Hemocompatibility of poly(ɛ-caprolactone) lipid-core nanocapsules stabilized with polysorbate 80-lecithin and uncoated or coated with chitosan.
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.
Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil.
Eduardo A
EA
Bender
Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, PBox 15003, Porto Alegre, 91501-970, RS, Brazil.
Márcia D
MD
Adorne
Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil.
Letícia M
LM
Colomé
Faculdade de Ciências Farmacêuticas, Universidade de São Paulo, Av. Professor Lineu Prestes, 580, bloco 17, São Paulo, 05508-900, SP, Brazil.
Dulcinéia S P
DSP
Abdalla
Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil; Centro de Nanociência e Nanotecnologia, CNANO-UFRGS, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil.
Sílvia S
SS
Guterres
Programa de Pós-Graduação em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal do Rio Grande do Sul, Av. Ipiranga, 2752, Porto Alegre, 90610-000, RS, Brazil; Departamento de Química Orgânica, Instituto de Química, Universidade Federal do Rio Grande do Sul, PBox 15003, Porto Alegre, 91501-970, RS, Brazil; Centro de Nanociência e Nanotecnologia, CNANO-UFRGS, Universidade Federal do Rio Grande do Sul, Av. Bento Gonçalves, 9500, Porto Alegre, 91501-970, RS, Brazil. Electronic address: pohlmann@iq.ufrgs.br.
Adriana R
AR
Pohlmann
D001672:Biocompatible Materials; D001777:Blood Coagulation / Q000187:drug effects; D002626:Chemistry, Pharmaceutical; D048271:Chitosan / Q000737:chemistry / Q000633:toxicity*; D004337:Drug Carriers; D004339:Drug Compounding; D004910:Erythrocyte Membrane / Q000187:drug effects; D006461:Hemolysis / Q000187:drug effects; D006801:Humans; D054709:Lecithins / Q000737:chemistry / Q000633:toxicity*; D008027:Light; D008055:Lipids / Q000737:chemistry / Q000633:toxicity*; D008422:Materials Testing; D053769:Nanocapsules; D036103:Nanotechnology; D010314:Partial Thromboplastin Time; D010316:Particle Size; D010974:Platelet Aggregation / Q000187:drug effects; D011091:Polyesters / Q000737:chemistry / Q000633:toxicity*; D011136:Polysorbates / Q000737:chemistry / Q000633:toxicity*; D011517:Prothrombin Time; D012542:Scattering, Radiation; D013678:Technology, Pharmaceutical / Q000379:methods
D001672:Biocompatible Materials; D004337:Drug Carriers; D054709:Lecithins; D008055:Lipids; D053769:Nanocapsules; D011091:Polyesters; D011136:Polysorbates; C016240:polycaprolactone; D048271:Chitosan