5,6-Bis(benzylideneamino)-2-mercaptopyrimidin-4-ol (SCR7) is a new anti cancer molecule having capability to selectively inhibit non-homologous end joining (NHEJ), one of the DNA double strand break (DSB) repair pathways inside the cells. In spite of the promising potential as an anticancer agent, hydrophobicity of SCR7 decreases its bioavailability. Herein the entrapment of SCR7 in Pluronic copolymer is reported. The size of the aggregates was determined by transmission electron microscopy (TEM) and dynamic light scattering (DLS) which yields an average diameter of 23 nm. SCR7 encapsulated micelles (ES) were also characterized by small-angle neutron scattering (SANS). Evaluation of its biological properties by using a variety of techniques, including Trypan blue, MTT and Live-dead cell assays, reveal that encapsulated SCR7 can induce cytotoxicity in cancer cell lines, being more effective in breast cancer cell line. Encapsulated SCR7 treatment resulted in accumulation of DNA breaks within the cells, resulting in cell cycle arrest at G1 phase and activation of apoptosis. More importantly, we found ≈ 5 fold increase in cell death, when encapsulated SCR7 was used in comparison with SCR7 alone.

Nonhomologous end joining (NHEJ) of DNA double strand breaks (DSBs) inside cells can be selectively inhibited by 5,6-bis-(benzylideneamino)-2-mercaptopyrimidin-4-ol (SCR7) which possesses anticancer properties. The hydrophobicity of SCR7 decreases its bioavailability which is a major setback in the utilization of this compound as a therapeutic agent. In order to circumvent the drawback of SCR7, we prepared a polymer encapsulated form of SCR7. The physical interaction of SCR7 and Pluronic® copolymer is evident from different analytical techniques. The in vitro cytotoxicity of the drug formulations is established using the MTT assay.

The interaction of SDS/SDBS in aqueous gelatin solutions is studied above the gelation temperature by viscosity and circular dichroism (CD) measurements. The steep rise observed in the relative viscosity can be due the structural transitions leading to micellar growth of higher order. Circular dichroism spectra indicated that gelatin helped in inducing the sphere?rod transition, without suffering any conformational changes within it. The findings are particularly significant in terms of the head group contribution, hydrophobic interaction and the formation of formulated complexes.

RNA interference (RNAi) has been emerged as an effective method to silence a particular gene utilizing a sequence‐specific mechanism for gene regulation. It induces target mRNA degradation leading to a lower illness‐inducing gene product. RNAi represent a conserved mechanism. Novel concept of highly specific silencing of genes was revolutionized by the introduction of short interfering RNA (siRNA).This helped to overcome the drawbacks of RNAi and proved out to be a safer and efficient method than its counterpart finding its way into the pharmaceutical industry. Clinical trials enhanced the possibility of siRNA delivery and yielded promising results for the treatment of a wide range of illnesses but mainly for intractable diseases like cancer, inflammatory diseases, and genetic disorders. siRNA delivery methods were instrumental in developing it as a therapeutic, of which lipid encapsulation crept its way, to be a better in vivo delivery mechanism as it could be formulated effectively, being biodegradable, and has a lower toxicity level. However, the therapeutic potential of siRNA remains hampered due to a lack of a viable delivery method, a lower accuracy in tissue specificityand cytotoxicity. Hence the therapeutic usage of the method is in its budding stage. This review re‐examines the principle of siRNA, challenges in its delivery, and some recent advancesto overcome the obstacles in order to improve siRNA delivery.