Preparation and physicochemical characterizations of tanshinone IIA solid dispersion

Abstract

This investigation describes a novel approach to prepare solid dispersions of tanshinone IIA using a laboratory-scale planetary ball mill. Poloxamer 188 was employed as the surfactant carrier to improve the solubility and dissolution of the poorly soluble drug, tanshinone IIA. Solubility and dissolution were evaluated compared to the corresponding physical mixtures and pure drug. Furthermore, the physicochemical properties of the solid dispersions were investigated using scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry, Fourier transform infrared spectroscopy and ultraviolet spectrophotometry. The solid dispersion significantly enhanced drug solubility and dissolution compared with pure drug and the physical mixtures. Scanning electron microscopy, powder X-ray diffraction, differential scanning calorimetry and Fourier transform infrared spectroscopy analyses of tanshinone IIA/poloxamer 188 system confirmed that there were intermolecular interactions between tanshinone IIA and poloxamer 188 and no conversion to crystalline material. Tanshinone IIA existed in a microcrystalline form in the system. These results suggested that improvement of the dissolution rate could be correlated to the formation of a eutectic mixture between the drug and the carrier. After 60 days the solid dispersion samples were chemically and physically stable. The present studies indicated that the planetary ball mill technique could be considered as a novel and efficient method to prepare solid dispersion formulations.

An attempt to stabilize tanshinone IIA solid dispersion by the use of ternary systems with nano-CaCO3and poloxamer 188

“…[17] and Zhao et al . [15] During scanning of TSIIA/nano-CaCO 3 /poloxamer PMs [Figure 3c], the drug endothermic peak was found at 208.3°C, indicating that the absence of interaction between TSIIA and carriers in PMs and TSIIA existed in a virgin form in the system. In DSC spectra of tSDs [Figure 3d], the characteristic peak of TSIIA had completely disappeared, suggesting that the drug may be present in tSDs as amorphous state, which was responsible for the enhancement of drug dissolution.…”

“…Similar observations have been reported by Zhao et al . [15] The FTIR spectrum of carriers showed the peaks at 3487 cm -1 , which corresponded to -OH stretching vibration mode. This could be attributed to the presence of hydroxyl groups and (or) adsorbed water on the surface of nano-CaCO 3 particles.…”

“…[1011121314] Dissolution rates can be improved by particle size reduction, increased wettability through mixing with highly soluble carriers, and maintenance of the drug in the amorphous form. [151617] Although the application of SDs has been reported regularly in the pharmaceutical literature, only a few commercial products rely on the SDs strategy. One of the main reasons for this discrepancy is the possible thermodynamical instability of amorphous drug[1819] that have the tendency to change to a more stable state under recrystallization on storage,[202122] which inevitably results in decreased solubility and the dissolution rate.…”

Preparation, characterization, and in vivo evaluation of tanshinone IIA solid dispersions with silica nanoparticles

“…26 Currently, the typical carriers widely used for the formulation of SDs consist of organic materials that are highly water soluble and/or polymeric in nature. [27][28][29][30] In addition to these carriers, inert hydrophilic carriers, such as inorganic silica-based materials 31,32 which have relatively large specific surface areas, and thus produce powders in which the drug may be highly dispersed, are receiving increasing attention. Takeuchi et al [33][34][35] reported that SDs with porous silica or colloidal silica prepared using the spray-drying method can improve the dissolution property of tolbutamide and indomethacin.…”

Hydrogen peroxide-mediated oxidative stress and collagen synthesis in cardiac fibroblasts: Blockade by tanshinone IIA

“…Tanshinone IIA (Tan IIA) is a major component of Salvia miltiorrhiza Bunge known as Danshen which has long been used for prevention and treatment of cardiovascular diseases in China (Ren et al, 2010;Zhao et al, 2011;Gao et al, 2012). Accumulating studies show that Tan IIA possesses many biological properties, largely depending on its anti-oxidative effects (Yang et al, 2008;Chen et al, 2012).…”