title: Development of a 5-fluorouracil-loaded PLGA microsphere delivery system by a solid-in-oil-in-hydrophilic oil (S/O/hO) novel method for the treatment of tumors.
abstract: Tumor treatment requires a long-term regimen of chemotherapy, and both surgical tumor resection and radiation therapy are also used. The present study aimed to develop a novel method for 5-fluorouracil (5-FU)-loaded microspheres which enhance the therapeutic effects of chemotherapy, the quality of life of patients and reduce chemotherapy systemic side-effects. The preparation of a 5-FU microsphere delivery system by a solid-in-oil-in-hydrophilic oil (S/O/hO) novel method was carried out and then in vitro and in vivo evaluation of the 5-FU-microsphere delivery system was conducted. The 5-FU microsphere delivery system prepared had sustained-release function and achieved local treatment efficacy for tumors. The encapsulation efficiency of the 5-FU microsphere delivery system was >90% [better than the fabrication method using water-in-oil-in-water (W/O/W)]. The drug release profile from the 5-FU-loaded sustained-release microsphere delivery system matched the pseudo zero-order equation for 30 days in vitro. The plasma concentration of 5-FU was higher than the water solution by subcutaneous injection. The tumor growth rate of rabbits using the 5-FU microsphere delivery system was much lower than the rate in rabbit using a subcutaneous injection of 5-FU water solution. The 5-FU-loaded sustained-release microspheres using the novel method (S/O/hO) is a potential and effective method with which to inhibit tumor growth.
authors.affiliation: Shanghai Tenth People's Hospital, Shanghai 200072, P.R. China.
authors.forename: Qing
authors.initials: Q
authors.lastname: Lin
authors.affiliation: School of Pharmacy, Shanghai JiaoTong University, Shanghai 200240, P.R. China.
authors.forename: Yunpeng
authors.initials: Y
authors.lastname: Cai
authors.affiliation: School of Pharmacy, Shanghai JiaoTong University, Shanghai 200240, P.R. China.
authors.forename: Minglu
authors.initials: M
authors.lastname: Yuan
authors.affiliation: School of Pharmacy, Shanghai JiaoTong University, Shanghai 200240, P.R. China.
authors.forename: Lin
authors.initials: L
authors.lastname: Ma
authors.affiliation: School of Pharmacy, Shanghai JiaoTong University, Shanghai 200240, P.R. China.
authors.forename: Mingfeng
authors.initials: M
authors.lastname: Qiu
authors.affiliation: School of Pharmacy, Shanghai JiaoTong University, Shanghai 200240, P.R. China.
authors.forename: Jing
authors.initials: J
authors.lastname: Su
mesh_terms: D000818:Animals; D000964:Antimetabolites, Antineoplastic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D003692:Delayed-Action Preparations; D004339:Drug Compounding; D016503:Drug Delivery Systems; D005472:Fluorouracil / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D057927:Hydrophobic and Hydrophilic Interactions; D007700:Kinetics; D008863:Microspheres; D009369:Neoplasms / Q000188:drug therapy* / Q000473:pathology; D011817:Rabbits; D047368:Tumor Burden / Q000187:drug effects; D023041:Xenograft Model Antitumor Assays
chemical_list: D000964:Antimetabolites, Antineoplastic; D003692:Delayed-Action Preparations; D005472:Fluorouracil