Oil-in-water nanoemulsions are suitable for carrying hydrophobic compounds: Indomethacin as a model of anti-inflammatory drug

Kwasigroch, Björn; Escribano, Elvira; Morán, María del Carmen; Queralt, Josep; Busquets, Montserrat; Estelrich, Joan

doi:10.1016/j.ijpharm.2016.11.016

Cited by 25 publications

(14 citation statements)

References 38 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…On the other hand, it is important to emphasize that the anti‐inflammatory activity of guayusa extracts was higher than that exhibited by acetylsalicylic acid and indomethacin, individually known for their anti‐inflammatory activity …”

Section: Resultsmentioning

confidence: 97%

Changes in phytochemical composition, bioactivity and in vitro digestibility of guayusa leaves (Ilex guayusa Loes.) in different ripening stages

et al. 2017

View full text Add to dashboard Cite

show abstract

Section: Resultsmentioning

confidence: 97%

Changes in phytochemical composition, bioactivity and in vitro digestibility of guayusa leaves (Ilex guayusa Loes.) in different ripening stages

et al. 2017

View full text Add to dashboard Cite

show abstract

“…Quantitative viability of the 3T3 and HeLa cells in the presence of MNPs was assessed using the MTT and NR assays, as described elsewhere. 58 The first measures metabolic activity in the mitochondria of viable cells, 59 whereas NR accumulates in the lysosomes of viable undamaged cells. 60 3T3 cells (1 × 10 5 cells mL –1 ) and HeLa cells (5 × 10 4 cells mL –1 ) were seeded onto a 96-well plate in 100 μL of complete medium.…”

Section: Discussionmentioning

confidence: 99%

Effect of PEGylation on Ligand-Targeted Magnetoliposomes: A Missed Goal

Estelrich¹,

Busquets

Morán

2017

ACS Omega

Self Cite

View full text Add to dashboard Cite

We tested the targeting efficiency of magnetoliposomes (MLPs) labeled with tripeptide arginine-glycine-aspartic acid (RGD) on two types of cells: HeLa cells expressing RGD receptors and 3T3 cells lacking RGD receptors. The targeting ability of RGD-MLPs was compared to that of bare MLPs and MLPs stabilized with poly(ethylene glycol) (PEG). Cellular internalization of these liposomes was determined by flow cytometry and confocal microscopy, which showed that both types of cells took up more nontargeting MLPs than targeting RGD-MLPs or PEG-MLPs, with PEG-MLPs showing the lowest degree of internalization. The presence of specific receptors on HeLa cells did not facilitate the binding of RGD-MLPs, probably due to the presence of PEG chains on the liposomal surface. The polymer increases the circulation time of the liposomes in the organism but reduces their interactions with cells. Despite the localization of the RGD peptide on the tip of PEG in RGD-MLPs, the interaction between the liposome and cell was still limited. To avoid this drawback, targeting drug delivery systems can be prepared with two types of PEG: one of a short length to enable biocompatibility and the other of a longer chain to carry the ligand.

show abstract

“…This makes nanoemulsions an attractive candidate for study using QbD approaches that include mixture process variable design of experiments. Nanoemulsions are also promising carriers for anti-inflammatory drugs and/or natural products (9)(10)(11) and potential future pain nanomedicines. Non-steroidal anti-inflammatory drugs (NSAIDs) are commonly prescribed to treat pain, as these drugs are non-addictive alternatives to opioids.…”

Section: Electronic Supplementary Materialsmentioning

confidence: 99%

Development of Theranostic Perfluorocarbon Nanoemulsions as a Model Non-Opioid Pain Nanomedicine Using a Quality by Design (QbD) Approach

et al. 2019

View full text Add to dashboard Cite

Pain nanomedicine is an emerging field in response to current needs of addressing the opioid crisis in the USA and around the world. Our group has focused on the development of macrophage-targeted perfluorocarbon nanoemulsions as inflammatory pain nanomedicines over the past several years. We present here, for the first time, a quality by design approach used to design pain nanomedicine. Specifically, we used failure mode, effects, and criticality analysis (FMECA) which identified the process and composition parameters that were most likely to impact nanoemulsion critical quality attributes (CQAs). From here, we applied a unique combination approach that compared multiple linear regression, boosted decision tree regression, and partial least squares regression methods in combination with correlation plots. The presented combination approach allowed for indepth analyses of which formulation steps in the nanoemulsification processes control nanoemulsion droplet diameter, stability, and drug loading. We identified that increase in solubilizer (transcutol) content increased drug loading and decreased nanoemulsion stability. This was mitigated by inclusion of perfluorocarbon oil in the internal phase. We observed negative correlation (R 2 = 0.4357, p value 0.0054) between the amount of PCE and the percent diameter increase (destabilization), and no correlation between processing parameters and percent diameter increase over time. Further, we identified that increased sonication time decreases nanoemulsion drug loading but does not significantly impact droplet diameter or stability. We believe the methods presented here can be useful in the development of various nanomedicines to produce higher-quality products with enhanced manufacturing and design control.

show abstract

Oil-in-water nanoemulsions are suitable for carrying hydrophobic compounds: Indomethacin as a model of anti-inflammatory drug

Cited by 25 publications

References 38 publications

Changes in phytochemical composition, bioactivity and in vitro digestibility of guayusa leaves (Ilex guayusa Loes.) in different ripening stages

Changes in phytochemical composition, bioactivity and in vitro digestibility of guayusa leaves (Ilex guayusa Loes.) in different ripening stages

Effect of PEGylation on Ligand-Targeted Magnetoliposomes: A Missed Goal

Development of Theranostic Perfluorocarbon Nanoemulsions as a Model Non-Opioid Pain Nanomedicine Using a Quality by Design (QbD) Approach

Contact Info

Product

Resources

About