Poly (lactide-co-glycolide) acid nanoencapsulation of a synthetic coumarin: Cytotoxicity and bio-distribution in mice, in cancer cell line and interaction with calf thymus DNA as target

Evaluation of anti-cancer activity of PLGA nanoparticles containing crocetin

“…The better efficacy of crocetin loaded into PLGA NPs in comparison to free crocetin maybe due to differential cellular uptake and improve the aqueous solubility of crocetin which further enhances its efficacy to induce apoptosis in cancer cells. This finding is similar to other studies in which drug loaded in PLGA NPs could increase cellular uptake, bioactivity, and bioavailability of compound (Anand et al 2010, Bhattacharyya et al 2011, Nair et al 2012). …”

“…Poly (lactic-co-glycolic acid) (PLGA) is one of the well-known Food and Drug Administration (FDA)-approved biodegradable and biocompatible polyester which have been widely used as a carrier for gene, vaccine, protein, and peptide delivery (Acharya and Sahoo 2011, Danhier et al 2012, Kim et al 2005. A wide variety of hydrophobic drugs including natural phytochemicals like curcumin, coumarin, and many others have been successfully encapsulated in PLGA as nano-formulation for use in therapeutic applications (Bhattacharyya et al 2011, Lu et al 2009, Makadia and Siegel 2011.…”

SC-III3, a novel scopoletin derivative, induces autophagy of human hepatoma HepG2 cells through AMPK/mTOR signaling pathway by acting on mitochondria

“…However, either in vitro or in vivo antitumor effect of scopoletin is far less profound, and a high elimination rate leads its in vivo effect to maintain only a few minutes. Some derivatives of scopoletin have been reported to exhibit better antitumor effects in vitro and in vivo than scopoletin [12]. We recently synthesized a series of new scopoletin derivatives with different substituents and founded that SC-III3, one of the novel scopoletin derivatives, showed potent antitumor activity at lower concentrations against most of the tested human tumor cell lines in vitro, and significant inhibition of the transplanted mouse Lewis lung carcinomas in vivo [13].…”

Pulmonary delivered polymeric micelles – Pharmacokinetic evaluation and biodistribution studies

“…4C) was similar to the nominal loading ratio (5.14:1) in the micelles ( Table 1). Considering that coumarin-6 is practically impermeable to the blood-brain barrier (BBB) [41], it could be deduced that coumarin-6 penetrated through the BBB encapsulated into micelles. In the literature, little is known about the translocation of the inhaled pharmaceutical nanocarriers from a biopharmaceutical point of view [42].…”