- A novel polymer micelle as a targeted drug delivery system for 10-hydroxycamptothecin with high drug-loading properties and anti-tumor efficacy
-
A novel polyethylene glycol-polycaprolactone-poly-L-tyrosine (MPEG-PCL-PTyr) amphiphilic triblock copolymer micelle was synthesized for the first time. 10-hydroxycamptothecin (HCPT) was embedded in MPEG-PCL-PTyr nanomicelles using the emulsion solvent evaporation method. A series of was conducted to confirm the structure of the compound and to evaluate the physical properties of the MPEG-PCL-PTyr nanomicelles. Cellular uptake, cytotoxicity, and apoptosis were assessed using flow cytometry and MTT assays. Confocal microscopy and flow cytometry results demonstrated that the nanocapsules carrying HCPT had significantly increased anti-tumor activity against HepG2 cells and could target HepG2 cell lysosomes with obvious liver targeting. In addition, the drug-loaded nanomicelles could significantly block the S phase of cancer cells and induce apoptosis; thus, they could be potential carriers for future 10-HCPT delivery and cancer treatment.
- Guo, Yuyan,Gao, Tao,Fang, Fang,Sun, Shuang,Yang, Dayu,Li, Yongji,Lv, Shaowa
-
-
- Polyamino acid carrier with acid-sensitive connecting arm in middle as well as preparation method and application of polyamino acid carrier
-
The invention discloses a polyamino acid carrier with an acid-sensitive connecting arm in the middle as well as a preparation method and application of the polyamino acid carrier. The polyamino acid carrier contains a hydrophilic part, a hydrophobic part and a responsive connecting arm; a specific disulfide bond is introduced into the carrier design, the disulfide bond can be controllably broken into sulfydryl in vitro, the small molecule with the sulfydryl fragment or the gene with sulfydryl inherent on the surface is bonded with the protein drug again, and a covalent disulfide bond is formedto complete chemical bonding delivery of the drug. The polyamino acid carrier and the drug are bonded in a covalent bond manner, so that the drug can be stably transported in systemic circulation. When the carrier reaches high-metabolism and high-reducibility parts such as tumors or inflammations, disulfide bonds are broken again under the condition of high glutathione (GSH), and the activity ofthe drug is released and recovered. Therefore, the purposes of firstly masking the drug activity, then stably delivering the drug in vivo and recovering accurate regulation and control of the drug activity after the drug reaches a target position are achieved.
- -
-
Paragraph 0050-0053
(2020/09/20)
-
- ENANTIOMERIC QUANTIFICATIONS OF AMINO ACIDS THROUGH THEIR Nα-ACYL AMIDES BY GAS CHROMATOGRAPHY.
-
Apparent separation of 1.1 or higher on Chiralsil Val III can be obtained for Nα-acyl N-alkyl aminoacid amides allowing the use of short capillary gas chromatographic columns.A clean derivatization protocol without racemization is described, proceding through the NCA derivatives that are prepared from "in situ" silylated amino acids with trimethylsilyl cyanide.
- Hosten, N.,Anteunis, M. J. O.
-
-