Abstract
3',6-dimethoxy-3'',4''-(methylenedioxy)-2,5-epoxylignan-4'-ol (DMEO), an epoxylignan isolated from Piper nigrum, has currently captured attention for its potential antitumor effect. However, low stability is limiting its therapeutic application. The application of nanocapsulation would be the main strategy for overcoming this problem. DMEO-loaded nanocapsules were prepared by an emulsion-diffusion method using Eudragit RL 100 (at concentrations of 1, 1.5 and 2%) and polyvinyl alcohol. As the polymer content increased, the encapsulation efficiency and mean particle size also increased. After 6 months of storage at 25°C (0% RH), no crystalline peaks were observed in the diffraction patterns of all nanocapsules, thereby suggested that the physical stability of nanoencapsulated DMEO was not affected by the concentration ratio of the polymer-stabilizer combinations.
Highlights
The hedgehog (Hh) pathway is required for the growth and proliferation of various cancers[1]
The unchanged position of the largest peak of DMEO, which remains at 19.3° 2θ (Figure 2a, 2b and 2c), indicates that there is no change in the diffraction pattern of DMEO after 6 months of storage
It is important for the DMEO particles to remain stable during 6 months of storage to ensure that the resulting DMEO-loaded nanocapsules meet the minimal standard requirements of drug formulation stability
Summary
The hedgehog (Hh) pathway is required for the growth and proliferation of various cancers[1]. The signaling begins with the binding of Hh protein ligand to its membrane receptor Ptch, which represses the activity of Smoothened (Smo). The direct association of GLI with a specific binding site (5’-GACCACCCA-3’) in the promoter region of the target gene has been reported to contribute to pancreatic and prostate cancer cells[3]. DMEO was confirmed to have Hh signaling inhibitory activity and to be selectively cytotoxic against PANC1. The synthetic epoxylignan of DMEO related compound was reported to inhibit the mRNA expression of protein patched homolog (Ptch) in human pancreatic cancer cells (PANC1) and is considered to be a prospective drug candidate to treat cancer related to the GLI signaling pathway. The nanoencapsulation of DMEO is one of the ways of overcoming the problem
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