization was done via solubility and drug loading parameters. Characterization of the optimized formulation ARPZ-loaded SBA-15 (60%) (1.5:1 w/w) for possible molecular interaction between the ARPZ and silica was carried out by using FTIR, crystalline characteristics via PXRD, thermal analysis through DSC, and TGA, and pore size and surface area were determined by Brunauer–Emmett–Teller (nitrogen adsorption isotherm). Furthermore, an in vitro release study was examined by paddle-type dissolution apparatus (USP type II) in pH 1.2 buffer.ResultsThe optimized ARPZ-loaded SBA-15 (60%) showed a drug loading of 37–38% w/w. Incorporating the drug inside SBA-15 pores reduced the values of three parameters of empty SBA-15, (a) pore size from 5.21 to 4.19 nm, (b) pore volume from 0.652 to 0.178 cm3/g, and (c) specific surface area from 622.4 to 136.7 mg2/g. Crystalline ARPZ was converted to amorphous upon incorporation into pores of mesoporous silica. Optimized ARPZ-loaded SBA-15 (60%) exhibited more than 3 to fourfold enhancement in equilibrium solubility and dissolution after 15 min, respectively, compared to the pure ARPZ. The results showed an improvement in the solubility of ARPZ upon incorporation into pores of mesoporous silica SBA-15.ConclusionSBA-15 was found more suitable for the solubility enhancement of the poorly water-soluble drug ARPZ.Graphical Abstract
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