Solubility, Antioxidation, and Oral Bioavailability Improvement of Mangiferin Microparticles Prepared Using the Supercritical Antisolvent Method

Abstract

In view of the poor water solubility and low oral bioavailability of mangiferin (MG), in this study, the supercritical antisolvent (SAS) technology was used to prepare mangiferin microparticles (MG MPs) with N,N-dimethylformamide (DMF) as solvent and carbon dioxide as antisolvent, so as to improve its water solubility, antioxidant capacity and oral bioavailability. Four factors affecting the solubility of the MG MPs were investigated by orthogonal design (OAD), including precipitation pressure, precipitation temperature, MG concentration and feeding speed, and the optimal preparation conditions were determined by range and variance analysis (ANOVA). Under the optimal conditions, the spherical MG MPs with an average diameter of 532.8 nm was obtained, and the yield of the powder was about 95.3%. Scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FTIR), X-Ray Diffractometry (XRD), differential scanning calorimetry (DSC), and thermal gravimetric (TG) were used to analyze the characteristics of the MG MPs. The results obtained showed that the chemical structure of the MG did not change before and after supercritical crystallization, but its particle size and crystallinity decreased significantly. The MG MPs had a higher solubility, and was about 4.26, 2.1 and 2.5 times than that of free MG in water, artificial gastric juice (AGJ) and artificial intestinal juice (AIJ), respectively. The dissolution rate of the MG MPs were also obviously higher than that of free MG. Furthermore, the bioavailability of the MG MPs in vivo was about 2.07 times higher than that of the free MG, and its antioxidant capacity was also much higher than that of free MG, which was close to vitamin C.

Design of Nanotechnological Carriers for Ocular Delivery of Mangiferin: Preformulation Study

“…The DSC analysis of MGN was also carried out. In accord with the literature data [37,38], MGN had an endothermic peak centered at 272.11 °C (Figure S1, supporting information). The effect of different molar fraction of MGN (0.03; 0.045; 0.06; 0.09; 0.12; 0.15) on the biomembrane model made of MLV of 1,2-dimyristoyl-sn-glycero-3-…”

Pharmacokinetic and metabolomic analyses of Mangiferin calcium salt in rat models of type 2 diabetes and non-alcoholic fatty liver disease

“…It has shown many kinds of biological activities and pharmacological actions such as antioxidative, antidiabetic, hypolipidemic, antiviral, immunomodulatory, anticancer, analgesic and hepatoprotective effects [16][17][18][19][20]. But the characteristic of its low aqueous solubility and low fat solubility can affect the absorption process of drugs in vivo, which leads to a low bioavailability [21,22]. It makes us have to suffer such problems like mangiferin is hard to further develop a new medicine and its clinical application has certain limitation.…”

Supercritical Antisolvent Process for Pharmaceutical Applications: A Review

“…For these purposes, the SAS technique is one of the most effective micronization techniques based on the use of supercritical CO 2 . Up to now, several active compounds, such as antibiotics [25,[58][59][60][61][62][63][64], NSAIDs [46,65], antioxidant compounds [1,6,7,38,66], anticancer drugs [3,4,[67][68][69], and others [2,32,[70][71][72], were micronized in the form of nanoparticles, sub-microparticles, and microparticles using the SAS process.…”

“…Regarding the pharmaceutical field, using the SAS process, up to now, micronized drug particles and several polymer/active compound composites have been proposed for different biomedical applications [31][32][33][34][35]. Indeed, SAS precipitated particles can be used for drug delivery by oral, parenteral, transdermal, or topical routes [2,[36][37][38][39][40][41][42]. The versatile SAS particles can be used in powder form for the oral administration of composites or the preparation of aerosol formulations, mainly for the treatment of respiratory diseases; they can also be used for the production of medicated patches or active topical gels, by incorporating nanoparticles/microparticles into various types of dressings, supports or pomades, respectively.…”