title: Preparation and investigation of high solid content PTX-loaded nanoparticles dispersion via nanoprecipitation method.
abstract: The improvement of the solid content of the hydrophobic drugs (such as paclitaxel (PTX), etc.) loaded nanoparticles (NPs) dispersion is important for enhancing drug-loaded efficiency and reducing the cost in production and application. A diblock copolymer methoxy poly(ethylene glycol)-b-poly(ε-caprolactone-co-1,4,8-trioxa[4.6]spiro-9-undecanone) (mPECT) is synthesized via the ring-opening polymerization of ε-caprolactone and 1,4,8-trioxa[4.6]spiro-9-undecanone (TOSUO) with methoxy poly(ethyleneglycol) (mPEG） as the initiator. The chemical structures and thermal properties of mPECT are characterized by (1)HNMR, Fourier transform infrared (FT-IR), gel permeation chromatography, differential scanning calorimetry, etc. PEG45.45-b-P(C28.33-co-T5.38) (mPECT-2) is able to self-assemble into stable NPs in water via nanoprecipitation method at a high solid content (≤25 wt%) and their freeze-dried powders can well re-disperse in water. The paclitaxel (PTX) is chosen as a hydrophobic drug model and successfully encapsulate into the mPECT-2 NPs via the same method at a high solid content. The encapsulation efficiency, cytotoxicity and in vitro release of PTX-loaded NPs are investigated. The results suggest that the behavior of the drug-loaded mPECT-2 NPs prepared at a solid content of 25 wt% is similar to that of NPs prepared at a solid content of 1 wt%, which indicate that increasing solid content of polymer has no negative effect on the properties of NPs dispersion in application. In summary, the freeze-dried NPs prepared from the high solid content dispersion (≤25 wt%) has a good redispersibility and exhibits great potential in cost control of preparing NPs dispersion used as drug delivery system.
authors.affiliation: a Department of Polymer Science and Technology , School of Chemical Engineering and Technology, Tianjin University , Tianjin 300072 , China.
authors.forename: Yuzhang
authors.initials: Y
authors.lastname: Xiang
authors.forename: Miao
authors.initials: M
authors.lastname: Xiao
authors.forename: Shangcong
authors.initials: S
authors.lastname: Han
authors.forename: Shuxin
authors.initials: S
authors.lastname: Xu
authors.forename: Yan
authors.initials: Y
authors.lastname: Cao
authors.forename: Zesheng
authors.initials: Z
authors.lastname: Lv
authors.forename: Jianfeng
authors.initials: J
authors.lastname: Liu
authors.forename: Jinjian
authors.initials: J
authors.lastname: Liu
authors.forename: Liandong
authors.initials: L
authors.lastname: Deng
authors.forename: Anjie
authors.initials: A
authors.lastname: Dong
mesh_terms: D000972:Antineoplastic Agents, Phytogenic / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D045744:Cell Line, Tumor; D002470:Cell Survival / Q000187:drug effects; D003692:Delayed-Action Preparations; D005612:Freeze Drying; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D046529:Microscopy, Electron, Transmission; D053769:Nanocapsules / Q000737:chemistry*; D050997:Nanomedicine / Q000379:methods; D017239:Paclitaxel / Q000737:chemistry*; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry; D011092:Polyethylene Glycols / Q000737:chemistry; D017550:Spectroscopy, Fourier Transform Infrared
chemical_list: D000972:Antineoplastic Agents, Phytogenic; D003692:Delayed-Action Preparations; D053769:Nanocapsules; D011091:Polyesters; D011092:Polyethylene Glycols; D017239:Paclitaxel
keywords: Keywords; freeze-dried nanoparticles; high solid content; nanoparticles; redispersibility