title: Optimizing particle size of docetaxel-loaded micelles for enhanced treatment of oral epidermoid carcinoma.
abstract: Understanding how the size of nanocarriers affects their fate in biological systems in vivo is of fundamental importance for rational design of drug delivery systems. In this study, five docetaxel (DTX)-loaded methoxy poly(ethylene glycol)-poly(lactide) micelles of different sizes (30-230nm) were prepared. It was observed that the permeation of micelles within both the multicellular tumor spheroids and tumor xenografts in mice was dependent on the size of the micelle. In addition, the size of micelles influenced their pharmacokinetic behavior. DTX-loaded pH-sensitive micelle based on poly(ethylene glycol)-poly(lactide)-poly(β-amino ester) (DTX-pHPM) was constructed to further illustrate the effect of particle size. As expected, DTX-pHPM improved tumor penetration, uptake by tumor cells, and prolonged circulation time, consequently demonstrating the highest inhibition of in vivo tumor growth (84.4%) in oral epidermoid carcinoma. Taken together, our findings can aid in designing nano-scale drug delivery systems for cancer therapy by optimizing the particle size.
authors.affiliation: College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, China.
authors.forename: Yang
authors.initials: Y
authors.lastname: Yu
authors.affiliation: Ministry of Education (MOE) Key Laboratory of Synthesis and Functionalization, Department of Polymer Science and Engineering, 5 Zhejiang University, Hangzhou, China. Electronic address: lyqiu@zju.edu.cn.
authors.forename: Liyan
authors.initials: L
authors.lastname: Qiu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000008:administration & dosage*; D002294:Carcinoma, Squamous Cell / Q000188:drug therapy*; D000077143:Docetaxel; D016503:Drug Delivery Systems; D006801:Humans; D051379:Mice; D008823:Micelles; D009062:Mouth Neoplasms / Q000188:drug therapy*; D010316:Particle Size; D011092:Polyethylene Glycols; D043823:Taxoids / Q000008:administration & dosage*
chemical_list: D000970:Antineoplastic Agents; D008823:Micelles; D043823:Taxoids; D000077143:Docetaxel; D011092:Polyethylene Glycols
keywords: Biodistribution; Docetaxel; Micelles; Particle size; Pharmacokinetics