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1.
Food Chem ; 368: 130859, 2022 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-34425339

RESUMO

DHA loaded nanoliposomes, stabilized by ß-sitosterol, were prepared by thin film hydration-sonication method. The characteristics and membranes properties of DHA-NLs with different ß-sitosterol content were measured. The samples with the same formulation were used to measure the resistance of environment stress and controlled release & absorption of DHA in vitro and in vivo. The results showed that the maximal encapsulation efficiency of DHA-NLs was (86.95 ± 0.95)%, when the ratio of soybean lecithin to ß-sitosterol was 5:1. The particle size of all samples was within 200 nm and relative retention rate was more than 60% after 3 weeks storage. The area under the curve of DHA concentration of DHA-NLs and DHA-emulsion groups was 1.32 and 1.08, respectively. In summary, the nanoliposomes were promising to improve the absorption of DHA in form of ethyl ester.


Assuntos
Lecitinas , Sitosteroides , Emulsões , Lipossomos , Tamanho da Partícula
2.
AAPS PharmSciTech ; 22(8): 269, 2021 Nov 11.
Artigo em Inglês | MEDLINE | ID: mdl-34762193

RESUMO

Brucine, one of the natural medications obtained from Nux vomica seeds, is used as an anti-inflammatory drug. Several investigations were performed to overcome its drawbacks, which will affect significantly its pharmaceutical formulation. The goal of the current investigation was to design, optimize, and evaluate the anti-inflammatory performance of BRU ethosomal gel. Brucineethosomal formulations were prepared using thin film hydration method and optimized by central composite design approach using three independent variables (lecithin concentration, cholesterol concentration, and ethanol percentage) and three response variables (vesicular size, encapsulation efficiency, and skin permeation). The optimized formulation was examined for its stability and then incorporated into HPMC gel to get BRU ethosomal gel. The obtained BRU-loaded ethosomal gel was evaluated for its physical properties, in vitro release, and ex vivo permeation and skin irritation. Finally, carrageenan-induced rat hind paw edema test was adopted for the anti-inflammatory activity. The developed BRU ethosomal gel exhibited good physical characteristics comparable with the conventional developed BRU gel. In vitro release of BRU from ethosomal gel was effectively extended for 6 h. Permeation of BRU from ethosomes was significantly higher than all formulations (p < 0.05), since it recorded steady state transdermal flux value 0.548 ± 0.03 µg/cm2 h with enhancement ratio 2.73 ± 0.23. Eventually, BRU ethosomal gel exhibited potent anti-inflammatory activity as manifested by a significant decrease in rat hind paw inflammation following 24 h. In conclusion, the study emphasized the prospective of ethosomal gel as a fortunate carrier for intensifying the anti-inflammatory effect of Brucine.


Assuntos
Absorção Cutânea , Pele , Administração Cutânea , Animais , Anti-Inflamatórios/metabolismo , Lecitinas/metabolismo , Lipossomos/metabolismo , Estudos Prospectivos , Ratos , Pele/metabolismo , Estricnina/análogos & derivados
3.
IET Nanobiotechnol ; 15(3): 309-317, 2021 May.
Artigo em Inglês | MEDLINE | ID: mdl-34694664

RESUMO

Co-surfactant free l-ascorbic acid (LAA) nanoemulsions were prepared using mixed surfactants (Soya lecithin and Tween 80). Response surface methodology (RSM) was used to optimise the emulsifying conditions for LAA nanoemulsions. The effects of water proportion (6%-14% w/w), homogenisation pressure (80-160 MPa), surfactant concentrations (4%-12% w/w) and LAA concentration (0.5-1.3 w/w) on responses (size of droplets and nanoemulsion stability) were investigated. RSM results showed that the values of responses can be successfully predicted through second-order polynomial model. The coefficients of determinations for droplet size and nanoemulsion stability were 0.9375 and 0.9027, respectively. The optimum preparation conditions for l-LAA nanoemulsion were 9.04% water proportion, 114.48 MPa homogenisation pressure, 7.36% surfactant concentration and 1.09% LAA concentration. At the end of one month storage study, the retention of LAA in optimised nanoemulsions stored at 4°C and 25°C were 74.4% and 66.7%, respectively. These results may provide valuable contributions for food and pharmaceutical industry to develop delivery system for food additives and nutraceutical components.


Assuntos
Ácido Ascórbico , Tensoativos , Emulsões , Lecitinas , Tamanho da Partícula
4.
Int J Mol Sci ; 22(19)2021 Oct 06.
Artigo em Inglês | MEDLINE | ID: mdl-34639136

RESUMO

BACKGROUND: α-cyclodextrin (α-CD) is one of the dietary fibers that may have a beneficial effect on cholesterol and/or glucose metabolism, but its efficacy and mode of action remain unclear. METHODS: In the present study, we examined the anti-hyperglycemic effect of α-CD after oral loading of glucose and liquid meal in mice. RESULTS: Administration of 2 g/kg α-CD suppressed hyperglycemia after glucose loading, which was associated with increased glucagon-like peptide 1 (GLP-1) secretion and enhanced hepatic glucose sequestration. By contrast, 1 g/kg α-CD similarly suppressed hyperglycemia, but without increasing secretions of GLP-1 and insulin. Furthermore, oral α-CD administration disrupts lipid micelle formation through its inclusion of lecithin in the gut luminal fluid. Importantly, prior inclusion of α-CD with lecithin in vitro nullified the anti-hyperglycemic effect of α-CD in vivo, which was associated with increased intestinal mRNA expressions of SREBP2-target genes (Ldlr, Hmgcr, Pcsk9, and Srebp2). CONCLUSIONS: α-CD elicits its anti-hyperglycemic effect after glucose loading by inducing lecithin inclusion in the gut lumen and activating SREBP2, which is known to induce cholecystokinin secretion to suppress hepatic glucose production via a gut/brain/liver axis.


Assuntos
Trato Gastrointestinal/metabolismo , Hiperglicemia/prevenção & controle , Lecitinas/metabolismo , Período Pós-Prandial , Canais de Potássio Corretores do Fluxo de Internalização/fisiologia , Proteína de Ligação a Elemento Regulador de Esterol 2/metabolismo , alfa-Ciclodextrinas/farmacologia , Animais , Trato Gastrointestinal/efeitos dos fármacos , Hiperglicemia/etiologia , Hiperglicemia/metabolismo , Hiperglicemia/patologia , Masculino , Camundongos , Camundongos Endogâmicos C57BL , Camundongos Knockout , Proteína de Ligação a Elemento Regulador de Esterol 2/genética
5.
Eur Phys J E Soft Matter ; 44(11): 132, 2021 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-34718875

RESUMO

Understanding the physical and chemical properties of viral infections at molecular scales is a major challenge for the scientific community more so with the outbreak of global pandemics. There is currently a lot of effort being placed in identifying molecules that could act as putative drugs or blockers of viral molecules. In this work, we computationally explore the importance in antiviral activity of a less studied class of molecules, namely surfactants. We employ all-atoms molecular dynamics simulations to study the interaction between the receptor-binding domain of the SARS-CoV-2 spike protein and the phospholipid lecithin (POPC), in water. Our microsecond simulations show a preferential binding of lecithin to the receptor-binding motif of SARS-CoV-2 with binding free energies significantly larger than [Formula: see text]. Furthermore, hydrophobic interactions involving lecithin non-polar tails dominate these binding events, which are also accompanied by dewetting of the receptor binding motif. Through an analysis of fluctuations in the radius of gyration of the receptor-binding domain, its contact maps with lecithin molecules, and distributions of water molecules near the binding region, we elucidate molecular interactions that may play an important role in interactions involving surfactant-type molecules and viruses. We discuss our minimal computational model in the context of lecithin-based liposomal nasal sprays as putative mitigating therapies for COVID-19.


Assuntos
Lecitinas/química , Simulação de Acoplamento Molecular , Fosfatidilcolinas/química , Glicoproteína da Espícula de Coronavírus/química , Tensoativos/química , Sítios de Ligação , Interações Hidrofóbicas e Hidrofílicas , Sprays Nasais , Ligação Proteica , Glicoproteína da Espícula de Coronavírus/metabolismo
6.
J Phys Chem B ; 125(36): 10195-10212, 2021 09 16.
Artigo em Inglês | MEDLINE | ID: mdl-34491062

RESUMO

Cholesterol is known for its role in maintaining the correct fluidity and rigidity of the animals cell membranes and thus their functions. Assessing the content and the role of cholesterol in lipid bilayers is therefore of crucial importance for a deeper understanding and control of membrane functioning. In this computational work, we investigate bilayers built from three types of glycerophospholipid phosphatidylcholine (PC) lipids, namely dipalmitoylphosphatidylcholine (DPPC), 1-palmitoyl-2-oleoyl-sn-glycero-3-phosphocholine (POPC), and dioleoylphosphatidylcholine (DOPC), and containing different amounts of cholesterol by analyzing the second-harmonic generation (SHG) nonlinear optical (NLO) response of a probe molecule, di-8-ANEPPS, inserted into the membranes. This molecular property presents the advantage to be specific to interfacial regions such as lipid bilayers. To unravel these effects, Molecular Dynamics (MD) simulations have been performed on both DPPC and DOPC lipids by varying the cholesterol mole fraction (from 0 to 0.66), while POPC was only considered as a pure bilayer. In the case of the structural properties of the bilayers, all the analyses converge toward the same conclusion: as the mole fraction of cholesterol increases, the systems become more rigid, confirming the condensing effect of cholesterol. In addition, the chromophore is progressively more aligned with respect to the normal to the bilayer. On the contrary, addition of unsaturation disorders the lipid bilayers, with barely no impact on the alignment of the chromophore. Then, using the frames obtained from the MD simulations, the first hyperpolarizability ß of the dye in its environment has been computed at the TDDFT level. On the one hand, the addition of cholesterol induces a progressive increase of the diagonal component the ß tensor parallel to the bilayer normal. On the other hand, larger ß values have been calculated for the unsaturated than for the saturated lipid systems. In summary, this study illustrates the relationship between the composition and structure of the bilayers and the NLO responses of the embedded dye.


Assuntos
Bicamadas Lipídicas , Fosfatidilcolinas , Colesterol , Lecitinas , Compostos de Piridínio
7.
Int J Pharm ; 608: 121114, 2021 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-34543618

RESUMO

Lecithin-chitosan hybrid nanoparticles are emerging as a promising nanocarrier for topical drug delivery. They could achieve a maximized encapsulation of hydrophobic drugs due to the lipophilic nature of lecithin that comprises the core while enhancing retention in the upper skin layers using the positively charged polymeric coat of chitosan. The aim of this study is to incorporate tacrolimus; a hydrophobic anti-proliferative agent into lecithin chitosan hybrid nanoparticles by ethanolic injection technique using a suitable co-solvent to enhance encapsulation of the drug and allow a satisfactory release profile in the upper skin layers. Tacrolimus was successfully incorporated into the synthesized particles using olive oil and Tween 80 as co-solvents, with particle size (160.9 nm ± 15.9 and 118.7 nm ± 13.3, respectively) and EE (88.27% ± 4.3 and 66.72% ± 1.8, respectively). The in vitro drug release profile showed a faster release pattern for the Tween 80-containing particles over a 48-hour period (79.98% vs. 35.57%), hence, were selected for further investigation. The hybrid nanoparticles achieved significantly higher skin deposition than the marketed product (63.51% vs. 34.07%) through a 24-hour time interval, particularly, to the stratum corneum and epidermis skin layers. The in vivo results on IMQ-mouse models revealed superior anti-psoriatic efficacy of the synthesized nanoparticles in comparison to the marketed product in terms of visual observation of the skin condition, PASI score and histopathological examination of autopsy skin samples. Additionally, the in vivo drug deposition showed superior skin deposition of the nanoparticles compared to the marketed product (74.9% vs. 13.4%).


Assuntos
Quitosana , Nanopartículas , Psoríase , Animais , Quitosana/uso terapêutico , Portadores de Fármacos/uso terapêutico , Lecitinas , Camundongos , Tamanho da Partícula , Psoríase/tratamento farmacológico , Tacrolimo/uso terapêutico
8.
Langmuir ; 37(33): 10200-10213, 2021 08 24.
Artigo em Inglês | MEDLINE | ID: mdl-34379976

RESUMO

Self-emulsifying drug-delivery systems (SEDDS) have been extensively shown to increase oral absorption of solvation-limited compounds. However, there has been little clinical and commercial use of these formulations, in large part because the demonstrated advantages of SEDDS have been outweighed by our inability to precisely predict drug absorption from SEDDS using current in vitro assays. To overcome this limitation and increase the biological relevancy of in vitro assays, an absorption function can be incorporated using biomimetic membranes. However, the effects that SEDDS have on the integrity of a biomimetic membrane are not known. In this study, a quartz crystal microbalance with dissipation monitoring and total internal reflection fluorescence microscopy were employed as complementary methods to in vitro lipolysis-permeation assays to characterize the interaction of various actively digested SEDDS with a liquescent artificial membrane comprising lecithin in dodecane (LiDo). Observations from surface analysis showed that interactions between the digesting SEDDS and LiDo membrane coincided with inflection points in the digestion profiles. Importantly, no indications of membrane damage could be observed, which was supported by flux profiles of the lipophilic model drug felodipine (FEL) and impermeable marker Lucifer yellow on the basal side of the membrane. There was a correlation between the digestion kinetics of the SEDDS and the flux of FEL, but no clear correlation between solubilization and absorption profiles. Membrane interactions were dependent on the composition of lipids within each SEDDS, with the more digestible lipids leading to more pronounced interactions, but in all cases, the integrity of the membrane was maintained. These insights demonstrate that LiDo membranes are compatible with in vitro lipolysis assays for improving predictions of drug absorption from lipid-based formulations.


Assuntos
Biomimética , Sistemas de Liberação de Medicamentos , Administração Oral , Emulsões , Intestino Delgado , Lecitinas , Solubilidade
9.
Colloids Surf B Biointerfaces ; 207: 112029, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34399158

RESUMO

Sophorolipids (SLs) constitute a group of unique biosurfactants (BS) in the light of their outstanding properties, among which their antimicrobial activities stand out. SLs can exist mainly in an acidic and a lactonic form, both of which display inhibitory activity. Given the amphipathic nature of SLs it is feasible that these antimicrobial actions are the result of the perturbation of the physicochemical properties of targeted membranes. Thus, in this work we have carried out a biophysical study to unveil the molecular details of the interaction of an acidic SL with a model phospholipid membrane made of 1,2-dipalmitoy-sn-glycero-3-phosphocholine (DPPC). Using differential scanning calorimetry it was found that SL altered the phase behaviour of DPPC at low molar fractions, producing fluid phase immiscibility with the result of formation of biosurfactant-enriched domains within the phospholipid bilayer. Fourier-transform infrared spectroscopy showed that SL interacted with DPPC increasing ordering of the phospholipid acyl chain palisade and hydration of the lipid/water interface. Small angle X-ray scattering showed that SL did not modify bilayer thickness in the biologically relevant Lα fluid phase. SL was found to induce contents leakage in 1-palmitoy-2-oleoy-sn-glycero-3-phosphocholine (POPC) unilamellar liposomes, at sublytic concentrations below the cmc. This SL-induced membrane permeabilization at concentrations below the onset for membrane solubilization can be the result of the formation of laterally segregated domains, which might contribute to provide a molecular basis for the reported antimicrobial actions of SLs.


Assuntos
Lecitinas , Fosfatidilcolinas , Varredura Diferencial de Calorimetria , Bicamadas Lipídicas , Membranas , Ácidos Oleicos , Fosfolipídeos
10.
Int J Pharm ; 607: 121016, 2021 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-34411652

RESUMO

Quercetin, a flavonoid with possible neuroprotective action has been recently suggested for the early-stage treatment of Alzheimer's disease. The low solubility and extended first pass effect render quercetin unsuitable for oral administration. Alternatively, brain targeting is more feasible with nasal delivery, by-passing, non-invasively, Blood-Brain Barrier and ensuring rapid onset of action. Aiming to increase quercetin's disposition into brain, nasal powders consisting of quercetin-cyclodextrins (methyl-ß-cyclodextrin and hydroxypropyl-ß-cyclodextrin) lyophilizates blended with spray-dried microparticles of mannitol/lecithin were prepared. Quercetin's solubility at 37 °C and pH 7.4 was increased 19-35 times when complexed with cyclodextrins. Blending lyophilizates in various ratios with mannitol/lecithin microparticles, results in powders with improved morphological characteristics as observed by X-ray Diffraction and Scanning Electron Microscopy analysis. In vitro characterization of these powders using Franz cells, revealed rapid dissolution and permeation 17 (methyl-ß-cyclodextrin) to 48 (hydroxypropyl-ß-cyclodextrin) times higher than that of pure quercetin. Ex vivo powders' transport across rabbit nasal mucosa was found more efficient in comparison with the pure Que. The overall better performance of quercetin-hydroxypropyl-ß-cyclodextrin powders is confirmed by ex vivo experiments revealing amount of quercetin permeated ranging from 0.03 ± 0.01 to 0.22 ± 0.05 µg/cm2 for hydroxypropyl-ß-cyclodextrin and 0.022 ± 0.01 to 0.17 ± 0.04 µg/cm2 for methyl-ß-cyclodextrin powders, while the permeation of pure quercetin was negligible.


Assuntos
Ciclodextrinas , Lecitinas , 2-Hidroxipropil-beta-Ciclodextrina , Animais , Encéfalo , Varredura Diferencial de Calorimetria , Manitol , Mucosa Nasal , Pós , Quercetina , Coelhos , Solubilidade , Difração de Raios X
11.
J Oleo Sci ; 70(8): 1069-1080, 2021 Aug 05.
Artigo em Inglês | MEDLINE | ID: mdl-34248099

RESUMO

The effects of bile salts on the emulsifier adsorption layer play a crucial role in lipid digestion. The current study selected sodium cholate (NaCh) and lecithin as model compounds for bile salts and food emulsifiers, respectively. The interface dilational rheological and emulsification properties of NaCh and lecithin were carried out. The results showed that the NaCh molecules could quickly diffuse from the bulk to interface, which broke the tightly-arranged interfacial layer of lecithin and enhanced the viscoelasticity of interfacial film. As a result, the interfacial adsorption layer, which was originally dominated by the slow relaxation processes within the interface, was transformed into one controlled by the fast molecular diffusion exchange. This accelerated the exchange of materials between the bulk and interface, thereby creating suitable conditions for the interfacial adsorption of lipases, which promoted the digestion process. These results provided a mechanism for the promotion of lipid digestion by bile salts from the perspective of interfacial viscoelasticity and relaxation processes. A deeper understanding of the interfacial behavior of bile salts with emulsifiers would provide a basis for the rational design of interfacial layer for modulating lipid digestion.


Assuntos
Emulsificantes/química , Lecitinas/química , Colato de Sódio/química , Adsorção , Difusão , Digestão , Emulsões/química , Hidrólise , Lipase/química , Reologia , Tensão Superficial , Triglicerídeos/química , Viscosidade
12.
Int J Biol Macromol ; 185: 861-875, 2021 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-34237363

RESUMO

Peppermint oil (PO) is the most prominent oil using in pharmaceutical formulations with its significant therapeutic value. In this sense, this oil is attracting considerable attention from the scientific community due to its traditional therapeutic claim, biological and pharmacological potential in recent research. An organic solvent-free and environment-friendly electrohydrodynamic assisted (EHDA) technique was employed to prepared PO-loaded alginate microbeads. The current study deals with the development, optimization, in vitro characterization, in vivo gastrointestinal tract drug distribution and ex-vivo mucoadhesive properties, antioxidant, and anti-inflammatory effects of PO-loaded alginate microbeads. The optimization results indicated the voltage and flow rate have a significant influence on microbeads size and sphericity factor and encapsulation efficiency. All these optimized microbeads showed a better drug release profile in simulated intestinal fluid (pH 6.8) at 2 h. However, a minor release was found in acidic media (pH 1.2) at 2 h. The optimized formulation showed excellent mucoadhesive properties in ex-vivo and good swelling characterization in intestine media. The microbeads were found to be well distributed in various parts of the intestine in in vivo study. PO-loaded alginate microbeads similarly showed potential antioxidant effects with drug release. The formulation exhibited possible improvement of irritable bowel syndrome (IBS) in MO-induced rats. It significantly suppressed proinflammatory cytokines, i.e., interleukin- IL-1ß, and upregulated anti-inflammatory cytokine expression, i.e., IL-10. It would be a promising approach for targeted drug release after oral administration and could be considered an anti-inflammatory therapeutic strategy for treating IBS.


Assuntos
Alginatos/química , Anti-Inflamatórios/administração & dosagem , Síndrome do Intestino Irritável/tratamento farmacológico , Lecitinas/química , Óleos Vegetais/administração & dosagem , Administração Oral , Animais , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Modelos Animais de Doenças , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Hidrodinâmica , Concentração de Íons de Hidrogênio , Síndrome do Intestino Irritável/induzido quimicamente , Loperamida/efeitos adversos , Masculino , Microesferas , Estrutura Molecular , Óleos Vegetais/química , Óleos Vegetais/farmacologia , Ratos
13.
Andrologia ; 53(10): e14183, 2021 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-34255371

RESUMO

This study was to evaluate the effects of two different ultrastructures of lecithin including nanoparticles (NPE mostly nanomicelles) and lecithin nanoliposome (NLE) with egg yolk extender (EYE) on goat sperm cryopreservation. Semen samples were collected from 6 goats, then pooled, diluted and then frozen. Motility and motion parameters, plasma membrane integrity and functionality, morphology, apoptosis status (Annexin V-PI), acrosome integrity, DNA fragmentation and in vitro fertilisation were assessed. Total motility and most motion parameters were higher in EYE (p < .05) compared with the two lecithin extenders, while there were no significant differences between NLE and NPE. NLE and NPE had higher values for viable spermatozoa (Annexin V-PI) (p < .05) compared with EYE. The highest value for dead spermatozoa was observed in EYE (p = .08). A higher percentage of DNA fragmentation (p < .05) was detected in EYE compared with NPE. Plasma membrane integrity and functionality, morphology, acrosome integrity and fertility of spermatozoa indicated no significant differences between extenders. Data suggested that ultrastructural changes of lecithin (micelles versus. liposome) could not improve the sperm cryosurvival of goat spermatozoa. Moreover, we cannot also claim that lecithin-based diluent supplies better protection compared with the egg yolk in goat.


Assuntos
Lecitinas , Preservação do Sêmen , Animais , Criopreservação , Crioprotetores/farmacologia , Gema de Ovo , Cabras , Masculino , Preservação do Sêmen/veterinária , Motilidade Espermática , Espermatozoides
14.
J Pharm Sci ; 110(11): 3648-3658, 2021 11.
Artigo em Inglês | MEDLINE | ID: mdl-34303675

RESUMO

Relationship between the stability of fat nano-emulsions and the incorporated drug at the molecular level are rarely known. Herein, fat nano-emulsions containing dihydropyridine drugs were prepared and the microstructure of their palisade layers were investigated.The prepared 1.0 mg/mL nimodipine nano-emulsion was found to contain 65.50% drug in the palisade layer. The increasing drug concentration led to a decrease-increase-decrease trend in centrifugal stability constant, particle size and proton nuclear magnetic resonance (1H NMR) signal intensity of the lecithin trimethyl ammonium group in the nimodipine and felodipine nano-emulsions. The 1H NMR spectra of test solutions including nano-emulsions suggest that increasing drugs penetrated into the palisade layer, resulting in the lecithin arrangement from loose to tight, and then from monolayer to bilayer. Nimodipine and felodipine nano-emulsions showed two valley values at concentrations of 0.15 and 0.75 mg/mL, and 0.30 and 0.90 mg/mL respectively, which indicated that the nano-emulsion has two more stable states corresponding to the tightly arranged mono- and bi-palisade layer. These two concentrations are positively correlated with lipophilicity of nimodipine and felodipine. Further, nimodipine liposomes were prepared to validate the effect of drugs on the arrangement of lecithin in the palisade layer. 1H NMR characterizations of the liposomes showed a similar profile to that of nano-emulsions. These results demonstrated that the increasing drug concentration could cause a rearrangement of lecithin in the palisade layer, thus affecting emulsion stability.


Assuntos
Di-Hidropiridinas , Lecitinas , Estabilidade de Medicamentos , Emulsões , Tamanho da Partícula
15.
Food Chem ; 365: 130542, 2021 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-34265644

RESUMO

The Zein-Lecithin-Epigallocatechin gallate (EGCG) complex nanoparticles were fabricated by anti-solvent coprecipitation method. The Zein-Lecithin (Z-L) nanocomplexes exhibited great encapsulation efficiency of 68.5% for EGCG, and the encapsulated EGCG still had good antioxidative capacity. The cumulative release of EGCG in simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) were 19% and 92%, respectively, and the release was closest to Fick release in SGF and First release in SIF. Fluorescence spectroscopy (FL), Fourier transform infrared spectroscopy (FTIR) and X-ray diffraction (XRD) experiments revealed that the EGCG was successfully encapsulated by Z-L nanocomplexes through electrostatic, hydrophobic and hydrogen bonding interactions. The Zein-Lecithin-EGCG complex nanoparticles exhibited excellent stability and great sustained-release performance, which will be the alternative for potential application in the food industry.


Assuntos
Nanopartículas , Zeína , Catequina/análogos & derivados , Preparações de Ação Retardada , Digestão , Lecitinas , Tamanho da Partícula
16.
Int J Pharm Compd ; 25(3): 241-245, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34125715

RESUMO

In vitro release tests are used to evaluate drug release of semisolid dosage forms for topical applications. We evaluated the capability of an in vitro release tests method to determine differences in drug release from three strengths of ketoprofen and from two different base formulations; a Pluronic lecithin organogel versus Lipoderm cream. Tests were conducted using two different apparatuses; the Phoenix DB-6 Dry Heat Diffusion Tester and immersion cells adapted to a USP 2 dissolution tester to compare their relative performance and test results. Our results demonstrate the ability of the method to discern differences in ketoprofen release rates proportional to drug concentration, differences in ketoprofen release rates between formulations with release from Pluronic lecithin organogel greater than that from Lipoderm at all concentrations, and comparability of results between apparatuses.


Assuntos
Cetoprofeno , Géis , Temperatura Alta , Imersão , Lecitinas , Poloxâmero , Absorção Cutânea
17.
Langmuir ; 37(27): 8115-8128, 2021 07 13.
Artigo em Inglês | MEDLINE | ID: mdl-34191521

RESUMO

Marine oil dispersants typically contain blends of surfactants dissolved in solvents. When introduced to the crude oil-seawater interface, dispersants facilitate the breakup of crude oil into droplets that can disperse in the water column. Recently, questions about the environmental persistence and toxicity of commercial dispersants have led to the development of "greener" dispersants consisting solely of food-grade surfactants such as l-α-phosphatidylcholine (lecithin, L) and polyoxyethylenated sorbitan monooleate (Tween 80, T). Individually, neither L nor T is effective at dispersing crude oil, but mixtures of the two (LT blends) work synergistically to ensure effective dispersion. The reasons for this synergy remain unexplained. More broadly, an unresolved challenge is to be able to predict whether a given surfactant (or a blend) can serve as an effective dispersant. Herein, we investigate whether the LT dispersant effectiveness can be correlated with thermodynamic phase behavior in model systems. Specifically, we study ternary "DOW" systems comprising LT dispersant (D) + a model oil (hexadecane, O) + synthetic seawater (W), with the D formulation being systematically varied (across 0:100, 20:80, 40:60, 60:40, 80:20, and 100:0 L:T weight ratios). We find that the most effective LT dispersants (60:40 and 80:20 L:T) induce broad Winsor III microemulsion regions in the DOW phase diagrams (Winsor III implies that the microemulsion coexists with aqueous and oil phases). This correlation is generally consistent with expectations from hydrophilic-lipophilic deviation (HLD) calculations, but specific exceptions are seen. This study then outlines a protocol that allows the phase behavior to be observed on short time scales (ca. hours) and provides a set of guidelines to interpret the results. The complementary use of HLD calculations and the outlined fast protocol are expected to be used as a predictive model for effective dispersant blends, providing a tool to guide the efficient formulation of future marine oil dispersants.


Assuntos
Poluição por Petróleo , Petróleo , Poluentes Químicos da Água , Lecitinas , Poluição por Petróleo/análise , Polissorbatos , Tensoativos , Poluentes Químicos da Água/análise
18.
Molecules ; 26(11)2021 May 28.
Artigo em Inglês | MEDLINE | ID: mdl-34071530

RESUMO

Anti-cancer activity of catechin nanoemulsions prepared from Oolong tea leaf waste was studied on prostate cancer cells DU-145 and DU-145-induced tumors in mice. Catechin nanoemulsions composed of lecithin, Tween-80 and water in an appropriate proportion was prepared with high stability, particle size of 11.3 nm, zeta potential of -67.2 mV and encapsulation efficiency of 83.4%. Catechin nanoemulsions were more effective than extracts in inhibiting DU-145 cell growth, with the IC50 being 13.52 and 214.6 µg/mL, respectively, after 48 h incubation. Furthermore, both catechin nanoemulsions and extracts could raise caspase-8, caspase-9 and caspase-3 activities for DU-145 cell apoptosis, arresting the cell cycle at S and G2/M phases. Compared to control, catechin nanoemulsion at 20 µg/mL and paclitaxel at 10 µg/mL were the most effective in reducing tumor volume by 41.3% and 52.5% and tumor weight by 77.5% and 90.6% in mice, respectively, through a decrease in EGF and VEGF levels in serum.


Assuntos
Catequina/química , Emulsões/química , Nanopartículas/química , Folhas de Planta/metabolismo , Neoplasias da Próstata/tratamento farmacológico , Chá/química , Animais , Antineoplásicos/farmacologia , Apoptose , Caspase 8/metabolismo , Ciclo Celular , Linhagem Celular Tumoral , Endocitose , Humanos , Concentração Inibidora 50 , Lecitinas/química , Limite de Detecção , Masculino , Camundongos , Camundongos SCID , Nanotecnologia/métodos , Transplante de Neoplasias , Neoplasias Experimentais/tratamento farmacológico , Tamanho da Partícula , Polissorbatos/química , Controle de Qualidade , Solventes , Água/química
19.
Int J Nanomedicine ; 16: 4017-4030, 2021.
Artigo em Inglês | MEDLINE | ID: mdl-34140769

RESUMO

Purpose: This study was aimed at developing the trispecific antibodies (anti-EGFR/anti-FAP/anti-mPEG, TsAb) or dual bispecific antibodies (anti-EGFR/anti-mPEG and anti-FAP/anti-mPEG) docetaxel (DTX)-loaded mPEGylated lecithin-stabilized micelles (mPEG-lsbPMs) for improving the targeting efficiency and therapeutic efficacy. Methods: mPEG-lsbPMs were simply prepared via thin film method. The trispecific antibodies or bispecific antibodies bound the mPEG-lsbPMs by anti-mPEG Fab fragment. The formulations were characterized by DLS and TEM; in vitro and in vivo studies were also conducted to evaluate the cellular uptake, cell cytotoxicity and therapeutic efficacy. Results: The particle sizes of mPEG-lsbPMs with or without the antibodies were around 100 nm; the formulations showed high encapsulation efficiencies of 97.12%. The TsAb and dual bispecific antibodies were fabricated and demonstrated their targeting ability. Two EGFR-overexpressed cell lines (HT-29 and MIA PaCa-2) were co-cultured with FAP-overexpressed WS1 cells (HT-29/WS1; MIA PaCa-2/WS1) to mimic a tumor coexisting in the tumor microenvironment. Cellular binding study revealed that the binding of anti-FAP micelles to three co-culture ratios (4:1, 1:1, and 1:4) of HT-29/EGFR to WS1/FAP was significantly higher than that for TsAb micelles and dual (1:1) micelles, and the binding of those targeting antibodies to WS1/FAP and MIA PaCa-2/EGFR was equally efficacious resulting in a similar binding amount of the TsAb and dual BsAbs (1:1) with the co-culture of MIA PaCa-2/EGFR and WS1/FAP at a 1:1 ratio. Antitumor efficacy study showed that treatment with DTX-loaded mPEG-lsbPMs modified with or without BsAbs, dual BsAbs (1:1), and TsAbs was enhanced in inhibiting tumor growth compared with that for Tynen® while showing fewer signs of adverse effects. Conclusion: Active targeting of both tumors and TAF-specific antigens was able to increase the affinity of DTX-loaded mPEG-lsbPMs toward tumor cells and TAFs leading to successive uptake by tumor cells or TAFs which enhanced their chemotherapeutic efficacy against antigen-positive cancer cells.


Assuntos
Anticorpos Biespecíficos/farmacologia , Antineoplásicos Imunológicos/administração & dosagem , Antineoplásicos Imunológicos/farmacologia , Docetaxel/administração & dosagem , Portadores de Fármacos/química , Animais , Anticorpos Biespecíficos/administração & dosagem , Anticorpos Biespecíficos/química , Antineoplásicos Imunológicos/farmacocinética , Fibroblastos Associados a Câncer/efeitos dos fármacos , Linhagem Celular Tumoral , Técnicas de Cocultura , Docetaxel/farmacocinética , Portadores de Fármacos/administração & dosagem , Sistemas de Liberação de Medicamentos/métodos , Receptores ErbB/antagonistas & inibidores , Receptores ErbB/imunologia , Humanos , Injeções Intradérmicas , Lecitinas/química , Masculino , Camundongos Nus , Micelas , Tamanho da Partícula , Polietilenoglicóis/química , Ratos Sprague-Dawley , Microambiente Tumoral/efeitos dos fármacos , Ensaios Antitumorais Modelo de Xenoenxerto
20.
Drug Deliv ; 28(1): 873-883, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-33960250

RESUMO

The aim of this investigation was to develop an etomidate intravenous lipid emulsion (ETM-ILE) and evaluate its properties in vitro and in vivo. Etomidate (ETM) is a hydrophobic drug, and organic solvents must be added to an etomidate injectable solution (ETM-SOL) to aid dissolution, that causes various adverse reactions on injection. Lipid emulsions are a novel drug formulation that can improve drug loading and reduce adverse reactions. ETM-ILE was prepared using high-pressure homogenization. Univariate experiments were performed to select key conditions and variables. The proportion of oil, egg lecithin, and poloxamer 188 (F68) served as variables for the optimization of the ETM-ILE formulation by central composite design response surface methodology. The optimized formulation had the following characteristics: particle size, 168.0 ± 0.3 nm; polydispersity index, 0.108 ± 0.028; zeta potential, -36.4 ± 0.2 mV; drug loading, 2.00 ± 0.01 mg/mL; encapsulation efficiency, 97.65% ± 0.16%; osmotic pressure, 292 ± 2 mOsmol/kg and pH value, 7.63 ± 0.07. Transmission electron microscopy images showed that the particles were spherical or spheroidal, with a diameter of approximately 200 nm. The stability study suggested that ETM-ILE could store at 4 ± 2 °C or 25 ± 2 °C for 12 months. Safety tests showed that ETM-ILE did not cause hemolysis or serious vascular irritation. The results of the pharmacokinetic study found that ETM-ILE was bioequivalent to ETM-SOL. However, a higher concentration of ETM was attained in the liver, spleen, and lungs after administration of ETM-ILE than after administration of ETM-SOL. This study found that ETM-ILE had great potential for clinical applications.


Assuntos
Anestésicos Intravenosos/administração & dosagem , Anestésicos Intravenosos/farmacocinética , Etomidato/administração & dosagem , Etomidato/farmacocinética , Emulsões Gordurosas Intravenosas/química , Anestésicos Intravenosos/farmacologia , Animais , Química Farmacêutica , Estabilidade de Medicamentos , Etomidato/farmacologia , Concentração de Íons de Hidrogênio , Lecitinas/química , Masculino , Tamanho da Partícula , Poloxâmero/química , Coelhos , Distribuição Aleatória , Ratos , Ratos Sprague-Dawley , Óleo de Soja/química , Propriedades de Superfície
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