Liquid formulation containing doxorubicin-loaded lipid-core nanocapsules: Cytotoxicity in human breast cancer cell line and in vitro uptake mechanism

Antonow, Michelli Barcelos; Asbahr, Ana Carolina Cavazzin; Raddatz, Paula; Beckenkamp, Aline; Buffon, Andréia; Guterres, Sílvia Stanisçuaski; Pohlmann, Adriana Raffin

doi:10.1016/j.msec.2017.03.099

Cited by 25 publications

(10 citation statements)

References 47 publications

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“…The number of nanoparticles can be expressed as the molar concentration of colloidal particles in the formulation 11 , and this allows the estimation of the number of excipient molecules that compose each individual particle 4 , two important parameters that represent a real advance in the structural elucidation of nanocolloids.…”

Section: Discussionmentioning

confidence: 99%

Use of nanoparticle concentration as a tool to understand the structural properties of colloids

Ribeiro

Couto

Fraceto

et al. 2018

Sci Rep

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Elucidation of the structural properties of colloids is paramount for a successful formulation. However, the intrinsic dynamism of colloidal systems makes their characterization a difficult task and, in particular, there is a lack of physicochemical techniques that can be correlated to their biological performance. Nanoparticle tracking analysis (NTA) allows measurements of size distribution and nanoparticle concentration in real time. Its analysis over time also enables the early detection of physical instability in the systems not assessed by subtle changes in size distribution. Nanoparticle concentration is a parameter with the potential to bridge the gap between in vitro characterization and biological performance of colloids, and therefore should be monitored in stability studies of formulations. To demonstrate this, we have followed two systems: extruded liposomes exposed to increasing CHCl3 concentrations, and solid lipid nanoparticles prepared with decreasing amounts of poloxamer 188. NTA and dynamic light scattering (DLS) were used to monitor changes in nanoparticle number and size, and to estimate the number of lipid components per particle. The results revealed a strong negative correlation between particle size (determined by DLS) and concentration (assessed by NTA) in diluted samples, which should be adopted to monitor nanocolloidal stability, especially in drug delivery.

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Section: Discussionmentioning

confidence: 99%

Use of nanoparticle concentration as a tool to understand the structural properties of colloids

Ribeiro

Couto

Fraceto

et al. 2018

Sci Rep

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“…Thus, a high therapeutic effect can be achieved with lower administration doses. Other studies have also shown that the association of antitumor drugs to carrier systems such as doxorubicin, bromelain and imiquimod, are able to significantly decrease the viability of tumor cells (MCF-7 and SiHa) compared to the free drug [ 72 , 73 , 74 ]. This reinforces the potentiality of formulations developed with a view to increase the therapeutic efficacy of the 5FU drug, with lower doses.…”

Section: Discussionmentioning

confidence: 99%

An Inhalable Powder Formulation Based on Micro- and Nanoparticles Containing 5-Fluorouracil for the Treatment of Metastatic Melanoma

Zatta

Frank

Reolon³

et al. 2018

Nanomaterials

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Melanoma is the most aggressive and lethal type of skin cancer, with a poor prognosis because of the potential for metastatic spread. The aim was to develop innovative powder formulations for the treatment of metastatic melanoma based on micro- and nanocarriers containing 5-fluorouracil (5FU) for pulmonary administration, aiming at local and systemic action. Therefore, two innovative inhalable powder formulations were produced by spray-drying using chondroitin sulfate as a structuring polymer: (a) 5FU nanoparticles obtained by piezoelectric atomization (5FU-NS) and (b) 5FU microparticles of the mucoadhesive agent Methocel™ F4M for sustained release produced by conventional spray drying (5FU-MS). The physicochemical and aerodynamic were evaluated in vitro for both systems, proving to be attractive for pulmonary delivery. The theoretical aerodynamic diameters obtained were 0.322 ± 0.07 µm (5FU-NS) and 1.138 ± 0.54 µm (5FU-MS). The fraction of respirable particles (FR%) were 76.84 ± 0.07% (5FU-NS) and 55.01 ± 2.91% (5FU-MS). The in vitro mucoadhesive properties exhibited significant adhesion efficiency in the presence of Methocel™ F4M. 5FU-MS and 5FU-NS were tested for their cytotoxic action on melanoma cancer cells (A2058 and A375) and both showed a cytotoxic effect similar to 5FU pure at concentrations of 4.3 and 1.7-fold lower, respectively.

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“…In the ideal scenario, lipid-based NPs can be prepared using a low energy process, do not require the use of organic solvent, and can be scaled up [90][91][92]. Thus, numerous lipophilic cytotoxic drugs have been encapsulated in lipid-based NPs, such as paclitaxel, etoposide, docetaxel, SN38, and doxorubicin; some drugs have been modified to be more lipophilic, such as carbonyl-grafted gemcitabine [93][94][95][96][97]. However, there are currently no lipid-based NPs either on the market or undergoing clinical trials.…”

Section: Lipid-based Nanoparticlesmentioning

confidence: 99%

Advances in treatment formulations for acute myeloid leukemia

Briot

Roger

Thépot

et al. 2018

Drug Discovery Today

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Acute myeloid leukemia (AML) is the most common cause of leukemia-related mortality. The combination of cytarabine and anthracycline has been the gold standard of treatment over the past 40 years, but the distribution of the drugs in the body leads to severe adverse effects. Poor prognosis of older patients with AML is the consequence not only of comorbidities, but also of chemoresistance resulting from frequent secondary AML. Numerous strategies using nanotechnologies are in development to improve drug targeting, pharmacokinetics, administration route, chemoresistance, and adverse effects generally observed. Among the four new drugs approved for AML by the US Food and Drug Administration (FDA) in 2017, Vyxeos is a novel liposomal formulation of historical AML drugs. Here, we review current AML treatments and discuss how the development of new formulations will change the therapeutic armamentarium.

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Liquid formulation containing doxorubicin-loaded lipid-core nanocapsules: Cytotoxicity in human breast cancer cell line and in vitro uptake mechanism

Cited by 25 publications

References 47 publications

Use of nanoparticle concentration as a tool to understand the structural properties of colloids

Use of nanoparticle concentration as a tool to understand the structural properties of colloids

An Inhalable Powder Formulation Based on Micro- and Nanoparticles Containing 5-Fluorouracil for the Treatment of Metastatic Melanoma

Advances in treatment formulations for acute myeloid leukemia

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