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2.
Chem Commun (Camb) ; 56(9): 1353-1356, 2020 Jan 30.
Artigo em Inglês | MEDLINE | ID: mdl-31904054

RESUMO

A novel cyclodextrin molecular tube with one fully modified and one unmodified end was facilely synthesized by selective desilylation of a 6-O-tert-butyldimethylsilylated ß-cyclodextrin dimer possessing multiple linkers. This molecular tube showed a selective inclusion ability toward cis-unsaturated fatty acid esters by utilizing the asymmetric cylindrical nanocavity.


Assuntos
Ésteres/química , Ácidos Graxos Insaturados/química , beta-Ciclodextrinas/química , Estrutura Molecular , Estereoisomerismo , beta-Ciclodextrinas/síntese química
3.
J Photochem Photobiol B ; 203: 111765, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31923806

RESUMO

A potential strategy has been demonstrated, for the first time, for switching the mode of delivery of drugs or small molecular systems from endogenous to exogenous, simply by engineering the chain length of micellar carriers. Ethidium bromide (EB) is exploited as the model drug which has been successfully delivered to natural DNA through endogenous and exogenous modes by tuning the chain length of anionic sodium n-alkyl sulfate micelles. ß-cyclodextrin (ß-CD) is exploited as an extrinsic stimulant for the exogenous delivery of EB to DNA. Multi-spectroscopic techniques involving absorption, emission, fluorescence anisotropy, fluorescence decay analysis, circular dichroism, DNA helix melting etc. have established tuning of the delivery mode between endogenous and exogenous. Differential binding affinity of the model drug with different micelles of varying chain length relative to that with DNA is capitalized to make the switching feasible. Although endogenous mode avoids external stimulant and associated problems, a regulation of the stimulant concentration makes the other mode controllable and quantitative. With appropriate choice of carrier micelle and modulation of this developed strategy can radically change the therapeutic research enabling one to take a control over the drug delivery mode to exploit the advantage of one or the other selectively, whenever required.


Assuntos
DNA/química , Portadores de Fármacos/química , Etídio/química , Micelas , Dicroísmo Circular , Polarização de Fluorescência , Desnaturação de Ácido Nucleico , beta-Ciclodextrinas/química
4.
Braz Oral Res ; 33: e112, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-31939496

RESUMO

This clinical trial compared the efficacy of doxycycline (DOX) in ß-cyclodextrin (DOX)/ßCD) with DOX- alone in gel on thirty-three subjects with periodontitis. Patients were randomized to group 1 GI; 10% DOX + scaling and root planning (SRP); group 2 (GII (10% DOX /ß-CD + SRP), and group 3 (GIII; SRP). Gels were applied in GI and GII at baseline (T0) and 30 days later (T1). Periodontal Probing Depth (PPD), Clinical Attachment Level (CAL), Bleeding on Probing (BOP) and Visible Plaque Index (VPI) were evaluated at (T0), 30 days (T1) and 60 days after T0 (T2). Bone density was analyzed after 18 months (T3). GII showed the most significant reduction of PPD (2.62 mm; p <0.003), and greatest gain in CAL (2.54 mm p <0.003) at T2. BOP and the VPI had a strong reduction in all groups at T2 (p <0.05), both decreased by ≥5 times and 2 times, respectively, in all groups at T1. Bone density increased in all groups in radiographs (T3). The use of DOX encapsulated in ß-CD gel with SRP resulted in significant improvements in clinical periodontal parameters; such molecular inclusion of doxycycline into ß-CD in gel for local application is relatively simple and useful in dentistry.


Assuntos
Antibacterianos/uso terapêutico , Doxiciclina/uso terapêutico , Periodontite/tratamento farmacológico , beta-Ciclodextrinas/uso terapêutico , Adulto , Índice de Placa Dentária , Raspagem Dentária/métodos , Método Duplo-Cego , Composição de Medicamentos , Feminino , Géis , Humanos , Masculino , Pessoa de Meia-Idade , Perda da Inserção Periodontal , Índice Periodontal , Aplainamento Radicular/métodos , Resultado do Tratamento , Adulto Jovem
5.
Food Chem Toxicol ; 135: 110940, 2020 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-31693914

RESUMO

Eplingiella fruticosa (Lamiaceae), formally known as Hyptis fruticosa, is an important aromatic medicinal herb used in folk medicine in northeastern Brazil. We aimed to evaluate the anti-hyperalgesic effect of essential oil obtained from E. fruticosa (HypEO) complexed with ßCD (HypEO-ßCD) in a chronic widespread non-inflammatory muscle pain animal model (a mice fibromyalgia-like model, FM). The HypEO was extracted by hydro distillation and its chemical composition was determined by GC-MS/FID. Moreover, Fos protein expression in the spinal cord was assessed by immunofluorescence. (E)-caryophyllene, bicyclogermacrene, 1,8-cineole, α-pinene, ß-pinene and 21 other compounds were identified in the HypEO. The treatment with HypEO-ßCD produced a longer-lasting anti-hyperalgesic effect compared to HypEO, without alterations in motor coordination or myorelaxant effects. Moreover, HypEO and HypEO-ßCD produced a significant anti-hyperalgesic effect over 7 consecutive treatment days. Immunofluorescence assay demonstrated a decrease in Fos protein expression in the spinal cord (p < 0.001). We demonstrated that the anti-hyperalgesic effect produced by HypEO was improved after complexation with ß-CD and this seems to be related to the central pain-inhibitory pathway, suggesting the possible use of E. fruticosa for chronic pain management.


Assuntos
Analgésicos/uso terapêutico , Hiperalgesia/tratamento farmacológico , Lamiaceae/química , Mialgia/tratamento farmacológico , Óleos Voláteis/uso terapêutico , beta-Ciclodextrinas/uso terapêutico , Analgésicos/isolamento & purificação , Animais , Masculino , Camundongos , Óleos Voláteis/isolamento & purificação , Folhas de Planta/química , Proteínas Proto-Oncogênicas c-fos/metabolismo , Medula Espinal/efeitos dos fármacos , Medula Espinal/metabolismo
6.
J Chromatogr A ; 1609: 460519, 2020 Jan 04.
Artigo em Inglês | MEDLINE | ID: mdl-31521379

RESUMO

In this work, tetraalkylammonium amino acid ionic liquids (TAA-AAILs) were first applied to non-aqueous capillary electrophoresis (NACE) to establish synergistic systems with a conventional chiral selector, native ß-cyclodextrin (ß-CD). Excellent enantioseparations of some dansyl-amino acid (Dns-AA) samples were achieved. A series of comparison experiments and a molecular docking study were performed to validate the synergistic effect of TAA-AAILs and ß-CD in NACE. Several interesting results were observed compared with previously reported chiral ILs-related aqueous CE studies. In particular, the direct enantioselectivity of TAA-AAILs was observed for the first time by using it as sole chiral selector in NACE. This was an encouraging finding because it was the first direct and convincing evidence that AAILs were able to participate in the enantiorecognition process in the conventional chiral selectors-based synergistic systems. The new TAA-AAILs synergistic NACE system was further optimized in terms of alkyl chain length, TAA-AAILs concentration, ß-CD concentration, electrolyte composition and applied voltage, etc. Best enantioseparations of Dns-AAs were obtained when 100 mM ß-CD and 10 mM tetramethylammonium-l-arginine (TMA-l-Arg) were added in an NMF buffer containing 50 mM Tris and 35 mM CA (apparent pH 7.85) under UV detection. The applied voltage was set at 30 kV. The method was then successfully employed for the determination of enantiomeric impurities of a real AA sample. This work proved that the use of chiral ILs as additives in NACE is a promising approach for enantioseparation.


Assuntos
Eletroforese Capilar/métodos , Líquidos Iônicos/química , Arginina/análogos & derivados , Arginina/química , Tampões (Química) , Eletrólitos/química , Concentração de Íons de Hidrogênio , Simulação de Acoplamento Molecular , Compostos de Amônio Quaternário/química , Estereoisomerismo , beta-Ciclodextrinas/química
7.
Spectrochim Acta A Mol Biomol Spectrosc ; 224: 117411, 2020 Jan 05.
Artigo em Inglês | MEDLINE | ID: mdl-31362187

RESUMO

The present study delves into the interaction of a potent cancer-cell photosensitizer Norharmane (NHM) with non-ionic triblock copolymer P123, followed by the assessment of the stability of the formed complex in the presence of ß-cyclodextrin (ß-CD). Spectroscopic results unveil the modulation of the prototropic equilibrium of NHM within the constrained microheterogeneous medium of the copolymer micelle to be favoured towards the neutral species of NHM over the cationic counterpart; which has been aptly rationalized invoking the key role of hydrophobic interaction in the association process and is further reinforced from steady-state and time-resolved spectroscopic measurements. The micropolarity of the probe-binding site has been evaluated by the archetypal ET(30) analysis revealing that the cationic probe remains in the corona region of the micelle instead of penetrating deeper into the micellar core. Moreover, the effect of ß-CD on the stability of the NHM-bound P123 aggregates has also been investigated, revealing that ß-CD can be used as a potential host for the release of the micelle-encapsulated drug through an inclusion complex formation with the P123 monomers. The result is expected to be of potential interest from medical perspective owing to the context of efficient drug release at their potential sites.


Assuntos
Antineoplásicos , Micelas , Fármacos Fotossensibilizantes , beta-Ciclodextrinas/química , Antineoplásicos/análise , Antineoplásicos/química , Antineoplásicos/farmacocinética , Liberação Controlada de Fármacos , Modelos Moleculares , Fármacos Fotossensibilizantes/análise , Fármacos Fotossensibilizantes/química , Fármacos Fotossensibilizantes/farmacocinética , Espectrometria de Fluorescência
8.
Food Chem ; 303: 125419, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31470276

RESUMO

ß-Cyclodextrin- and 2-hydroxypropyl-ß-cyclodextrin/Danube common nase (Chondrostoma nasus L.) oil complexes (ß-CD- and HP-ß-CD/CNO) have been obtained for the first time. The fatty acid (FA) profile of the CNO indicates an important content of polyunsaturated fatty acids, the most important being eicosapentaenoic acid (EPA, 6.3%) and docosahexaenoic acid (DHA, 1.6%), both ω-3 FAs. The complexes have been obtained by kneading method. The moisture content and successful of molecular encapsulation have been evaluated by thermal and spectroscopic techniques. Thermogravimetry and differential scanning calorimetry analyses reveals that the moisture content of CD/CNO complexes significantly decreased, compared to starting CDs. On the other hand, the crystallinity index was for the first time determined for such type of complexes, the ß-CD/CNO complex having values of 43.9(±18.3)%, according to X-ray diffractometry. FA profile and CD/CNO characteristics sustain the use of these ω-3 based complexes for food supplements or functional food products, but further studies are needed.


Assuntos
2-Hidroxipropil-beta-Ciclodextrina/química , Óleos de Peixe/química , beta-Ciclodextrinas/química , Animais , Varredura Diferencial de Calorimetria , Cyprinidae , Solubilidade , Difração de Raios X
9.
Chemosphere ; 240: 124948, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-31726616

RESUMO

Zearalenone is a xenoestrogenic mycotoxin produced by Fusarium species. High exposure with zearalenone induces reproductive disorders worldwide. Cyclodextrins are ring-shaped host molecules built up from glucose units. The apolar cavity of cyclodextrins can entrap so-called guest molecules. The formation of highly stable host-guest type complexes with cyclodextrins can decrease the biological effect of the guest molecule. Therefore, cyclodextrins may be suitable to decrease the toxicity of some xenobiotics even after the exposure. In this study, the protective effect of beta-cyclodextrins against zearalenone-induced toxicity was investigated in HeLa cells and zebrafish embryos. Fluorescence spectroscopic studies demonstrated the formation of stable complexes of zearalenone with sulfobutyl-, methyl-, and succinyl-methyl-substituted beta-cyclodextrins at pH 7.4 (K = 1.4-4.7 × 104 L/mol). These chemically modified cyclodextrins considerably decreased or even abolished the zearalenone-induced loss of cell viability in HeLa cells and mortality in zebrafish embryos. Furthermore, the sublethal effects of zearalenone were also significantly alleviated by the co-treatment with beta-cyclodextrins. To test the estrogenic effect of the mycotoxin, a transgenic bioindicator zebrafish model (Tg(vtg1:mCherry)) was also applied. Our results suggest that the zearalenone-induced vitellogenin production is partly suppressed by the hepatotoxicity of zearalenone in zebrafish. This study demonstrates that the formation of stable zearalenone-cyclodextrin complexes can strongly decrease or even abolish the zearalenone-induced toxicity, both in vitro and in vivo. Therefore, cyclodextrins appear as promising new mycotoxin binders.


Assuntos
Substâncias Protetoras/farmacologia , Zearalenona/toxicidade , Peixe-Zebra/embriologia , beta-Ciclodextrinas/farmacologia , Animais , Ciclodextrinas/química , Estrogênios/farmacologia , Células HeLa/efeitos dos fármacos , Humanos , Micotoxinas/metabolismo , Substâncias Protetoras/química , Reprodução/efeitos dos fármacos , beta-Ciclodextrinas/química , beta-Ciclodextrinas/metabolismo
10.
Chem Commun (Camb) ; 56(7): 1042-1045, 2020 Jan 23.
Artigo em Inglês | MEDLINE | ID: mdl-31868189

RESUMO

A novel enzyme-responsive supramolecular polysaccharide assembly composed of disulfide linked adamantane-naphthalimide fluorescent camptothecin prodrug (AdaCPT) and ß-CD modified hyaluronic acid (HACD) was constructed, possessing low cellular cytotoxicity and exhibiting targeted cellular imaging and controlled drug release at specific sites while providing a concurrent means for the real-time tracking of drug delivery.


Assuntos
Antineoplásicos/farmacologia , Camptotecina/farmacologia , Portadores de Fármacos/química , Corantes Fluorescentes/farmacologia , Pró-Fármacos/farmacologia , Adamantano/análogos & derivados , Adamantano/síntese química , Adamantano/farmacologia , Adamantano/toxicidade , Animais , Antineoplásicos/síntese química , Antineoplásicos/toxicidade , Camptotecina/síntese química , Camptotecina/toxicidade , Liberação Controlada de Fármacos , Corantes Fluorescentes/síntese química , Corantes Fluorescentes/toxicidade , Células HCT116 , Humanos , Ácido Hialurônico/química , Camundongos , Microscopia Confocal/métodos , Microscopia de Fluorescência/métodos , Células NIH 3T3 , Naftalimidas/síntese química , Naftalimidas/farmacologia , Naftalimidas/toxicidade , Pró-Fármacos/síntese química , Pró-Fármacos/toxicidade , beta-Ciclodextrinas/química
11.
Talanta ; 207: 120315, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31594591

RESUMO

In this paper, silver nanoclusters (AgNCs) were synthesized by one facile, low-cost and green method with histidine acting as the stabilizer and ascorbic acid performing as reducing agent. AgNCs displayed excellent fluorescence property and good biocompatibility and were further functionalized by ß-cyclodextrin (CD-AgNCs) for the highly sensitive detection of alkaline phosphatase (ALP) activity. ALP catalyzed the dephosphorylation of p-nitrophenylphosphate (NPP) to produce p-nitrophenol (NP), and NP can effectively quench the fluorescence of CD-AgNCs via the inner filter effect (IFE) due to the UV-vis absorption spectrum of NP had considerable overlap with the excitation spectrum of CD-AgNCs. Benefiting from the IFE and the host-guest interaction between CD and NP, this CD-AgNCs based system for ALP activity analysis displayed a good linear range of 0.02-10.0 U L-1 and the detection limit as low as 0.0046 U L-1. In addition, this proposed strategy also showed satisfactory performance for ALP analysis in human serum samples and bioimaging of intracellular ALP in living cells, indicating the great application prospect of this system for ALP activity analysis in medical related researches.


Assuntos
Fosfatase Alcalina/metabolismo , Espaço Intracelular/enzimologia , Limite de Detecção , Nanoestruturas/química , Imagem Óptica/métodos , Prata/química , beta-Ciclodextrinas/química , Adulto , Humanos , Células MCF-7
12.
Chem Commun (Camb) ; 56(2): 313-316, 2019 Dec 19.
Artigo em Inglês | MEDLINE | ID: mdl-31808779

RESUMO

A host-guest recognition-regulated aggregation-induced emission (AIE) strategy is developed based on the interaction between cyclodextrin-functionalized copper nanoclusters and di(adamantan-1-yl)phosphine as a connector, which significantly improves the AIE efficiency and stability and can be applied to long-term in situ imaging of MUC1 protein.


Assuntos
Adamantano/análogos & derivados , Nanopartículas Metálicas/química , Mucina-1/análise , Fosfinas/química , beta-Ciclodextrinas/química , Linhagem Celular Tumoral , Cobre/química , Corantes Fluorescentes/química , Humanos , Medições Luminescentes/métodos , Microscopia Confocal/métodos
14.
Polim Med ; 49(1): 35-43, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31769938

RESUMO

BACKGROUND: Poorly water-soluble drugs do not dissolve well in aqueous-based gastrointestinal fluid; therefore, they are not well absorbed. Thus, employing a suitable solubility enhancing technique is necessary for such a drug. Drug/HP­ß­CD complexation is a promising way to improve solubility and dissolution of a poorly water-soluble drug. Levodropropizine was used as a model drug in this study. OBJECTIVES: The purpose of this research was to enhance the aqueous solubility and dissolution rate of levodropropizine by employing the inclusion complexation technique. MATERIAL AND METHODS: A microparticle formulation was prepared from levodropropizine and hydroxypropyl-ß-cyclodextrin (HP­ß­CD) in a 1:1 molar ratio through the spray-drying technique. The host-guest relationship between levodropropizine and HP­ß­CD was also investigated using the molecular docking computational methodology. The aqueous solubility and dissolution rate of levodropropizine in formulations were assessed and compared with those of the drug alone. X-ray diffraction (XRD), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), and Fourier transform infrared spectroscopy (FTIR) were applied for the solid-state characterization of the prepared samples. RESULTS: According to the research outcomes, the levodropropizine/HP­ß­CD formulation had enhanced the aqueous solubility (351.12 ±13.26 vs 92.76 ±5.00 mg/mL) and dissolution rate (97.83 ±3.36 vs 3.12 ±1.76% in 10 min) of levodropropizine, compared to the plain drug powder. The levodropropizine/ HP­ß­CD formulation had converted the crystalline drug into its amorphous counterpart. Furthermore, no covalent interaction was found to exist between levodropropizine and HP­ß­CD. The spray-dried particles were discrete. Each particle had a shriveled appearance. CONCLUSIONS: The levodropropizine/HP­ß­CD formulation is, therefore, recommended for the more effective administration of levodropropizine through the oral route.


Assuntos
Propilenoglicóis , beta-Ciclodextrinas , 2-Hidroxipropil-beta-Ciclodextrina , Varredura Diferencial de Calorimetria , Microscopia Eletrônica de Varredura , Simulação de Acoplamento Molecular , Propilenoglicóis/química , Propilenoglicóis/farmacologia , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , beta-Ciclodextrinas/química , beta-Ciclodextrinas/farmacologia
16.
Chem Commun (Camb) ; 55(96): 14466-14469, 2019 Nov 28.
Artigo em Inglês | MEDLINE | ID: mdl-31728462

RESUMO

We report a supramolecular photo-responsive antibiotic (azobenzene-norfloxacin/αCD). This supramolecule exhibited a higher "on-off" ratio of antibacterial ability than azobenzene-norfloxacin alone under UV irradiation. It offers an approach to efficiently regulate the activity of antibiotics by combining the supramolecular and light-regulating strategies together.


Assuntos
Antibacterianos/química , Compostos Azo/química , beta-Ciclodextrinas/química , Antibacterianos/farmacologia , Bactérias/efeitos dos fármacos , Farmacorresistência Bacteriana/efeitos dos fármacos , Isomerismo , Norfloxacino/química , Norfloxacino/farmacologia , Temperatura Ambiente , Raios Ultravioleta
17.
Life Sci ; 239: 116961, 2019 Dec 15.
Artigo em Inglês | MEDLINE | ID: mdl-31654745

RESUMO

Neuropathic pain (NP) is a difficult condition to treat because of the modest efficacy of available drugs. New treatments are required. In the study we aimed to investigate the effects of the essential oil from Lippia grata alone or complexed in ß-cyclodextrin (LG or LG-ßCD) on persistent inflammatory and neuropathic pain in a mouse model. We also investigated Ca2+ currents in rat dorsal root ganglion (DRG) neurons. Male Swiss mice were treated with LG or LG/ß-CD (24 mg/kg, i.g.) and their effect was evaluated using an acute inflammatory pleurisy model and nociception triggered by intraplantar injection of an agonist of the TRPs channels. We also tested their effect in chronic pain models: injection of Freund's Complete Adjuvant and partial sciatic nerve ligation (PSNL). In the pleurisy model, LG reduced the number of leukocytes and the levels of TNF-α and IL-1ß. It also inhibited cinnamaldehyde and menthol-induced nociceptive behavior. The pain threshold in mechanical and thermal hyperalgesia was increased and paw edema was decreased in models of inflammatory and neuropathic pain. PSNL increased inflammatory protein contents and LG and LG-ßCD restored the protein contents of TNF-α, NF-κB, and PKA, but not IL-1ß and IL-10. LG inhibited voltage gated Ca2+ channels from DRG neurons. Our results suggested that LG or LG-ßCD produce anti-hyperalgesic effect in chronic pain models through reductions in TNF-α levels and PKA, and inhibited voltage-gated calcium channels and may be innovative therapeutic agents for the management of NP.


Assuntos
Hiperalgesia/tratamento farmacológico , Lippia/metabolismo , beta-Ciclodextrinas/farmacologia , Animais , Dor Crônica/tratamento farmacológico , Modelos Animais de Doenças , Gânglios Espinais/efeitos dos fármacos , Hiperalgesia/metabolismo , Masculino , Camundongos , Neuralgia/tratamento farmacológico , Nociceptividade/efeitos dos fármacos , Óleos Voláteis/farmacologia , Dor/tratamento farmacológico , Dor/metabolismo , Medição da Dor/efeitos dos fármacos , Limiar da Dor/efeitos dos fármacos , Extratos Vegetais/farmacologia , Ratos , Ratos Wistar , beta-Ciclodextrinas/metabolismo
18.
Int J Nanomedicine ; 14: 7017-7038, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31564863

RESUMO

Background: Fabrication of a smart drug delivery system that could dramatically increase the efficiency of chemotherapeutic drugs and reduce the side effects is still a challenge for pharmaceutical researchers. By the emergence of nanotechnology, a huge window was opened towards this goal, and a wide type of nanocarriers were introduced for delivering the chemotherapeutic to the cancer cells, among them are cyclodextrins with the ability to host different types of hydrophobic bioactive molecules through inclusion complexation process. Aim: The aim of this study is to design and fabricate a pH-responsive theranostic nanocapsule based on cyclodextrin supramolecular nano-structure. Materials and methods: This nanostructure contains iron oxide nanoparticles in the core surrounded with three polymeric layers including polymeric ß-cyclodextrin, polyacrylic acid conjugated to sulfadiazine, and polyethylenimine functionalized with ß-cyclodextrin. Sulfadiazine is a pH-responsive hydrophobic component capable of making inclusion complex with ß-cyclodextrin available in the first and third layers. Doxorubicin, as an anti-cancer drug model, was chosen and the drug loading and release pattern were determined at normal and acidic pH. Moreover, the biocompatibility of the nanocapsule (with/without drug component) was examined using different techniques such as MTT assay, complement activation, coagulation assay, and hemolysis. Results: The results revealed the successful preparation of a spherical nanocapsule with mean size 43±1.5 nm and negatively charge of -43 mV that show 160% loading efficacy. Moreover, the nanocapsule has an on/off switching release pattern in response to pH that leads to drug released in low acidic pH. The results of the biocompatibility tests indicated that this nano drug delivery system had no effect on blood and immune components while it could affect cancer cells even at very low concentrations (0.3 µg mL-1). Conclusion: The obtained results suggest that this is a "switchable" theranostic nanocapsule with potential application as an ideal delivery system for simultaneous cancer diagnosis and therapy.


Assuntos
Nanocápsulas/química , Polietilenoimina/química , Nanomedicina Teranóstica , beta-Ciclodextrinas/química , Animais , Doxorrubicina/química , Doxorrubicina/farmacologia , Sistemas de Liberação de Medicamentos , Liberação Controlada de Fármacos , Compostos Férricos/química , Hemólise/efeitos dos fármacos , Humanos , Concentração de Íons de Hidrogênio , Células MCF-7 , Camundongos , Nanocápsulas/ultraestrutura , Tempo de Tromboplastina Parcial , Tempo de Protrombina , Eletricidade Estática , Compostos de Sulfidrila/síntese química , Compostos de Sulfidrila/química , Difração de Raios X , beta-Ciclodextrinas/síntese química
19.
Drugs Today (Barc) ; 55(9): 537-544, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31584571

RESUMO

On March 19, 2019, the United States Food and Drug Administration (FDA) approved Zulresso (brexanolone) for intravenous use for the treatment of postpartum depression (PPD) in adult women. The decision was based on three recent clinical trials following an FDA priority review and breakthrough therapy designation. Brexanolone is now available through a restricted process called the Zulresso Risk Evaluation and Mitigation Strategy Program that requires the drug to be administered by a healthcare provider in a certified healthcare facility. Brexanolone represents an important new treatment option to address treatment-resistant depressive symptoms. In this article, we discuss the current critical need for PPD treatments, the mechanisms of brexanolone action, and the efficacy and drug safety studies that led to FDA approval. Additionally, we discuss some limitations of the current formulation, specific populations of women that might benefit from this treatment, and how new drugs on the horizon may increase the ability to treat PPD in a variety of patient populations.


Assuntos
Depressão Pós-Parto/tratamento farmacológico , Pregnanolona/uso terapêutico , beta-Ciclodextrinas/uso terapêutico , Aprovação de Drogas , Combinação de Medicamentos , Feminino , Humanos , Estados Unidos , United States Food and Drug Administration
20.
J Agric Food Chem ; 67(43): 11931-11941, 2019 Oct 30.
Artigo em Inglês | MEDLINE | ID: mdl-31589419

RESUMO

Lipid-based delivery systems (LBDSs) are widely applied in pharmaceuticals and health care because of the increased bioavailability of lipophilic components when they are coadministered with high-fat meals. However, how to accurately control their in vivo release and stability is still challenging. Here, after introducing the simple esterification and coprecipitation, we created the dual-functional composite ODS-ß-CD-VE by the coassembly of ß-cyclodextrin (ß-CD), octadecenyl succinic anhydride (ODSA), and vitamin E (VE). The resulting dual-functional particle presented a uniform sheetlike shape and nanometer size. In addition, its chemical structure was clarified in detail via nuclear magnetic resonance (NMR), Fourier transform infrared spectroscopy (FTIR), and X-ray diffraction (XRD). Benefiting from the antioxygenation of VE, lipid oxidation in the ODS-ß-CD-VE-stabilized Pickering emulsion was effectively inhibited. Meanwhile, pH-induced protonation/deprotonation of carboxyl groups guaranteed that the emulsions kept steady at pH ≤4 but were unsteady under neutral conditions. In this way, the lipids contained in the emulsion were protected from gastric juice and then digested and accurately released as n-3 polyunsaturated fatty acids (PUFA) in the simulated intestine environment. This strategy sheds some light on the rational and efficient construction of LBDSs for nutrient supplements and even pharmaceuticals in a living digestive tract.


Assuntos
Preparações de Ação Retardada/química , Ácidos Graxos Insaturados/química , Vitamina E/química , beta-Ciclodextrinas/química , Preparações de Ação Retardada/metabolismo , Digestão , Emulsões/química , Ácidos Graxos Insaturados/metabolismo , Trato Gastrointestinal/metabolismo , Humanos , Concentração de Íons de Hidrogênio , Modelos Biológicos
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