Silymarin Encapsulated Poly(D, L-lactic-co-glycolic acid) Nanoparticles: A Prospective Candidate for Prostate Cancer Therapy

Abstract

Silymarin, a clinically proved hepato-protective herbal drug having significant anti-cancerous property towards prostate cancer, is inadequately utilized for cancer therapy due to its hydrophobic nature and poor bioavailability. In this work, we have developed silymarin Poly(D,L-lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) in order to improve the therapeutic efficacy of silymarin towards prostate cancer by single emulsion solvent evaporation technique. The prepared nanoparticles had an encapsulation efficiency of 60% and a loading efficiency of 13%. The silymarin-PLGA NPs (SNPs) characterization, using DLS and SEM analysis revealed its size as less than 300 nm. FT-IR analysis confirmed encapsulation of silymarin by the SNPs, whereas XRD and TGA proved amorphous nature of the SNPs. In vitro drug release study demonstrated a slow and sustained release of encapsulated drug from the SNPs in physiological conditions. The hemocompatibility of the SNPs was established by in vitro hemolysis and coagulation assays. In vitro cell viability studies revealed preferential toxicity of SNPs towards prostate cancer cells (PC-3) compared to normal cells (Vero) in a dose dependant way. Cell uptake studies using confocal microscopy confirmed internalization of the SNPs by PC-3 cells. Furthermore, in vitro cell migration assay showed a concentration and time dependent inhibitory effect of SNPs on PC-3 cell migration. Finally, flow-cytometry based apoptosis assay suggested induction of apoptosis mediated death in PC-3 cells by the SNPs. Overall, the prepared SNPs proved as a promising candidate for prostate cancer therapy.

Preparation and characterization of silymarin synchronized-release microporous osmotic pump tablets

“… 5 , 6 SM has also been proved to possess significant anti-cancerous properties toward liver and prostate cancers. 7 SM is mainly composed of five active components, including taxifolin (TF), silychristin (SC), silydianin (SD), silybin (SB), and isosilybin (ISB). 8 Currently, there are commercially available SM-loaded products such as Legalon ®9 and Silipide ®10 capsules.…”

<p>Novel Drug Delivery Systems for Loading of Natural Plant Extracts and Their Biomedical Applications</p>

“…146 More examples of herbal loaded NE are presented in Table 1. 142,143,[147][148][149] Nanocrystals They are pure drug crystals with nanosized particles (Figure 9) in which toxic side effects resulting from the encapsulating/solubilizing excipients may be eliminated. 150 The best known features of nanocrystals are high drug-loading capacity and platform stability that render them to be widely used to deliver poorly hydrophilic materials in the form of a colloidal dispersion.…”

Advanced Nanotechnologies for Enhancing the Bioavailability of Silymarin: A State of the Art

“…In a different study, SIL NPs were prepared by Snima et al [97] through ESE method using PLGA as polymeric nanocarrier. The particle hydrodynamic diameter was about 220 nm and SIL entrapment efficiency was 60%.…”