KOtBu-Mediated Reductive Cyanation of Tertiary Amides for Synthesis of α-Aminonitriles.

A simple, mild, catalyst-free, and efficacious KOtBu-mediated reductive cyanation reaction of tertiary amides under hydrosilylation conditions has been described. A series of α-aminonitriles is obtained in moderate to high yield with good functional group tolerance. The reaction works well with a readily available amide substrate, a cheap and versatile base KOtBu, and a commercially available hydrosilane (EtO)3SiH and is convenient for workup and purification.

Recent Advancements in Serum Albumin-Based Nanovehicles Toward Potential Cancer Diagnosis and Therapy.

Recently, drug delivery vehicles based on nanotechnology have significantly attracted the attention of researchers in the field of nanomedicine since they can achieve ideal drug release and biodistribution. Among the various organic or inorganic materials that used to prepare drug delivery vehicles for effective cancer treatment, serum albumin-based nanovehicles have been widely developed and investigated due to their prominent superiorities, including good biocompatibility, high stability, nontoxicity, non-immunogenicity, easy preparation, and functionalization, allowing them to be promising candidates for cancer diagnosis and therapy. This article reviews the recent advances on the applications of serum albumin-based nanovehicles in cancer diagnosis and therapy. We first introduce the essential information of bovine serum albumin (BSA) and human serum albumin (HSA), and discuss their drug loading strategies. We then discuss the different types of serum albumin-based nanovehicles including albumin nanoparticles, surface-functionalized albumin nanoparticles, and albumin nanocomplexes. Moreover, after briefly discussing the application of serum albumin-based nanovehicles used as the nanoprobes in cancer diagnosis, we also describe the serum albumin-based nanovehicle-assisted cancer theranostics, involving gas therapy, chemodynamic therapy (CDT), phototherapy (PTT/PDT), sonodynamic therapy (SDT), and other therapies as well as cancer imaging. Numerous studies cited in our review show that serum albumin-based nanovehicles possess a great potential in cancer diagnostic and therapeutic applications.

Irradiation pretreatment enhances the therapeutic efficacy of platelet-membrane-camouflaged antitumor nanoparticles.

BACKGROUND: Cell membrane-based nanocarriers are promising candidates for delivering antitumor agents. The employment of a simple and feasible method to improve the tumor-targeting abilities of these systems is appealing for further application. Herein, we prepared a platelet membrane (PM)-camouflaged antitumor nanoparticle. The effects of irradiation pretreatment on tumor targeting of the nanomaterial and on its antitumor action were evaluated. RESULTS: The biomimetic nanomaterial constructed by indocyanine green, poly(d,l-lactide-co-glycolide), and PM is termed PINPs@PM. A 4-Gy X-ray irradiation increased the proportions of G2/M phase and Caveolin-1 content in 4T1 breast cancer cells, contributing to an endocytic enhancement of PINPs@PM. PINPs@PM produced hyperthermia and reactive oxygen species upon excitation by near-infrared irradiation, which were detrimental to the cytoplasmic lysosome and resulted in cell death. Irradiation pretreatment thus strengthened the antitumor activity of PINPs@PM in vitro. Mice experiments revealed that irradiation enhanced the tumor targeting capability of PINPs@PM in vivo. When the same dose of PINPs@PM was intravenously administered, irradiated mice had a better outcome than did mice without X-ray pretreatment. CONCLUSION: The study demonstrates an effective strategy combining irradiation pretreatment and PM camouflage to deliver antitumor nanoparticles, which may be instrumental for targeted tumor therapy.

PLGA-Based Drug Delivery Systems for Remotely Triggered Cancer Therapeutic and Diagnostic Applications.

Intelligent drug delivery systems based on nanotechnology have been widely developed and investigated in the field of nanomedicine since they were able to maximize the therapeutic efficacy and minimize the undesirable adverse effects. Among a variety of organic or inorganic nanomaterials available to fabricate drug delivery systems (DDSs) for cancer therapy and diagnosis, poly(D,L-lactic-co-glycolic acid) (PLGA) has been extensively employed due to its biocompatibility and biodegradability. In this paper, we review the recent status of research on the application of PLGA-based drug delivery systems (DDSs) in remotely triggered cancer therapy and the strategies for tumor imaging provided by PLGA-based DDSs. We firstly discuss the employment of PLGA-based DDSs for remotely triggered cancer therapy, including photo-triggered, ultrasound-triggered, magnetic field-triggered, and radiofrequency-triggered cancer therapy. Photo-triggered cancer therapy involves photodynamic therapy (PDT), photothermal therapy (PTT), and photo-triggered chemotherapeutics release. Ultrasound-triggered cancer therapy involves high intensity focused ultrasound (HIFU) treatment, ultrasound-triggered chemotherapeutics release, and ultrasound-enhanced efficiency of gene transfection. The strategies which endows PLGA-based DDSs with imaging properties and the PLGA-based cancer theranostics are further discussed. Additionally, we also discuss the targeting strategies which provide PLGA-based DDSs with passive, active or magnetic tumor-targeting abilities. Numerous studies cited in our review demonstrate the great potential of PLGA-based DDSs as effective theranostic agent for cancer therapy and diagnosis.

[Enhancers on the transmembrane transport of chlorogenic acid].

To investigate the influence of the difference enhancers on the transport mechanism of chlorogenic acid (CGA) across Caco-2 cells model, a RP-HPLC method was adopted to detect the concentrations of CGA. At the concentrations of 20 to 80 microg x mL(-1), the difference of absorption rate constants (K(a)) was not statistically significant. At the concentrations of 40 and 20 microg x mL(-1), the ratios of apparent permeability coefficients (P(app)) of the apical to basolateral and the basolateral to apical were 1.14 and 1.18, respectively. With the effect of enhancers K(a) and P(app) increased, the absorption half-life (T1/2) decreased. CGA passed through the Caco-2 cell membrane mainly by passive transport. It showed that monocarboxylic acid transporter (MCT) could be involved in the across membrane transport process of CGA. Borneol had no effect on the cell membrane transport processes. The order of increasing absorption of CGA caused by the enhancers was sodium lauryl sulphate > sodium taurocholate > carbomer.

[Recent development of targeted drug delivery system].

Targeted drug delivery can significantly increase the concentration of the drug in treatment site, and decrease the dosage of drugs, cost of treatment and the drug's adverse effects on the body. So targeted drug delivery is the hotspot of recent studies. This paper reviews the development of targeted drug delivery research in recent years, including three areas: passive targeting, active targeting, and physical and chemical targeting.