PMID- 28184163 OWN - NLM STAT- MEDLINE DCOM- 20170404 LR - 20220317 IS - 1178-2013 (Electronic) IS - 1176-9114 (Print) IS - 1176-9114 (Linking) VI - 12 DP - 2017 TI - Docetaxel-loaded PLGA and PLGA-PEG nanoparticles for intravenous application: pharmacokinetics and biodistribution profile. PG - 935-947 LID - 10.2147/IJN.S121881 [doi] AB - Docetaxel is a highly potent anticancer agent being used in a wide spectrum of cancer types. There are important matters of concern regarding the drug's pharmacokinetics related to the conventional formulation. Poly(lactide-co-glycolide) (PLGA) is a biocompatible/biodegradable polymer with variable physicochemical characteristics, and its application in human has been approved by the United States Food and Drug Administration. PLGA gives polymeric nanoparticles with unique drug delivery characteristics. The application of PLGA nanoparticles (NPs) as intravenous (IV) sustained-release delivery vehicles for docetaxel can favorably modify pharmacokinetics, biofate, and pharmacotherapy of the drug in cancer patients. Surface modification of PLGA NPs with poly(ethylene glycol) (PEG) can further enhance NPs' long-circulating properties. Herein, an optimized fabrication approach has been used for the preparation of PLGA and PLGA-PEG NPs loaded with docetaxel for IV application. Both types of NP formulations demonstrated in vitro characteristics that were considered suitable for IV administration (with long-circulating sustained-release purposes). NP formulations were IV administered to an animal model, and docetaxel's pharmacokinetic and biodistribution profiles were determined and compared between study groups. PLGA and PEGylated PLGA NPs were able to modify the pharmacokinetics and biodistribution of docetaxel. Accordingly, the mode of changes made to pharmacokinetics and biodistribution of docetaxel is attributed to the size and surface properties of NPs. NPs contributed to increased blood residence time of docetaxel fulfilling their role as long-circulating sustained-release drug delivery systems. Surface modification of NPs contributed to more pronounced docetaxel blood concentration, which confirms the role of PEG in conferring long-circulation properties to NPs. FAU - Rafiei, Pedram AU - Rafiei P AD - Division of Pharmacy, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, SK, Canada. FAU - Haddadi, Azita AU - Haddadi A AD - Division of Pharmacy, College of Pharmacy and Nutrition, University of Saskatchewan, Saskatoon, SK, Canada. LA - eng PT - Journal Article DEP - 20170127 PL - New Zealand TA - Int J Nanomedicine JT - International journal of nanomedicine JID - 101263847 RN - 0 (Antineoplastic Agents) RN - 0 (Drug Carriers) RN - 0 (Taxoids) RN - 0 (poly(lactic-glycolic acid)-poly(ethyleneglycol) copolymer) RN - 15H5577CQD (Docetaxel) RN - 1SIA8062RS (Polylactic Acid-Polyglycolic Acid Copolymer) RN - 26009-03-0 (Polyglycolic Acid) RN - 33X04XA5AT (Lactic Acid) RN - 34346-01-5 (Polyglactin 910) RN - 3WJQ0SDW1A (Polyethylene Glycols) SB - IM MH - Animals MH - Antineoplastic Agents/administration & dosage/blood/*pharmacokinetics MH - Chemistry, Pharmaceutical MH - Docetaxel MH - Drug Carriers/administration & dosage/*chemistry MH - *Drug Delivery Systems MH - Female MH - Humans MH - Lactic Acid/*chemistry MH - Mice MH - Mice, Inbred BALB C MH - Nanoparticles/*chemistry MH - Particle Size MH - Polyethylene Glycols/*chemistry MH - Polyglactin 910/*chemistry MH - Polyglycolic Acid/*chemistry MH - Polylactic Acid-Polyglycolic Acid Copolymer MH - Taxoids/administration & dosage/blood/*pharmacokinetics MH - Tissue Distribution PMC - PMC5291330 OTO - NOTNLM OT - biodistribution OT - docetaxel OT - emulsification solvent evaporation OT - pharmacokinetics OT - poly(lactide-co-glycolide) OT - poly(lactide-co-glycolide)-poly(ethylene glycol) OT - polymeric nanoparticles OT - sustained release COIS- The authors report no conflicts of interest in this work. EDAT- 2017/02/12 06:00 MHDA- 2017/04/05 06:00 PMCR- 2017/01/27 CRDT- 2017/02/11 06:00 PHST- 2017/02/11 06:00 [entrez] PHST- 2017/02/12 06:00 [pubmed] PHST- 2017/04/05 06:00 [medline] PHST- 2017/01/27 00:00 [pmc-release] AID - ijn-12-935 [pii] AID - 10.2147/IJN.S121881 [doi] PST - epublish SO - Int J Nanomedicine. 2017 Jan 27;12:935-947. doi: 10.2147/IJN.S121881. eCollection 2017.