Fabrication, characterization and in vitro evaluation of silibinin nanoparticles: an attempt to enhance its oral bioavailability

Abstract

BackgroundSilibinin has gained in importance in the past few decades as a hepatoprotector and is used widely as oral therapy for toxic liver damage, liver cirrhosis, and chronic inflammatory liver diseases, as well as for the treatment of different types of cancers. Unfortunately, it has low aqueous solubility and inadequate dissolution, which results in low oral bioavailability.Materials and methodsIn this study, nanoparticles (NPs) of silibinin, which is a hydrophobic drug, were manufactured using two cost-effective methods. Antisolvent precipitation with a syringe pump (APSP) and evaporative precipitation of nanosuspension (EPN) were used. The prepared NPs were characterized using different analytical techniques such as scanning electron microscopy (SEM), fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), and X-ray powder diffractometry (XRD) and were sifted for their bioavailability through in vitro dissolution and solubility studies. Moreover, the prepared NPs were evaluated for antimicrobial activity against a battery of bacteria and yeast.ResultsDSC and XRD studies indicated that the prepared NPs were amorphous in nature, with more solubility and dissolution compared to the crystalline form of this drug. NPs prepared through the EPN method had better results than those prepared using the APSP method. Antimicrobial activities of the NPs were improved compared to the unprocessed drugs, while having comparable activities to standard antimicrobial drugs.ConclusionResults indicate that the NPs have significantly increased solubility, dissolution rate, and antimicrobial activities due to the conversion of crystalline structure into amorphous form.

Berberine nanoparticles with enhanced in vitro bioavailability: characterization and antimicrobial activity

“…The enhancement of the solubility may be attributed to the changes in the crystalline nature of BBR to a semi-crystalline or less crystalline form. 15 , 42 , 46 – 49 The nano form of BBR has more free energy compared to the micro form which further helps in improving the solubility of the NPs. It is evident from Figure 7 that the solubility of BBR in distilled water is very close to that of PBS (pH 6.8).…”

“… 10 Evaporative precipitation of nanosuspension (EPN) and anti-solvent precipitation with a syringe pump (APSP) are among the approaches that are used to address the problems of solubility, dissolution rate and bioavailability. 11 , 15 Fessi et al first developed and patented a solvent displacement method for the simple and rapid preparation of a nanosuspension as presented in Bilati et al 12 …”

Flavonoid Nanoparticles: A Promising Approach for Cancer Therapy

“…Free silibinin has low solubility and inadequate dissolution, which cause low oral bioavailability. The Sahibzada et al study shows two methods for manufacturing nanoparticles of silibinin (APSP—anti-solvent precipitation with a syringe pump and EPN—evaporative precipitation of nanosuspension), which increase its solubility, making this flavonoid a potential oral drug in cancer therapy [ 69 ]. Huo et al showed that the combination therapy of silibinin and paclitaxel (PTX) loaded in dextran-deoxycholic acid (Dex-DOCA) nanoparticles effectively accumulate in tumour sites by passive targeting and inhibit tumour growth through an enhanced intratumoural penetration in mice [ 70 ].…”

Formulation Strategies for Enhancing the Bioavailability of Silymarin: The State of the Art

“…That work was the first reporting SIL-loaded nanodispersion produced via microfluidics, enabling efficient control over the particle size, homogeneity, and drug release performance. The antisolvent precipitation with a syringe pump (APSP) was employed to produce SIL-loaded NPs in order to improve the bioavailability of the hydrophobic cargo [52].…”