Novel Findings about Double-Loaded Curcumin-in-HPβcyclodextrin-in Liposomes: Effects on the Lipid Bilayer and Drug Release

Fernández-Romero, Ana-María; Maestrelli, Francesca; Mura, Paola; Rabasco, A. M.; González-Rodrı́guez, Marı́a Luisa

doi:10.3390/pharmaceutics10040256

Cited by 37 publications

(26 citation statements)

References 68 publications

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“…This resulted in dilution of curcumin in the mixture and diminishing its characteristic peak. This was also reported by Fernández-Romero et al 83 Both the improved SD/P4 and SD/P6 displayed very broad peaks at 280.1°C and 293.6°C, respectively, which were reminiscent of the endothermic peaks of HPβCD, albeit with a shift to lower temperatures and very sharp decrease in intensity. The intensive reduction in dehydration peaks of HPβCD at 64.2°C and 65.1°C might be endorsed to the elimination of water during spray drying.…”

Section: Differential Scanning Calorimetry (Dsc)supporting

confidence: 84%

Design and Characterization of Spray-Dried Proliposomes for the Pulmonary Delivery of Curcumin

Adel

ElMeligy

Abdelrahim

et al. 2021

IJN

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Purpose The goal was to directly deliver curcumin, a natural polyphenolic anticancer and anti-inflammatory compound, to the lung tissues with minimal systemic exposure through the fabrication of proliposomes, overcoming its poor aqueous solubility and oral bioavailability. Methods Nano-spray drying was employed to prepare proliposomes using hydroxypropyl beta-cyclodextrin as a carrier. Lecithin and cholesterol were used as lipids, stearylamine and Poloxamer 188 were added as positive charge inducer and a surfactant, respectively. Different characterization parameters were evaluated like percentage yield, entrapment efficiency, drug loading, aerodynamic particle size, in vitro release besides morphological examination. Cytotoxicity studies on cell line A549 lung tumor cells as well as in vivo lung pharmacokinetic studies were also carried. Results The optimized formulations showed superior aerosolization properties coupled their enhanced ability to reach deep lung tissues with a high % of fine particle fraction. Cytotoxicity studies using MTT assay demonstrated enhanced growth inhibitory effect on lung tumor cells A549 and significant reduction of proinflammatory cytokines such as tumor necrosis factor-α, interleukin-6 and interleukin-10 compared to the pure drug. Results of lung pharmacokinetic tests confirmed the superiority of proliposomal curcumin over curcumin powder in both, the rate and extent of lung tissue absorption, as well as the mean residence time within the lung tissues. Conclusion The pulmonary delivery of curcumin-loaded proliposomes as dry powder provides a direct approach to lung tissues targeting while avoiding the limitations of the oral route and offering a non-invasive alternative to the parenteral one.

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Section: Differential Scanning Calorimetry (Dsc)supporting

confidence: 84%

Design and Characterization of Spray-Dried Proliposomes for the Pulmonary Delivery of Curcumin

Adel

ElMeligy

Abdelrahim

et al. 2021

IJN

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“…The presence of exotherms, which appear only in the aforementioned two samples (Fig. 6e,h), could be interpreted as the reorganization of quasi-solid aggregates (Cer is able to behave as a solid 55 and undergo some molecular rearrangements 56 ) which reportedly exhibit exotherms before endothermic transitions in DSC experiments for other highly hydrophobic non-lipid molecules such as curcumin 57 . However, these putative aggregates would only appear in the nSM-containing two-Cer samples, regardless of the presence or absence of lSM.…”

Section: Discussionmentioning

confidence: 91%

C24:0 and C24:1 sphingolipids in cholesterol-containing, five- and six-component lipid membranes

González-Ramírez

García-Arribas

Sot

et al. 2020

Sci Rep

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The biophysical properties of sphingolipids containing lignoceric (C24:0) or nervonic (C24:1) fatty acyl residues have been studied in multicomponent lipid bilayers containing cholesterol (Chol), by means of confocal microscopy, differential scanning calorimetry and atomic force microscopy. Lipid membranes composed of dioleoyl phosphatidylcholine and cholesterol were prepared, with the addition of different combinations of ceramides (C24:0 and/or C24:1) and sphingomyelins (C24:0 and/or C24:1). Results point to C24:0 sphingolipids, namely lignoceroyl sphingomyelin (lSM) and lignoceroyl ceramide (lCer), having higher membrane rigidifying properties than their C24:1 homologues (nervonoyl SM, nSM, or nervonoyl Cer, nCer), although with a similar strong capacity to induce segregated gel phases. In the case of the lSM-lCer multicomponent system, the segregated phases have a peculiar fibrillar or fern-like morphology. Moreover, the combination of C24:0 and C24:1 sphingolipids generates interesting events, such as a generalized bilayer dynamism/instability of supported planar bilayers. In some cases, these sphingolipids give rise to exothermic curves in thermograms. These peculiar features were not present in previous studies of C24:1 combined with C16:0 sphingolipids. Conclusions of our study point to nSM as a key factor governing the relative distribution of ceramides when both lCer and nCer are present. The data indicate that lCer could be easier to accommodate in multicomponent bilayers than its C16:0 counterpart. These results are relevant for events of membrane platform formation, in the context of sphingolipid-based signaling cascades. Sphingolipids are important structural membrane lipids, as well as second messengers in diverse cellular signaling cascades 1-4. Among the sphingolipid subfamilies, ceramides (Cer) have received the attention of investigators due to their particular biophysical properties and their role in apoptotic processes 5-8. Cer are also important in the stratum corneum of the skin 9. The biophysical properties of Cer cause dramatic changes in membranes, as this sphingolipid tends to induce the formation of segregated areas ('domains'), giving rise to bilayer lateral heterogeneity 10-13. In turn the presence of domains has an impact on the diffusivity of proteins and their capacity to cluster and exert their physiological effects 14-16. Mammals have 6 ceramide synthases, of which CerS5 predominantly produces C16:0 Cer, while CerS2 yields ceramides incorporating C22-C24 fatty acids 17. For long and very-long chain Cer (longer than 14 carbons in their N-acyl group), the effects on membranes may also include lipid trans-bilayer motion, or flip-flop 18 (therefore affecting bilayer asymmetry) and a notable increase in solute permeability across the membrane 19,20 , which may decisively distort cell homeostasis. Most of the experiments classically performed with model membranes have been focused on C16:0 ceramide (pCer), as it is a simple, saturated long-chain ceramide and, more importantly, C16:0 s...

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“…Cyclodextrins have been of interest for the pharmaceutical and cosmetic industry for many years [1–5]. Native cyclodextrins have been employed to improve physical stability of submicron emulsions for dermal delivery; skin permeation of incorporated drugs can be enhanced [6].…”

Section: Introductionmentioning

confidence: 99%

Effect of hydroxypropyl‐β‐cyclodextrin in fluid and semi‐solid submicron emulsions on physiological skin parameters during regular in vivo application

Pany¹,

Wohlgenannt²,

Klopprogge

et al. 2021

Intern J of Cosmetic Sci

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Objective The aim of the present study was to evaluate the effect of hydroxypropyl‐β‐cyclodextrin (HP‐β‐CD) in cosmetic submicron emulsions and submicron emulsion gels on physiological skin parameters during regular application in a clinical set‐up. Methods Formulation morphology was investigated using cryo‐transmission electron microscopy. Stability of the employed formulations was determined by photon correlation spectroscopy, measurement of pH and rheological properties. Effect on physiological skin parameters was evaluated during regular application over four weeks in a parallel group study (n = 15, healthy forearm skin) with a Corneometer, Sebumeter, skin‐pH‐Meter, Aquaflux and an Epsilon sensor. Confocal Raman spectroscopy was employed to monitor urea and NMF levels. Results Both submicron emulsions and gels showed satisfying storage stability irrespective of cyclodextrin incorporation. No statistically significant effects on skin barrier function and any of the observed parameters were obtained, indicating good skin tolerability of all tested formulations. Conclusion Results suggest good skin tolerability of the developed cosmetic submicron emulsions and gels with HP‐β‐CD.

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Novel Findings about Double-Loaded Curcumin-in-HPβcyclodextrin-in Liposomes: Effects on the Lipid Bilayer and Drug Release

Cited by 37 publications

References 68 publications

Design and Characterization of Spray-Dried Proliposomes for the Pulmonary Delivery of Curcumin

Design and Characterization of Spray-Dried Proliposomes for the Pulmonary Delivery of Curcumin

C24:0 and C24:1 sphingolipids in cholesterol-containing, five- and six-component lipid membranes

Effect of hydroxypropyl‐β‐cyclodextrin in fluid and semi‐solid submicron emulsions on physiological skin parameters during regular in vivo application

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