Hemocompatibility of poly(ε-caprolactone) lipid-core nanocapsules stabilized with polysorbate 80-lecithin and uncoated or coated with chitosan

被引:146
作者
Bender, Eduardo A. [2 ]
Adorne, Marcia D. [1 ]
Colome, Leticia M. [2 ]
Abdalla, Dulcineia S. P. [3 ]
Guterres, Silvia S. [2 ,4 ]
Pohlmann, Adriana R. [1 ,2 ,4 ]
机构
[1] Univ Fed Rio Grande do Sul, Inst Quim, Dept Quim Organ, BR-91501970 Porto Alegre, RS, Brazil
[2] Univ Fed Rio Grande do Sul, Fac Farm, Programa Pos Grad Ciencias Farmaceut, BR-90610000 Porto Alegre, RS, Brazil
[3] Univ Sao Paulo, Fac Ciencias Farmaceut, BR-05508900 Sao Paulo, Brazil
[4] Univ Fed Rio Grande do Sul, Ctr Nanociencia & Nanotecnol, CNANO UFRGS, BR-91501970 Porto Alegre, RS, Brazil
关键词
Hemocompatibility; Polymeric nanoparticles; Lipid-core nanocapsules; Polysorbate; 80; Lecithin; Chitosan; PHYSICOCHEMICAL PROPERTIES; NANOPARTICLES; NANOCARRIERS; DELIVERY; SYSTEMS; PROFILES; RELEASE; RATS; SIZE;
D O I
10.1016/j.ijpharm.2012.01.051
中图分类号
R9 [药学];
学科分类号
100702 [药剂学];
摘要
The hemocompatibility of nanoparticles is of critical importance for their systemic administration as drug delivery systems. Formulations of lipid-core nanocapsules, stabilized with polysorbate 80-lecithin and uncoated or coated with chitosan (LNC and LNC-CS), were prepared and characterized by laser diffraction (D[4,3]: 129 and 134 nm), dynamic light scattering (119 nm and 133 nm), nanoparticle tracking (D50: 124 and 139 nm) and particle mobility (zeta potential: -15.1 mV and + 9.3 mV) analysis. In vitro hemocompatibility studies were carried out with mixtures of nanocapsule suspensions in human blood at 2% and 10% (v/v). The prothrombin time showed no significant change independently of the nanocapsule surface potential or its concentration in plasma. Regarding the activated partial thromboplastin time, both suspensions at 2% (v/v) in plasma did not influence the clotting time. Even though suspensions at 10% (v/v) in plasma decreased the clotting times (p < 0.05), the values were within the normal range. The ability of plasma to activate the coagulation system was maintained after the addition of the formulations. Suspensions at 2% (v/v) in blood showed no significant hemolysis or platelet aggregation. In conclusion, the lipid-core nanocapsules uncoated or coated with chitosan are hemocompatible representing a potential innovative nanotechnological formulation for intravenous administration. (C) 2012 Elsevier B. V. All rights reserved.
引用
收藏
页码:271 / 279
页数:9
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