In vitro toxicity assessment of oral nanocarriers

Ciappellano, Silvia Gabriella; Tedesco, Erik; Venturini, M.; Benetti, Federico

doi:10.1016/j.addr.2016.08.007

Cited by 53 publications

(25 citation statements)

References 306 publications

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“…When the drug is loaded within any nano-formulation, which evaluates its optical properties, these hinder the light scattering ability of drug. Moreover, due to these nanomaterials, there is decreased emission of fluorescent probes leading to false optical measurement (Dhawan and Sharma, 2010;Dobrovolskaia et al, 2010;Powell et al, 2010;Ciappellano et al, 2016). Consequently, these problems can be solved by just removing the nanomaterial before reading the nanomedicine into the optical analyzer (Ahamed, 2011;Oostingh et al, 2011;Kroll et al, 2012;Costa et al, 2016).…”

Section: Characterization Of Nanomaterialsmentioning

confidence: 99%

“…The two most desired properties required for the evaluation of any successful nanomaterial is its efficacy and safety (Ciappellano et al, 2016). Nanomedicines are formulated to achieve specific objectives such as: 1) Solubility enhancement of hydrophobic drugs.…”

Section: Introductionmentioning

confidence: 99%

“…In this review, the challenges associated with formulation, characterization and drug delivery of nanomedicines have been discussed. The future directions to be followed to make these nanomedicines safe and effective have also been reviewed (Ciappellano et al, 2016).…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

Nanomedicines: Challenges and perspectives for future nanotechnology in the healthcare system

AJAZUDDIN¹,

Siddique²,

Alexander³

et al. 2019

Sci. Res. Essays

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A novel approach of combining nanotechnology to the pharmaceutical and biotechnological field resulted in the formation of nanomedicines. Nanomedicines have progressed to a more considerable extent for curing irremediable diseases such as neurological defects, cardiovascular defects, etc., because of its minute size which assists in increased surface area and hence a remarkable dissolution profile. In addition to the health care sector, modernization of nanotechnology has also been implemented in other industries like cosmetics, electronics, catalysis, and chemical industries. Nanoparticles can be made by using polymers, either lipids or inorganic compounds like metals. They can be prepared by using either top to bottom or bottom to top approach. Interestingly, polymeric nanoparticles have provided an enormous opportunity to alter the surface of the nanoparticles leading to better drug delivery and drug targeting. However, these have the potential to induce toxicity as well. Also, the toxicity profile still has to be investigated. Moreover, characterization of the nanomedicines is always trouble, which has created a gap between conventional drugs and nanomedicines.

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Section: Characterization Of Nanomaterialsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Nanomedicines: Challenges and perspectives for future nanotechnology in the healthcare system

AJAZUDDIN¹,

Siddique²,

Alexander³

et al. 2019

Sci. Res. Essays

View full text Add to dashboard Cite

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“…Additionally, evaluation of cell toxicity is also important, as the unique physicochemical characteristics of nanomaterials and their high reactivity can reflect on their toxicity (Ciappellano et al 2016). A common assay to evaluate cytotoxicity is the study of cell viability (Doktorovova et al 2014), which consists of an in vitro cell culture approach (Loh et al 2010).…”

Section: Introductionmentioning

confidence: 99%

β-carotene and α-tocopherol coencapsulated in nanostructured lipid carriers of murumuru (Astrocaryum murumuru) butter produced by phase inversion temperature method: characterisation, dynamicin vitrodigestion and cell viability study

Gomes

Sola

Rochetti

et al. 2019

Journal of Microencapsulation

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Hydrophobic bioactives can be more easily incorporated into food and have their bioavailability enhanced if nanostructured lipid carriers (NLC) are used as carriers. In the present study, betacarotene-loaded NLC were produced by low emulsification using murumuru butter and a mixture of Span 80 and Cremophor RH40 as surfactants. Their average diameter was 35 nm and alpha-tocopherol was required to protect the encapsulated b-carotene. Besides the evaluation of their physicochemical stability, NLC were submitted to dynamic in vitro digestion and cell viability assays with Caco-2 and HEPG cells. The bioaccessibility of beta-carotene in the dynamic system was about 42%. Regarding cell viability, results indicated NLC were toxic to the cell cultures tested. Such high toxicity is probably related to the type of surfactant used and to the extremely reduced particle size, which may have led to an intense and fast permeation of the NLC through the cells. ARTICLE HISTORY

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“…Both undifferentiated and differentiated Caco-2 models have been developed, with the undifferentiated being more susceptible than the differentiated and, therefore, effective in cytotoxicity and cytoprotective studies [4][5][6][7][8]. More complex differentiated models are suitable for studying transport mechanisms and efficacy of substances [9][10][11][12]. Focusing on the relevance of Caco-2 in the design, optimization, and selection of potential candidates in the development of oral drugs, cell monolayer lines have been used for the study of improving the oral absorption of highly lipophilic and poorly water-soluble drugs [13]; lipid-based self-emulsifying drug delivery systems [14]; and for the evaluation of new oral formulations based on nanotechnology, such as solid lipid nanoparticles (SLNps) [15], or bioadhesive drug delivery systems, such as chitosan-modified nanoparticles [10].…”

Section: Introductionmentioning

confidence: 99%

Validation of an Ex Vivo Permeation Method for the Intestinal Permeability of Different BCS Drugs and Its Correlation with Caco-2 In Vitro Experiments

et al. 2019

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The absorption study of drugs through different biological membranes constitutes an essential step in the development of new pharmaceutical dosage forms. Concerning orally administered forms, methods based on monolayer cell culture of Caco-2 (Caucasian colon adenocarcinoma) have been developed to emulate intestinal mucosa in permeability studies. Although it is widely accepted, it has disadvantages, such as high costs or high technical complexity, and limitations related to the simplified structure of the monolayer or the class of molecules that can be permeated according to the transport mechanisms. The aim of this work was to develop a new ex vivo methodology which allows the evaluation of the intestinal apparent permeability coefficient (Papp) while using fewer resources and to assess the correlation with Caco-2. To this end, pig (Sus scrofa) duodenum segments were mounted in Franz diffusion cells and used to permeate four different drugs: ketorolac tromethamine (Kt), melatonin (Mel), hydrochlorothiazide (Htz), and furosemide (Fur). No statistically significant differences (p > 0.05) were observed corelating Papp values from Franz diffusion cells and Caco-2 cell experiments for Kt, Htz, and Fur. However, there were statistically significant differences (p < 0.05) correlating Papp values and Mel. The difference is explained by the role of Mel in the duodenal epithelial paracellular permeability reduction. Ex vivo permeation may be an equivalent method to Caco-2 for drugs that do not produce intestinal membrane phenomena that could affect absorption.

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In vitro toxicity assessment of oral nanocarriers

Cited by 53 publications

References 306 publications

Nanomedicines: Challenges and perspectives for future nanotechnology in the healthcare system

Nanomedicines: Challenges and perspectives for future nanotechnology in the healthcare system

β-carotene and α-tocopherol coencapsulated in nanostructured lipid carriers of murumuru (Astrocaryum murumuru) butter produced by phase inversion temperature method: characterisation, dynamicin vitrodigestion and cell viability study

Validation of an Ex Vivo Permeation Method for the Intestinal Permeability of Different BCS Drugs and Its Correlation with Caco-2 In Vitro Experiments

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