The Preparation And Activity Research Of Paclitaxel Nanocrystals Combined With The IRGD Peptide

Paclitaxel has a good anti-tumor activity which it always was regarded as achemotherapy drug. Unfortunately, for a very long time, drug insolution as well astoxic to the patients are a barral to the chemotherapy technology development. Tosolve this problem, scientists always regard the development of new chemotherapydrug as an important way and it has been a hot spot for very long time. In this article,paclitaxel, represented by poorly soluble tumor chemotherapy drugs, for example,build a combination of the iRGD peptide with the ability to penetrate the tumorpaclitaxel nanocrystals, and carried out research in this new drug formulations tumortargeted therapy.In this article, we have done the following3works:1. We preparedpaclitaxel nanocrystals (PNs)which is of uniform particle size andthe size of approximately20nm using carboxyl Pluronic F127surfactant by emulsionfreeze-drying method. And the PNswere modified by iRGD peptide in order to buildnano-drug delivery systemwhich possess the ability of both tumor tissue and cellpenetration；2. Pharmacodynamic evaluation of NPs was test at cellular level. The resultsshowed that the molecular structure of PEGend of Pluronic F127can effectivelyreducethe interaction between NPs and macrophase, endow NPs with goodstealth.Integrin αvβ3was overpressionon mouse breast cancer cells (4T1) surface,which enhancedthe targeting ability of iPNs; In addition, cytotoxicity results showedthat NPs and iNPs possessed high cancer cell-killing ability;3. To investigate the ability of tumor penetration of NPs, we introduced3-Dculture system of cancer cells. Combined with confocal imaging system results showedthat, iRGD modification of NPs greatly enhanced the tumor penetration, thus greatlyimproved the effect of chemotherapy.