Carry-On Nitric-Oxide Luggage for Enhanced Chemotherapeutic Efficacy.

In this work, we proposed a carry-on nitric-oxide (NO) luggage strategy for enhanced chemotherapeutic efficacy. A stimuli-responsive NO-releasing polypeptide was prepared as the building block to assemble into a micelle as a chemodrug-carrier. The micelle was anchored with cRGD peptide with the aim of targeting to tumors' neoangiogenesis. In situ generation of NO at the tumor site can promote the neovascularization to recruit more chemotherapeutics. Besides, the introduced exogenous NO can directly induce apoptosis, synergistically with the chemotherapeutics. A specific near-infrared-region (NIR) NO-probe was also developed to be coloaded to the micelle to report the in situ NO-release. In vitro and in vivo experiments were performed to demonstrate the targeting capability, increased accumulation, real-time NO-release reporting phenomenon, improved antitumor efficacy, and favorable biosafety. Embedding NO into drug cargo as carry-on luggage for enhanced chemotherapeutic efficacy, hopefully, can cast new lights and build a basic principle in the future clinical translation of nanomedicines.

The Physicochemical Investigation of 17ß-Estradiol Crystalline Prepared by In Situ pH-Dependent Solubility Technique with Polyvinylpyrrolidone.

Micro-particles of 17ß-estradiol (ED) were prepared with polyvinylpyrrolidone (PVP) by in situ pH-dependent solubility technique. Products were characterized using multiple instruments, and molecular interactions between ED and PVP were explored. Powder X-ray diffraction and thermal analysis revealed crystalline ED in the micro-particles is hemihydrated. PVP was also present in the micro-particles. Laser particle size analysis and scanning electron microscopy revealed thin slice morphology, which might have resulted from the influence of PVP. Moreover, the results of contact angle, specific surface area, and dynamic vapor sorption showed that the surface properties of products were improved. These physicochemical properties of the micro-particles resulted in an obvious improvement in dissolution rate. Fourier transform infrared spectroscopy and 1H nuclear magnetic resonance revealed hydrogen bonding between ED and PVP. A method was established for the preparation of micro-particles through the addition of PVP during the reaction process.