Clinical studies examining the combination of paclitaxel (PTX) and everolimus (EVER), an mTOR inhibitor, have failed to result in significant improvements in efficacy and toxicity in patients with breast cancer (BC), relative to treatment with PTX alone. Recently, a research paper published in Molecular Pharmaceutics reported co-delivery of Paclitaxel and Everolimus by polymeric micelles at an optimal synergistic ratio to achieve specific, colocalized delivery of the combination therapy in BC cell lines. The nanoparticles were prepared from PLGA-PEG and PLGA-PEG-FITC (Nanosoft Polymers) had an average diameter of less than 100 nm and were capable of in vitro retention of the encapsulated PTX and EVER at the optimal synergistic molar ratio for over 7 days. The uptake of FITC-labeled NPs in SKBR3 cells was evaluated by flow cytometry, with approximately 41% of cells demonstrating detectable fluorescence after 24 h of exposure. The thorough and systematic approach used in this study to determine and evaluate a synergistic PTX:EVER ratio in conjunction with a potentially promising delivery vector for the drug combination could offer a future clinical benefit for patients with BC.  Mol Pharm. 2018 Jun 14. doi: 10.1021/acs.molpharmaceut.8b00217.

Targeted drug delivery has been an important issue for tumor therapy including photodynamic therapy (PDT). Folate receptor (FA) is over-expressed on the surface of many human cancer cells.  Recently, a research published in Biochemical and Biophysical Research Communications (BBRC) has reported FA-targeted nanoparticles carrying a photosensitizer (PS) for PDT of cancer. The nanoparticles were prepared from DSPE-MPEG and  DSPE-PEG5K-folate (Nanosoft Polymers) . The nanoparticles were highlighted with 1) Folate-modified PLGA nanoparticles (FA-PLGA-Pba NPs) were developed with non-toxic materials. 2) FA-PLGA-Pba NPs were stable in aqueous condition for long time without aggregation. 3) FA-PLGA-Pba NPs killed cancer cells effectively upon laser irradiation, and showed superior tumor-targeting in vivo.  In vivo and ex vivo imaging showed high accumulation of FA-PLGA-Pba NPs in tumor site during 24 h after intravenous injection to MKN28 tumor-bearing mice model. These results demonstrate that our FA-PLGA-Pba NPs are useful for tumor-targeted delivery of PS for cancer treatment by PDT. Biochem Biophys Res Commun. 2018 Apr 6;498(3):523-528. doi: 10.1016/j.bbrc.2018.03.013. Epub 2018 Mar 5.

Aminopeptidase N (APN/CD13) is closely related to the growth of cancers and is suggested as a suitable target for anti-cancer therapy.  Recently, a research group used the “one-bead-one-compound” (OBOC) approach on a microarray device to scren out a novel affinity peptide LN (YEVGHRC). It was found that LN could specifically recognize and bind to APN; Moreover, LN-functionalized liposomes (LN-LS) could achieve efficient nano-encapsulated drug delivery under APN-overexpressing tumor conditions in vitro and in vivo,   providing a new strategy for APN-positive tumor diagnosis and therapy. Biomater Sci. 2017 Feb 28;5(3):417-421.

HER2 is a biomarker of human breast cancer has become an important validated therapeutic target in breast cancer. Recently, a research published in Theranostics using OBOC to screen  a library of novel HER2 targeting peptides. These targeting peptides were conjugated to DSPE-PEG-Maleimide (Nanosoft Polymers) to develop HER2 targeted liposomes for doxorubicin delivery to improve the cancer therapy and diagnosis.  Geng L. et al. HER2 Targeting Peptides Screening and Applications in Tumor Imaging and Drug Delivery. Theranostics. 2016: 6(8): 1261-1273.

Polyethylenimine (PEI) as a cationic polymer is commonly used as a carrier for gene delivery. PEI-800 is less toxic than PEI-25K but it is also less efficient. A novel nanocarrier was developed by combining PEI-800 with a pH-sensitive lipid to form polymer-lipid hybrid nanoparticles (P/LNPs). They were synthesized by microfluidic focusing (MF). Two microfluidic devices were used to synthesize P/LNPs loaded with VEGF siRNA. A series of P/LNPs with different particle sizes and distributions were obtained by altering the flow rate and geometry of microfluidic chips, and introducing sonication. Furthermore, the P/LNPs can be loaded with VEGF siRNA efficiently and were stable in serum for 12 h. Finally, P/LNPs produced by the microfluidic chip showed greater cellular uptake as well as down-regulation of VEGF protein level in both A549 and MCF-7 with reduced cellular toxicity. All in all, the P/LNPs produced by MF method were shown to be a safe and efficient carrier for VEGF siRNA, with potential application for siRNA therapeutics. Molecules 2016, 21(10), 1314; https://doi.org/10.3390/molecules21101314