Precise engineering of dapivirine-loaded nanoparticles for the development of anti-HIV vaginal microbicides

Neves, José das; Sarmento, Bruno

doi:10.1016/j.actbio.2015.02.007

Cited by 66 publications

(40 citation statements)

References 63 publications

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“…Higher emulsifier-tolipid ratio may promote formation of smaller particles and provide higher stabilisation of nanosystem because of the reduction in interfacial tension between the lipid matrix and the hydrophilic phase [31]. The results showed that as liquid lipid-to-solid lipid ratio increased, particle size decreased from 175.39 nm (Formulation (6)) to 96.93 nm (Formulation (8)), which can be attributed to the increased amount of solid lipids that tend to facilitate the aggregation of particles.…”

Section: Formulation Optimisation Of Nob-nlcmentioning

confidence: 99%

Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

Huang

Dou

et al. 2017

Journal of Nanomaterials

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The objective of this manuscript was to investigate and optimise the potential of nanostructured lipid carriers (NLCs) as a carrier system for nobiletin (NOB), which was prepared by high-pressure homogenisation method. Additionally, this study was focused on the application of NOB-loaded NLC (NOB-NLC) in functional food. Response surface method with a three-level Box-Behnken design was validated through analysis of variance, and the robustness of the design was confirmed through the correspondence between the values measured in the experiments and the predicted ones. Properties of the prepared NOB-NLC, such asaverage, polydispersity, entrapment efficiency, zeta potential, morphology, and crystallinity, were investigated. NOB-NLC exhibited a spherical shape with a diameter of 112.27 ± 5.33 nm, zeta potential of −35.1 ± 2.94 mV, a polydispersity index of 0.251 ± 0.058, and an EE of 81.06% ± 6.02%. Results from X-ray diffraction and differential scanning calorimetry of NOB-NLC reviewed that the NOB crystal might be converted to an amorphous state. Fourier transform infrared spectroscopic analysis demonstrated that chemical interaction was absent between the compound and lipid mixture in NOB-NLC.

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Section: Formulation Optimisation Of Nob-nlcmentioning

confidence: 99%

Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

Huang

Dou

et al. 2017

Journal of Nanomaterials

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“…It is already known that higher amounts of surfactant may promote formation and stabilization of smaller particles due to the decrease in interfacial tension between the lipid and the aqueous phase 51 and, consequently, controls the aggregation of lipid particle. 45 …”

Section: Effect Of the Amount Of Drugmentioning

confidence: 99%

“…Also, the Box-Behnken design requires the performance of a minimum number of experiments when three factors are considered, as compared to others, namely, the central composite design. 51 The Box-Behnken experimental design allowed us to obtain 13 different formulations, with a triplication of the central point, resulting in a total of 15 formulations. The replication of the central point enables to estimate the experimental error.…”

Section: Experimental Designmentioning

confidence: 99%

“…Nonlinearity between factors and responses is also suggested, that is, the variance of one factor can produce a different degree of response at different levels or more than one factor is varied. 8,51,52 The polynomial equations were statistically validated using ANOVA and were considered statistically significant when F was higher than F critic for all responses. Results of the statistical analysis are summarized in Table 4.…”

Section: Experimental Designmentioning

confidence: 99%

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Design and statistical modeling of mannose-decorated dapsone-containing nanoparticles as a strategy of targeting intestinal M-cells

Vieira¹,

Chaves²,

Pinheiro³

et al. 2016

IJN

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The aim of the present work was to develop and optimize surface-functionalized solid lipid nanoparticles (SLNs) for improvement of the therapeutic index of dapsone (DAP), with the application of a design of experiments. The formulation was designed to target intestinal microfold (M-cells) as a strategy to increase internalization of the drug by the infected macrophages. DAP-loaded SLNs and mannosylated SLNs (M-SLNs) were successfully developed by hot ultrasonication method employing a three-level, three-factor Box–Behnken design, after the preformulation study was carried out with different lipids. All the formulations were systematically characterized regarding their diameter, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency, and loading capacity. They were also subjected to morphological studies using transmission electron microscopy, in vitro release study, infrared analysis (Fourier transform infrared spectroscopy), calorimetry studies (differential scanning calorimetry), and stability studies. The diameter of SLNs, SLN-DAP, M-SLNs, and M-SLN-DAP was approximately 300 nm and the obtained PDI was <0.2, confirming uniform populations. Entrapment efficiency and loading capacity were approximately 50% and 12%, respectively. Transmission electron microscopy showed spherical shape and nonaggregated nanoparticles. Fourier transform infrared spectroscopy was used to confirm the success of mannose coating process though Schiff’s base formation. The variation of the ZP between uncoated (approximately −30 mV) and mannosylated formulations (approximately +60 mV) also confirmed the successful coating process. A decrease in the enthalpy and broadening of the lipid melting peaks of the differential scanning calorimetry thermograms are consistent with the nanostructure of the SLNs. Moreover, the drug release was pH-sensitive, with a faster drug release at acidic pH than at neutral pH. Storage stability for the formulations for at least 8 weeks is expected, since they maintain the original characteristics of diameter, PDI, and ZP. These results pose a strong argument that the developed formulations can be explored as a promising carrier for treating leprosy with an innovative approach to target DAP directly to M-cells.

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“…products able to circumvent local male-to-female viral transmission events upon sexual intercourse, namely those based on nanotechnology [142]. We recently proposed the incorporation of a mucus-like fluid in either HEC-1-A or CaSki cell monolayers in order to better understand the effects of such additional barrier in the permeation and epithelial accumulation of the candidate microbicide drug dapivirine [143]. The aqueous fluid was modified from Owen & Katz [103] and contained 1.5% (w/v) pig gastric mucin type II, 0.5% (w/v) glucose, 0.351% (w/v) sodium chloride, 0.2% (w/v) lactic acid, 0.14% (w/v) potassium hydroxide, 0.1% (w/v) acetic acid, 0.04% (w/v) urea, 0.0222% (w/v) calcium hydroxide, 0.016% (w/v) glycerol and enough amount hydrochloride acid for pH 4.2.…”

Section: Supplementation Of Cell-based Mucosal Models With Artificialmentioning

confidence: 99%

The role of mucus in cell-based models used to screen mucosal drug delivery

Lechanteur

Neves

Sarmento

2018

Advanced Drug Delivery Reviews

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The increasing interest in developing tools to predict drug absorption through mucosal surfaces is fostering the establishment of epithelial cell-based models. Cell-based in vitro techniques for drug permeability assessment are less laborious, cheaper and address the concerns of using laboratory animals. Simultaneously, in vitro barrier models that thoroughly simulate human epithelia or mucosae may provide useful data to speed up the entrance of new drugs and new drug products into the clinics. Nevertheless, standard cell-based in vitro models that intend to reproduce epithelial surfaces often discard the role of mucus in influencing drug permeation/absorption. Biomimetic models of mucosae in which mucus production has been considered may not be able to fully reproduce the amount and architecture of mucus, resulting in biased characterization of permeability/absorption. In these cases, artificial mucus may be used to supplement cell-based models but still proper identification and quantification are required. In this review, considerations regarding the relevance of mucus in the development of cell-based epithelial and mucosal models mimicking the gastro-intestinal tract, the cervico-vaginal tract and the respiratory tract, and the impact of mucus on the permeability mechanisms are addressed. From simple epithelial monolayers to more complex 3D structures, the impact of the presence of mucus for the extrapolation to the in vivo scenario is critically analyzed. Finally, an overview is provided on several techniques and methods to characterize the mucus layer over cell-based barriers, in order to intimately reproduce human mucosal layer and thereby, improve in vitro/in vivo correlation.

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Precise engineering of dapivirine-loaded nanoparticles for the development of anti-HIV vaginal microbicides

Cited by 66 publications

References 63 publications

Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

Preparation and Characterisation of Nobiletin-Loaded Nanostructured Lipid Carriers

Design and statistical modeling of mannose-decorated dapsone-containing nanoparticles as a strategy of targeting intestinal M-cells

The role of mucus in cell-based models used to screen mucosal drug delivery

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