Physicochemical characterisation of cationic polybutylcyanoacrylat-nanoparticles by fluorescence correlation spectroscopy

Weyermann, Jörg; Lochmann, Dirk; Georgens, Christiane; Rais, Isam; Kreuter, Jörg; Karas, Michael; Wolkenhauer, Markus; Zimmer, Andreas

doi:10.1016/j.ejpb.2004.02.011

Cited by 16 publications

(8 citation statements)

References 28 publications

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“…The improved activity of drug-loaded NPs presented here highlights the relevance of this class of delivery system for leishmaniases. The PBCA-NFOH-NPs z-average (151.5 ± 61.97 nm) was similar to those obtained by Weyermann et al and Sommerfeld et al [13,14], who reported a z-average equal to 130-140 nm and 164-326 nm, respectively. The size of the NP determines its targeting abilities such as cell uptake.…”

Section: Discussionsupporting

confidence: 89%

Targeting Leishmania amazonensis amastigotes through macrophage internalisation of a hydroxymethylnitrofurazone nanostructured polymeric system

Monteiro

Löbenberg

Ferreira

et al. 2017

International Journal of Antimicrobial Agents

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Dextran-coated poly (n-butyl cyanoacrylate) nanoparticles (PBCA-NPs) were prepared and were evaluated for enhanced delivery of a promising anti-Leishmania drug candidate, hydroxymethylnitrofurazone (NFOH), to phagocytic cells. Currently available chemotherapy for leishmaniasis, such as pentavalent antimonials, presents low safety and efficacy. Furthermore, widespread drug resistance in leishmaniasis is rapidly emerging. To overcome these drawbacks, the use of nanosized delivery systems can reduce systemic drug toxicity and increase the drug concentration in infected macrophages, therefore improving treatment of leishmaniasis. PBCA-NPs containing NFOH (PBCA-NFOH-NPs) were prepared by an anionic emulsion polymerisation method. The z-average and polydispersity index (PDI) were determined by photon correlation spectroscopy, the zeta potential by microelectrophoresis and the entrapment efficiency by HPLC. Cytotoxicity was determined using macrophages from BALB/c mice. Efficacy tests were performed using Leishmania amazonensis promastigotes and amastigotes. The z-average of PBCA-NFOH-NPs was 151.5 ± 61.97 nm, with a PDI of 0.104 ± 0.01, a zeta potential of -10.1 ± 6.49 mV and an entrapment efficiency of 64.47 ± 0.43%. Efficacy in amastigotes revealed IC values of 0.33 µM and 31.2 µM for the nanostructured and free NFOH, respectively (95-fold increase). The cytotoxicity study indicated low toxicity of the PBCA-NFOH-NPs to macrophages. The selectivity index was 370.6, which is 49-fold higher than free NFOH (7.6). Such findings indicated that improved efficacy could be due to NP internalisation following site-specific drug delivery and reactivation of immune protective reactions by the NP components. Thus, PBCA-NFOH-NPs have the potential to significantly improve the treatment of leishmaniasis, with reduced systemic side effects.

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Section: Discussionsupporting

confidence: 89%

Targeting Leishmania amazonensis amastigotes through macrophage internalisation of a hydroxymethylnitrofurazone nanostructured polymeric system

Monteiro

Löbenberg

Ferreira

et al. 2017

International Journal of Antimicrobial Agents

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“…Many equipment designed for DLS may also have an attachment for electrophoretic light scattering to measure the zeta-potential important for colloids stability. An interesting variation of DLS is the fluorescence correlation spectroscopy (FCS) (102). FCS is a well-established technique to determine diffusion coefficient, size and mass of particles, as well as to characterize the binding of low molecular weight ligands to larger receptor molecules in solution.…”

Section: Dynamic Light Scattering (Dls)mentioning

confidence: 99%

Particle Size Analysis in Pharmaceutics: Principles, Methods and Applications

et al. 2006

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Physicochemical and biopharmaceutical properties of drug substances and dosage forms can be highly affected by the particle size, a critical process parameter in pharmaceutical production. The fundamental issue with particle size analysis is the variety of equivalent particle diameters generated by different methods, which is largely ascribable to the particle shape and particle dispersion mechanism involved. Thus, to enable selection of the most appropriate or optimal sizing technique, cross-correlation between different techniques may be required. This review offers an in-depth discussion on particle size analysis pertaining to specific pharmaceutical applications and regulatory aspects, fundamental principles and terminology, instrumentation types, data presentation and interpretation, in-line and process analytical technology. For illustration purposes, special consideration is given to the analysis of aerosols using time-of-flight and cascade impactor measurements, which is supported by a computational analysis conducted for this review.

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“…Due to its very high sensitivity and selectivity 13 the FCS technique has found numerous applications in fields ranging from cell biology 14,15 to polymer, colloid, and interface science 16–20 . FCS is perfectly suited for studying the formation of NCs 21,22 , their drug loading 23,24 , stability 25–27 , interactions with plasma proteins 28–32 and triggered release 33,34 . However, FCS has so far never been adapted to in situ blood measurements.…”

Section: Introductionmentioning

confidence: 99%

Monitoring drug nanocarriers in human blood by near-infrared fluorescence correlation spectroscopy

et al. 2018

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Nanocarrier-based drug delivery is a promising therapeutic approach that offers unique possibilities for the treatment of various diseases. However, inside the blood stream, nanocarriers’ properties may change significantly due to interactions with proteins, aggregation, decomposition or premature loss of cargo. Thus, a method for precise, in situ characterization of drug nanocarriers in blood is needed. Here we show how the fluorescence correlation spectroscopy that is a well-established method for measuring the size, loading efficiency and stability of drug nanocarriers in aqueous solutions can be used to directly characterize drug nanocarriers in flowing blood. As the blood is not transparent for visible light and densely crowded with cells, we label the nanocarriers or their cargo with near-infrared fluorescent dyes and fit the experimental autocorrelation functions with an analytical model accounting for the presence of blood cells. The developed methodology contributes towards quantitative understanding of the in vivo behavior of nanocarrier-based therapeutics.

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Physicochemical characterisation of cationic polybutylcyanoacrylat-nanoparticles by fluorescence correlation spectroscopy

Cited by 16 publications

References 28 publications

Targeting Leishmania amazonensis amastigotes through macrophage internalisation of a hydroxymethylnitrofurazone nanostructured polymeric system

Targeting Leishmania amazonensis amastigotes through macrophage internalisation of a hydroxymethylnitrofurazone nanostructured polymeric system

Particle Size Analysis in Pharmaceutics: Principles, Methods and Applications

Monitoring drug nanocarriers in human blood by near-infrared fluorescence correlation spectroscopy

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