Stealth PEG-PHDCA niosomes: Effects of Chain Length of PEG and Particle Size on Niosomes Surface Properties, In Vitro Drug Release, Phagocytic Uptake, In Vivo Pharmacokinetics and Antitumor Activity

尼奥体 PEG比率 药理学 药代动力学 体内 体外 粒径 化学 药品 400号桩 脂质体 色谱法 聚乙二醇 小泡 医学 生物化学 生物 经济 生物技术 物理化学 财务
作者
Bin Shi,Chao Fang,Yuanying Pei
出处
期刊:Journal of Pharmaceutical Sciences [Elsevier]
卷期号:95 (9): 1873-1887 被引量:96
标识
DOI:10.1002/jps.20491
摘要

A series of novel niosomes with the amphiphilic copolymer of poly (methoxy-polyethyleneglycol cyanoacrylate-co-n-hexadecyl cyanoacrylate) (PEG-PHDCA) acted as surface modification materials were prepared and Hydroxycamptothecin (HCPT) was used as a model drug. This work concentrated on the effects of PEG chain length and particle sizes on the niosomes surface properties, in vitro drug release, phagocytic uptake, in vivo pharmacokinetics and antitumor activity. Within the range of PEG Mw from 2000 to 10000, the increasing zeta potential (from −16.08 to −5.25 mv) and thicker fixed aqueous layer (3.82 to 5.78 nm) would facilitate the niosomes' stealth effects, while the reduced PEG chain density (from 0.53 to 0.17 PEG/nm2) and the quickened speed of drug release would diminish the effects. As a result, the PEG5000-PHDCA niosomes had the least phagocytic uptake, the longest half-life of 11.46 h and the best tumor inhibition rate of 97.1%. In the groups different in particle size (PEG5000-PHDCA niosomes from 92.5 to 204.6 nm), the bigger particles could be uptaken by macrophages more quickly, regardless of the changes of other physicochemical parameters. Correspondingly, PEG5000-PHDCA niosomes with particle sizes of 92.5, 144.2, 204.6 nm could extend the half-life of HCPT to 11.46, 6.33, 4.46 h, respectively. At last, the tumor inhibition rate of PEG5000-PHDCA niosomes (92.5 nm) at a dose of 2 mg/kg was five times that of HCPT injection at 4 mg/kg.The stealth effects of the PEG-PHDCA niosomes and the enhanced stability of lactone form of HCPT were accountable for the powerful antitumor effects of niosomes.
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