OBJECTIVE To prepare the self-assembled neurotoxin-loaded nanoparticles of core-shell type, and investigate its physicochemical properties and release behavior in vitro. METHODS The self-assembled neurotoxin-loaded nanoparticles of core-shell type were prepared with PEG-g-PECA by emulsion polymerization method. The orthogonal design was used to optimize the preparation technology. The transmission electron microscope(TEM) and Zeta sizer instrument were utilized to investigate the physicochemical properties of the nanoparticles, and the drug release behavior in PBS buffer at pH 7.4 and 6.8 in vitro were studied by dialysis method respectively. RESULTS The mean diameter of the nanoparticles were (89.6±8.9)nm with polydispersity index of (0.110±0.003). The entrapment efficiency was (58.43±0.62)%, and Zeta potential was (-38.81±0.47) mV. The in vitro release profiles of the nanoparticles in pH 7.4 and 6.8 PBS buffer were consistent with Weibull equation, lnln[1/(1-Q)]=0.474lnt-1.612 1,r=0.994 6 (pH 7.4) and lnln[1/(1-Q)]=0.351lnt–0.827 1, r=0.970 8 (pH 6.8) respectively. CONCLUSION PEG-g-PECA is suitable for preparation of self-assembled neurotoxin-loaded nanoparticles of core-shell type with high entrapment efficiency, stable properties and excellent drug sustained release behavior.
Key words
neurotoxin /
self-assembled nanoparticles of core-shell type /
poly(ethylene glycol)-g-polyethylcyanoacrylate block copolymer /
preparation /
in vitro release
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References
[1] CHEN R Z, WU X R. The analgesic effect of Neurotoxin from cobra(Naja naja) venom.[J]. Chin Pharm Bull(中国药理学通报),1988,4(2):113-116.
[2] DONG A J. Polyglycol grafted and modified cyanoacrylate copolymer and its prepn.China, 02148633.6 [P]. 2003-05-14.
[3] JIN Y G, LI T C, AI P, et al. Self-assembled drug delivery systems 1. Properties and in vitro/in vivo behavior of acyclovir self-assembled nanoparticles (SAN)[J]. Inter J Pharm,2006,309 (1-2):199-207.
[4] GAO K P, JIANG X G. Influence of particle size on transport of methotrexate across blood brain barrier by polysorbate 80-coated polybutylcyanoacrylate nanoparticles[J]. Inter J Pharm,2006,310(1-2):213-219.
[5] CHEN S, XU Y, XU F, et al. Separation and determination of amino acids by micellar electrokinetic chromatography coupling with novel multiphoton excited fluorescence detection[J]. J Chromatogr A,2007, 1162(2):149-153.
[6] MA J, DENG S H. Studies on preparation of rhG-CSF liposomes and its release behavior in vitro[J]. Chin Pharm J(中国药学杂志), 2008, 43(2):123-126.
[7] CHENG Q Y, FENG J, LI F Z. Brain delivery of neurotoxin-I-loaded nanoparticles through intranasal administration[J]. Acta Pharm Sin(药学学报), 2008,43(4):431-434.
[8] FONTANA G, LICCIARDI M, MANSUETO S, et al. Amoxicillin-loaded polyethylcyanoacrylate nanoparticles: influence of PEG coating on the particle size, drug release rate and phagocytic uptake[J]. Biomaterials,2001,22(21):2857-2865.
[9] YU Q, PAN S R, DU Z. Preparation and properties of self-assemble paclitaxel-loaded core-shell type nano-micelles[J]. Acta Pharm Sin(药学学报),2008,43(4):408-414.
[10] ZHANG Y T, DONG A J, DENG L D, et al. A new water-soluble nano-micelle formulation of paclitaxel loaded in amphiphilic block copolymer[J]. Chem Eng(化学工程), 2005,33(2):39-43.
[11] PONOS M, ATHANASSIOS I. Modeling in Biopharmaceutics, Pharmacokinetics, and Pharmacodynamics[M]. Vol 30. New York: Springer-Verlag,2005:23-27.
[12] LIU C G, FAN W W, CHEN X G, et al. Self-assembled nanoparticles based on linoleic-acid modified carboxymethyl- chitosan as carrier of adriamycin (ADR) [J]. Current Applied Physics,2007,7(Suppl1):125-129.
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