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2.
Pharm Res ; 36(10): 139, 2019 Jul 29.
Artigo em Inglês | MEDLINE | ID: mdl-31359156

RESUMO

PURPOSE: To identify the minimum interfacial bonding strength (IBS) required for bilayer tablets to sustain the stresses experienced during manufacturing, transportation, and handling. METHODS: Bilayer tablets of a number of formulations with systematically varied IBS were prepared on a materials testing macine. Five bilayer tablets with the same IBS were repeatedly dropped at a fixed height in a friabilator and integrity of the interface was periodically examined. The number of tablets free from observable defects at the interface was plotted as a function of the number of drops. The IBS for all five tablets to remain intact after 1000 drops was taken as the minimum IBS for a given formulation. RESULTS: The minimum IBS depends on both layer composition and tablet size. For bilayer tablets made with more brittle materials or a larger size, a higher minimum IBS is required to pass the survival test. The incorporation of HPMC leads to a lower minimum IBS. An IBS of 0.26 MPa is sufficient for all bilayer tablet formulations and sizes to pass the survival test in this work. CONCLUSIONS: A minimum IBS of 0.26 MPa is recommended as a tentative criterion for bilayer tablets of most materials to avoid quality issues arising from inadequate IBS.


Assuntos
Excipientes/química , Comprimidos/química , Celulose/química , Composição de Medicamentos/métodos , Estabilidade de Medicamentos , Lactose/química , Tamanho da Partícula , Estresse Mecânico , Propriedades de Superfície , Resistência à Tração
3.
J Agric Food Chem ; 67(33): 9220-9231, 2019 Aug 21.
Artigo em Inglês | MEDLINE | ID: mdl-31347838

RESUMO

Slow-release fungicide formulations (azoxystrobin, epoxiconazole, and tebuconazole) shaped as pellets and granules in a matrix of biodegradable poly(3-hydroxybutyrate) and natural fillers (clay, wood flour, and peat) were constructed. Infrared spectroscopy showed no formation of chemical bonds between components in the experimental formulations. The formulations of pesticides had antifungal activity against Fusarium verticillioides in vitro. A study of biodegradation of the experimental fungicide formulations in the soil showed that the degradation process was mainly influenced by the type of formulation without significant influence of the type of filler. More active destruction of the granules led to a more rapid accumulation of fungicides in the soil. The content of fungicides present in the soil as a result of degradation of the formulations and fungicide release was determined by their solubility. Thus, all formulations are able to function in the soil for a long time, ensuring gradual and sustained delivery of fungicides.


Assuntos
Argila/química , Preparações de Ação Retardada/química , Composição de Medicamentos/métodos , Fungicidas Industriais/química , Hidroxibutiratos/química , Poliésteres/química , Solo/química , Madeira/química , Preparações de Ação Retardada/farmacologia , Portadores de Fármacos/química , Composição de Medicamentos/instrumentação , Compostos de Epóxi/química , Compostos de Epóxi/farmacologia , Fungicidas Industriais/farmacologia , Fusarium/efeitos dos fármacos , Cinética , Pirimidinas/química , Pirimidinas/farmacologia , Estrobilurinas/química , Estrobilurinas/farmacologia , Triazóis/química , Triazóis/farmacologia
4.
Food Chem ; 298: 125045, 2019 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-31261002

RESUMO

In this study, sacha inchi oil (SIO) (Plukenetia volubilis L.) was microencapsulated via complex coacervation of ovalbumin (OVA) and sodium alginate (AL), and the microcapsule properties were characterized. The omega-3 content in the SIO was evaluated after in vitro gastric simulation and microencapsulation. The coacervate complex between OVA and AL was evaluated based on electrostatic interactions and developed for use as a wall material via the SIO microencapsulation process. The best mass ratio for the biopolymers (OVA:AL) was 4:1 at pH 3.8, and the complex exhibited a thermal resistance at 189.86 °C. The SIO microcapsules showed a high encapsulation efficiency of approximately 94.12% in the ratio (OVA:AL) of 1:1. Furthermore, microencapsulated SIO presented resistance under gastric conditions with a low release of acyl (ω-3) units. These results demonstrate that it is possible to use OVA:AL as encapsulating agents to protect bioactive compounds and to improve the thermal behavior of microcapsules.


Assuntos
Composição de Medicamentos/métodos , Euphorbiaceae/metabolismo , Óleos Vegetais/química , Alginatos/química , Varredura Diferencial de Calorimetria , Cápsulas/química , Euphorbiaceae/química , Ácidos Graxos Ômega-3/química , Concentração de Íons de Hidrogênio , Ovalbumina/química , Eletricidade Estática
5.
Zhongguo Zhong Yao Za Zhi ; 44(13): 2785-2791, 2019 Jul.
Artigo em Chinês | MEDLINE | ID: mdl-31359691

RESUMO

Extrusion-spheronisation method was used to prepare Rhus chinensis total phenolic acid pellets. The formula and preparation of R. chinensis total phenolic acid pellets were optimized. The formulas( drug loading capacity,diluent,wetting agent and anti-sticking agent) were determined by the single factor test with yield,appearance and performance as the indexes. The preparation was optimized by Box-Behnken design and response surface method,with the rate of extrusion,rate of spheronization and time of spheronization as the independent variables and the overall desirability value of yield,friability and roundness as the dependent variables. The optimal formula of pellets was as follows: drug loading capacity 28. 7%,MCC-lactose 9 ∶1,silicon dioxide as anti-sticking agent,and 60% ethanol as wetting agent. The optimal preparation was determined as follows: the rate of extrusion was 43 r·min-1,the rate of spheronization was 1 800 r·min-1,and the time of spheronization was 4 min. The absolute deviation between predicted value and estimated value under the conditions was less than 5. 0%,with a high degree of model fit. The preparation parameters obtained were accurate,reliable and reproducible. Under scanning electron microscopy( SEM),R. chinensis total phenolic acid pellets were uniform in diameter,round and smooth. The optimal formulation and process are stable and feasible for preparing R. chinensis total phenolic acid pellets.


Assuntos
Composição de Medicamentos/métodos , Hidroxibenzoatos/química , Rhus/química , Tamanho da Partícula , Solubilidade
6.
Plant Foods Hum Nutr ; 74(3): 334-341, 2019 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-31175546

RESUMO

The aim of the study was to investigate the potential of using ß-glucan as wall material to microencapsulate the elderberry extract. Firstly, the extract was obtained by the water-acetone extraction method to extract mainly anthocyanins from ground dried fruits. The extract was mixed with wall materials: maltodextrin-ß-glucan mixture and the control sample as a widely used combination of maltodextrin and arabic gum (92.5:7.5). In the examined samples the content of ß-glucan was 0.5, 1, 2 and 3%. Properties of encapsulated extracts of final powders were measured using particle size and morphology, encapsulation efficiency, color measurement, total anthocyanin and ascorbic acid content (TAC and TAAC) methods. Our results indicated that the ß-glucan wall material samples had higher process quality compared to control samples. Addition of ß-glucan insignificantly decreases encapsulation efficiency. Among powders with ß-glucan content, the powder with 1% ß-glucan content was characterized by the smallest (24 µm) particle size. The sample with 2% ß-glucan content had the highest water solubility and polydispersity index. Due to the encapsulation efficiency, moisture content, and water solubility index, the optimum condition of microencapsulation process for elderberry extract was for samples with 0.5% ß-glucan as wall material content. To conclude, due to high molecular weight of ß-glucan the higher than 0.5% ratio of ß-glucan is not recommended for spray-drying method. However, small quantity of health-beneficial ß-glucan could act as potential encapsulation agent in clean label products to replace Arabic gum.


Assuntos
Antocianinas/análise , Ácido Ascórbico/análise , Composição de Medicamentos/métodos , Extratos Vegetais/química , Sambucus nigra/química , beta-Glucanas/química , Dessecação , Frutas/química , Goma Arábica/química , Tamanho da Partícula , Polissacarídeos/química , Pós , Solubilidade , Água/química
7.
J Nanobiotechnology ; 17(1): 77, 2019 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-31226993

RESUMO

BACKGROUND: The design of efficient drug delivery vectors requires versatile formulations able to simultaneously direct a multitude of molecular targets and to bypass the endosomal recycling pathway of cells. Liposomal-based vectors need the decoration of the lipid surface with specific peptides to fulfill the functional requirements. The unspecific binding of peptides to the lipid surface is often accompanied with uncontrolled formulations and thus preventing the molecular mechanisms of a successful therapy. RESULTS: We present a simple synthesis pathway to anchor cysteine-terminal peptides to thiol-reactive lipids for adequate and quantitative liposomal formulations. As a proof of concept, we have synthesized two different lipopeptides based on (a) the truncated Fibroblast Growth Factor (tbFGF) for cell targeting and (b) the pH sensitive and fusogenic GALA peptide for endosomal scape. CONCLUSIONS: The incorporation of these two lipopeptides in the liposomal formulation improves the fibroblast cell targeting and promotes the direct delivery of cargo molecules to the cytoplasm of the cell.


Assuntos
Dissulfetos/química , Lipídeos/química , Peptídeos/química , Piridinas/química , Animais , Sobrevivência Celular/efeitos dos fármacos , Cisteína/química , Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos , Endossomos/metabolismo , Humanos , Concentração de Íons de Hidrogênio , Lipossomos/química , Camundongos , Estrutura Molecular , Imagem Óptica/métodos , Estudo de Prova de Conceito
8.
Semin Ophthalmol ; 34(4): 218-222, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31146619

RESUMO

Clinical pharmacology training for clinicians typically focuses on a drug's Active Pharmaceutical Ingredient. However, pharmaceutical formulation, the process of optimizing manufacturing methods and excipients to make a final drug product, is a critical process in determining whether a potential drug can become a realistic, routinely used therapeutic agent. This review focuses on the formulation methods used in commonly prescribed retina drug products.


Assuntos
Composição de Medicamentos/métodos , Sistemas de Liberação de Medicamentos/métodos , Preparações Farmacêuticas/administração & dosagem , Doenças Retinianas/tratamento farmacológico , Humanos , Lipossomos/química , Nanopartículas/química , Fosfolipídeos/química
9.
AAPS PharmSciTech ; 20(5): 208, 2019 Jun 03.
Artigo em Inglês | MEDLINE | ID: mdl-31161450

RESUMO

Individualized medicines for pediatrics are a useful alternative if there is no correct dosage marketed for this segment (easy to swallow, adequate volume and content, correct composition for pediatrics, good organoleptic properties, etc.). Its validation process must ensure quality testing: its content uniformity, physical (homogeneity after shaking), chemical, and microbiological stability. Some of these attributes are checked by the recommendations of European Pharmacopoeia (Ph. Eur.), International Conference of Harmonization (ICH), and National Formularies but others are not. The aim of this study is to develop a general high-demanding strategy to ensure the final quality of liquid dosage forms testing and developing standard operating processes (SOPs) for the elaboration of individualized oral liquid medicines for pediatric use. Furosemide was used as an example of the validation of an individualized liquid solution for pediatric use. Three SOPs were selected according to their composition and the recommendations of liquid dosage forms for pediatric use. Quality attributes according to National Formularies, Ph. Eur., and ICH were tested: pH, organoleptic properties, uniformity of mass of delivered dose from multidose containers, and chemical stability. In this study, a general high-demanding strategy was elaborated to validate oral liquid dosage forms, including validation of the analytical method used to test their quality. A second part focuses on the elaboration of liquid formulations for pediatrics with the highest standards of quality taking into account CQAs that were not contemplated by official compendial such as content uniformity and physical stability.


Assuntos
Excipientes/normas , Furosemida/normas , Pediatria/normas , Medicina de Precisão/normas , Administração Oral , Criança , Diuréticos/administração & dosagem , Diuréticos/normas , Composição de Medicamentos/métodos , Composição de Medicamentos/normas , Excipientes/administração & dosagem , Furosemida/administração & dosagem , Humanos , Pediatria/métodos , Soluções Farmacêuticas/administração & dosagem , Soluções Farmacêuticas/normas , Medicina de Precisão/métodos
10.
J Food Sci ; 84(6): 1592-1599, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31162880

RESUMO

The purpose of this study was to produce and characterize an inclusion complex between ß-cyclodextrin (ß-CD) and Exocarpium Citri Grandis essential oil (EEO), and to evaluate its antioxidant properties. The volatile compounds of EEO were characterized by gas chromatography-mass spectrometer. A comparison of the ß-CD, EEO, and the physical mixture with the inclusion complex revealed differences in their thermal stabilities and morphologies, which confirmed the formation of the ß-CD-EEO inclusion complex. Complexed with ß-CD, the ß-CD-EEO inclusion complex showed a higher stability and antioxidant activity when compared with physical mixture and EEO. Therefore, ß-CD can be used to form inclusion complexes with EEO to expand its potential applications in the food and drug industries. PRACTICAL APPLICATION: Exocarpium Citri Grandis is rich in essential oil and other ingredients. The optimized extraction, constituent composition, and encapsulation of EEO in ß-CD were investigated in this study. The results showed that the encapsulation process increased the antioxidant activity and stability of EEO, which provides both fundamental and practical knowledge for the application of EEO in the food and drug industries.


Assuntos
Antioxidantes/química , Citrus/química , Composição de Medicamentos/métodos , Óleos Voláteis/química , Estabilidade de Medicamentos , Frutas/química , beta-Ciclodextrinas/química
11.
J Agric Food Chem ; 67(26): 7506-7511, 2019 Jul 03.
Artigo em Inglês | MEDLINE | ID: mdl-31184879

RESUMO

The poor water solubility and oral bioavailability of many lipophilic polyphenols can be improved through the use of colloidal delivery systems. In this study, a pH-driven method was used to encapsulate curcumin, quercetin, and resveratrol within nanoliposomes. This method is based on the decrease in water-solubility of certain polyphenols when they move from alkaline to acid conditions. However, the chemical stability of some polyphenols is relatively poor under alkaline conditions. For this reason, the impact of pH on the chemical degradation of the three polyphenols was studied. The polyphenols were then encapsulated within nanoliposomes using the pH-driven method and the encapsulation efficiency (EE) and chemical stability were determined. The EE of curcumin, quercetin, and resveratrol in the nanoliposomes was 100, 54, and 93%, respectively. Differences in the EE were mainly attributed to differences in their stability under alkaline conditions. Our results show that the application of this method to other lipophilic polyphenols depends on the impact of pH on their solubility and chemical stability, which needs to be established on a case-by-case basis.


Assuntos
Composição de Medicamentos/métodos , Lipossomos/química , Nanopartículas/química , Polifenóis/química , Disponibilidade Biológica , Curcumina/química , Portadores de Fármacos/química , Concentração de Íons de Hidrogênio , Quercetina/química , Resveratrol/química , Solubilidade
12.
Pharm Res ; 36(8): 120, 2019 Jun 18.
Artigo em Inglês | MEDLINE | ID: mdl-31214939

RESUMO

PURPOSE: The first pressurised metered dose inhaler (pMDI) was introduced in 1956. Even with excellent inhaler technique typically only 20% of the dose deposits in the lungs where needed. It is hoped that a better understanding of the initial plume formation and expansion during dose release can help improve modelling, devices and ultimately transport to the lungs. We have used two high-speed imaging techniques to investigate the transient dose event. METHODS: Synchrotron phase-contrast X-Ray imaging is a technique that is sensitive to variations in the refractive index of materials in the X-ray region. Similarly, Schlieren imaging is an optical technique sensitive to the refractive index gradients which are often present in pMDI plumes due to gas density variations. We have combined and synchronised both techniques to investigate three commercial pMDIs actuators during dose release for various actuator/formulation combinations. RESULTS: We have observed temporal phases of propellant flowing in the orifice channel. At early times flash boiling takes place and drives gas emission, steep plume density gradients and liquid jets/droplets at the orifice. Evaporating liquid is present in the sump long after the dose is finished. Regional counter-flow is seen in plumes emitted into a mouth-throat geometry. CONCLUSIONS: As the foamy liquid-vapour mixture is forced out of the sump and into the orifice the liquid walls of the bubbles break into fragments which are forced out of the sump and tend to form a liquid-gas flow in the orifice channel. The period of high density plume observed by the schlieren technique corresponds to flash-boiling-driven liquid exiting the orifice channel.


Assuntos
Inaladores Dosimetrados , Administração por Inalação , Aerossóis , Composição de Medicamentos/métodos , Desenho de Equipamento/instrumentação , Etanol/química , Humanos , Cinética , Boca , Imagem Óptica/métodos , Faringe , Raios X
13.
Pharm Res ; 36(8): 122, 2019 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-31218556

RESUMO

PURPOSE: A non-propellant based foam (NPF) system was developed incorporating the antibiotics, pectin capped green nano-silver and sulfadiazine (SD) for the topical treatment of burn wounds as a convenient alternative to the existing therapies. METHODS: NPF were prepared using various surfactants and oils forming a nanoemulsion. Anti-microbial studies by resazurin microtitre assay, ex vivo diffusion, in vivo skin permeation and deposition studies, and acute irritation studies were carried out. NPF was applied onto secondary thermal wounds manifested on mice models followed by macroscopic and histological examinations. RESULTS: NPF had an average globule size of <75 nm. The viscosity was ~10 cP indicating the feasibility of expulsion from the container upon actuation. With no skin irritation, the foams showed a higher skin deposition of SD. A high contraction and an evident regeneration of the skin tissue upon treatment with NPF indicated a good recovery from the thermal injury was apparent from the histology studies. CONCLUSION: NPF represents an alternative topical formulation that can be employed as a safe and effective treatment modality for superficial second degree (partial thickness) burn wounds. With a minimal requirement of mechanical force, the no-touch application of NPF makes it suitable for sensitive and irritant skin surfaces.


Assuntos
Antibacterianos/farmacologia , Queimaduras/tratamento farmacológico , Nanopartículas Metálicas/química , Prata/química , Sulfadiazina/farmacologia , Cicatrização/efeitos dos fármacos , Administração Tópica , Animais , Antibacterianos/administração & dosagem , Queimaduras/patologia , Queimaduras/fisiopatologia , Composição de Medicamentos/métodos , Quimioterapia Combinada , Emulsões , Escherichia coli/efeitos dos fármacos , Química Verde , Humanos , Masculino , Camundongos , Óleos/química , Tamanho da Partícula , Permeabilidade , Pele/efeitos dos fármacos , Pele/patologia , Pele/fisiopatologia , Staphylococcus aureus/efeitos dos fármacos , Sulfadiazina/administração & dosagem , Tensoativos/química
14.
Pharm Res ; 36(8): 123, 2019 Jun 19.
Artigo em Inglês | MEDLINE | ID: mdl-31218557

RESUMO

PURPOSE: This investigation was aimed to explore the targeting potential of folate conjugated double liposomes (fDLs) bearing combination of synergistic drugs (Prednisolone and Methotrexate) for effective management of the rheumatoid arthritis (RA). METHODS: To overcome the drawbacks of monotherapy, a combination of prednisolone (PRD) (an anti-inflammatory agent) and methotrexate (MTX) (a disease modifying anti-rheumatoid agent, DMARDs) was chosen for dual targeting approach. fDLs were prepared in two steps i.e. development of inner liposomes (ILs) using thin film casting method followed by encapsulation of ILs within folate conjugated outer liposomes (double liposomes; fDLs). Developed liposomes were characterized for various physicochemical parameters and in vivo performance. RESULTS: fDLs were prepared using FA-PEG-4000-NH-DSPE conjugate. These double liposomes were having 429.3 ± 3.6 nm in size with 0.109 PDI, 8.01 ± 0.3 mV zeta potential (ζ) and 66.7 ± 3.9% and 45.3 ± 1.7% entrapments of PRD and MTX, respectively. After 24 h, the concentrations of PRD in blood were observed to be 8.66 ± 3.11 (ILs) and 15.13 ± 0.81% (DLs) while concentration of MTX were found to be 10.89 ± 0.69 and 2.34 ± 3.15% when given as ILs and fDLs, respectively. The concentration of both drugs in inflamed joint was observed to be higher than that in the non-inflamed joints. CONCLUSIONS: The folate conjugated double liposomes possess superior targeting efficiency than conjugated and unconjugated single liposomes.


Assuntos
Anti-Inflamatórios/farmacocinética , Antirreumáticos/farmacocinética , Artrite Reumatoide/tratamento farmacológico , Ácido Fólico/química , Lipossomos/química , Metotrexato/farmacocinética , Prednisolona/farmacocinética , Animais , Anti-Inflamatórios/administração & dosagem , Antirreumáticos/administração & dosagem , Artrite Experimental/tratamento farmacológico , Artrite Experimental/metabolismo , Artrite Reumatoide/metabolismo , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Quimioterapia Combinada , Humanos , Masculino , Metotrexato/administração & dosagem , Tamanho da Partícula , Fosfatidiletanolaminas/química , Polietilenoglicóis/química , Prednisolona/administração & dosagem , Ratos , Propriedades de Superfície , Distribuição Tecidual
15.
Pharm Res ; 36(8): 124, 2019 Jun 21.
Artigo em Inglês | MEDLINE | ID: mdl-31227928

RESUMO

PURPOSE: The aim of this work was to evaluate the use of short durations of externally applied heat with chemical penetration enhancers to improve delivery of isotretinoin to the skin and in particular via the follicular route. METHODS: A range of chemical penetration enhancers were screened for their ability to improve isotretinoin delivery into human skin with heat using infinite dose, Franz cell experiments conducted in a water bath at a higher temperature to simulate heated conditions. Following this a prototype external heating system was developed that provided short durations of heat and its ability to improve delivery of finite doses into the skin and hair follicles was assessed. RESULTS: The magnitude of the effect of heat on drug delivery was influenced by the choice of vehicle with changes in isotretinoin flux across skin ranging from not statistically significant to 25 fold increases with heat in the infinite dose studies. The prototype heating system provided significant increases in the total delivery of isotretinoin into the skin from an optimised vehicle. Drug distribution in the skin revealed significant increases in isotretinoin delivery to the hair follicles, and deeper skin layers, but not to the stratum corneum, providing strong evidence that the enhancement in delivery occurred mainly via the hair follicles. CONCLUSION: These data indicate that the use of short durations of heat combined with chemical penetration enhancers offers a valuable strategy for improving the delivery of drugs such as isotretinoin to the skin via the hair follicles. Graphical Abstract Schematic illustration of the sodium thiosulphate heating system on a Franz diffusion cell and the subsequent impact of a short burst of heat on the delivery of isotretinoin into human skin.


Assuntos
Fármacos Dermatológicos/farmacologia , Portadores de Fármacos/química , Folículo Piloso/química , Isotretinoína/farmacologia , Administração Cutânea , Fármacos Dermatológicos/administração & dosagem , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Feminino , Folículo Piloso/citologia , Temperatura Alta , Humanos , Isotretinoína/administração & dosagem , Permeabilidade , Pele/metabolismo , Absorção Cutânea , Tiossulfatos/química
16.
Nat Commun ; 10(1): 2566, 2019 06 12.
Artigo em Inglês | MEDLINE | ID: mdl-31189915

RESUMO

There is clinical and scientific interest in developing local anesthetics with prolonged durations of effect from single injections. The need for such is highlighted by the current opioid epidemic. Site 1 sodium channel blockers such as tetrodotoxin (TTX) are extremely potent, and can provide very long nerve blocks but the duration is limited by the associated systemic toxicity. Here we report a system where slow release of TTX conjugated to a biocompatible and biodegradable polymer, poly(triol dicarboxylic acid)-co-poly(ethylene glycol) (TDP), is achieved by hydrolysis of ester linkages. Nerve block by the released TTX is enhanced by administration in a carrier with chemical permeation enhancer (CPE) properties. TTX release can be adjusted by tuning the hydrophilicity of the TDP polymer backbone. In vivo, 1.0-80.0 µg of TTX released from these polymers produced a range of durations of nerve block, from several hours to 3 days, with minimal systemic or local toxicity.


Assuntos
Anestésicos Locais/administração & dosagem , Portadores de Fármacos/química , Bloqueio Nervoso/métodos , Bloqueadores dos Canais de Sódio/administração & dosagem , Tetrodotoxina/administração & dosagem , Anestesia Local/métodos , Anestésicos Locais/farmacocinética , Animais , Materiais Biocompatíveis/química , Materiais Biocompatíveis/toxicidade , Plásticos Biodegradáveis/química , Plásticos Biodegradáveis/toxicidade , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Preparações de Ação Retardada/administração & dosagem , Portadores de Fármacos/toxicidade , Composição de Medicamentos/métodos , Avaliação Pré-Clínica de Medicamentos , Liberação Controlada de Fármacos , Masculino , Camundongos , Permeabilidade , Ratos , Ratos Sprague-Dawley , Nervo Isquiático/efeitos dos fármacos , Bloqueadores dos Canais de Sódio/farmacocinética , Tetrodotoxina/farmacocinética , Fatores de Tempo , Resultado do Tratamento
17.
Microb Cell Fact ; 18(1): 87, 2019 May 20.
Artigo em Inglês | MEDLINE | ID: mdl-31109314

RESUMO

BACKGROUND: Saccharomyces cerevisiae AN120 osw2∆ spores were used as a host with good resistance to unfavorable environment. This work was undertaken to develop a new yeast spore-encapsulation of Candida parapsilosis Glu228Ser/(S)-carbonyl reductase II and Bacillus sp. YX-1 glucose dehydrogenase for efficient chiral synthesis in organic solvents. RESULTS: The spore microencapsulation of E228S/SCR II and GDH in S. cerevisiae AN120 osw2∆ catalyzed (R)-phenylethanol in a good yield with an excellent enantioselectivity (up to 99%) within 4 h. It presented good resistance and catalytic functions under extreme temperature and pH conditions. The encapsulation produced several chiral products with over 70% yield and over 99% enantioselectivity in ethyl acetate after being recycled for 4-6 times. It increased substrate concentration over threefold and reduced the reaction time two to threefolds compared to the recombinant Escherichia coli containing E228S and glucose dehydrogenase. CONCLUSIONS: This work first described sustainable enantioselective synthesis without exogenous cofactors in organic solvents using yeast spore-microencapsulation of coupled alcohol dehydrogenases.


Assuntos
Oxirredutases do Álcool/metabolismo , Bacillus/metabolismo , Candida parapsilosis/metabolismo , Composição de Medicamentos/métodos , Glucose 1-Desidrogenase/metabolismo , Saccharomyces cerevisiae/metabolismo , Esporos Fúngicos/metabolismo , Solventes
18.
AAPS PharmSciTech ; 20(5): 196, 2019 May 23.
Artigo em Inglês | MEDLINE | ID: mdl-31123934

RESUMO

Undesired-burst release effect is observed in a freely water-soluble drug formulated into a gastro-floating formulation with effervescent (GFFE) delivery system. In order to address this limitation, interpolymer complex (IPC) of two swellable and non-soluble polymers, poly-ammonium methacrylate and poly-vinyl acetate, was incorporated into hydroxypropyl methyl cellulose (HPMC)-based matrix GFFE. This research studied the effect and interaction of the IPC-HPMC blending on the drug release of GFFE using a freely water-soluble drug, metformin HCl, under different threshold concentration levels and curing effect. The interaction between the IPC and HPMC was characterized using vibrational spectroscopy and thermal analyses under curing and swelling conditions. Anti-solvent followed by lyophilization had better physicochemical and physicomechanic properties than spray dying technique. The interaction was observed by a specific shifting of the vibrational peaks and alteration of the thermal behavior pattern. These effects altered the drug release behavior. Thereafter, the IPC reduced burst release effects in the initial time and during testing, and the IPC improved the HPMC matrix robustness under mechanical stress testing below threshold concentration of HPMC matrix formulated in the GFFE.


Assuntos
Fármacos Gastrointestinais/síntese química , Derivados da Hipromelose/síntese química , Polímeros/síntese química , Água/química , Preparações de Ação Retardada/síntese química , Preparações de Ação Retardada/farmacocinética , Composição de Medicamentos/métodos , Liberação Controlada de Fármacos , Fármacos Gastrointestinais/farmacocinética , Derivados da Hipromelose/farmacocinética , Polímeros/farmacocinética , Solubilidade , Comprimidos
19.
J Food Sci ; 84(6): 1513-1521, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-31120593

RESUMO

Geotrichum citri-aurantii causes sour rot in citrus fruits and is responsible for important economic losses during storage. However, the availability of chemical fungicides for the control of this pathogen is limited. Thus, the aim of this research was to evaluate the antifungal efficacy of thymol and carvacrol encapsulated in 2-hydroxylpropyl-beta-cyclodextrin (HP-ß-CD) (prepared by the microwave irradiation method [MW] and solubility method [S]) for inhibition of G. citri-aurantii using in vitro bioassays broth (micro and macrodilutions methods) and inoculated food testing. Both encapsulated thymol and carvacrol were shown to be effective for inhibiting G. citri-aurantii growth in in vitro assays. Thymol was more effective in inhibiting G. citri-aurantii, while better encapsulation was provided by MW. HP-ß-CD-thymol encapsulated by MW (HP-ß-CD-thymol-MW) showed the lowest 50% effective dose (ED50 = 1.16 mM), minimum inhibitory concentration (MIC = 5.06 mM), and minimum fungicide concentration (MFC = 52.6 mM). HP-ß-CD-thymol-MW was found highly effective in reducing the growth rate and mycelial growth inhibition. Finally, HP-ß-CD-thymol-MW and HP-ß-CD-carvacrol-MW showed a higher persistent effect than thymol and carvacrol in their natural form in inhibiting this fungus. Therefore, HP-ß-CD-thymol-MW could be a promising alternative to synthetic fungicides for controlling G. citri-aurantii, the causal agent of citrus sour rot. PRACTICAL APPLICATION: Encapsulated thymol and carvacrol in HP-ß-Cyclodextrins are effective for controlling G. citri-aurantii in in vitro experiments. Encapsulation of thymol and carvacrol by microwave irradiation method (MW) was more effective than the solubility (S) method. Thymol was more effective than carvacrol, and the best results on G. citri-auriantii inhibition were achieved using the HP-ß-CD-thymol-MW method (which gave the lowest ED50 , MIC, and MFC).


Assuntos
Citrus/microbiologia , Composição de Medicamentos/métodos , Fungicidas Industriais/farmacologia , Geotrichum/efeitos dos fármacos , Monoterpenos/farmacologia , Timol/farmacologia , beta-Ciclodextrinas/química , Fungicidas Industriais/química , Geotrichum/crescimento & desenvolvimento , Testes de Sensibilidade Microbiana , Monoterpenos/química , Doenças das Plantas/microbiologia , Timol/química
20.
Chem Pharm Bull (Tokyo) ; 67(5): 445-451, 2019.
Artigo em Inglês | MEDLINE | ID: mdl-31061369

RESUMO

Electrodeposition is commonly used to deposit ceramic or metal coating on metallic implants. Its utilization in depositing polymer microcapsule coating is currently being explored. However, there is no encapsulation of drug within polymer microcapsules that will enhance its chemical and biological properties. Therefore, in this study, ginseng which is known for its multiple therapeutic effects was encapsulated inside biodegradable poly(lactic-co-glycolic acid) (PLGA) microcapsules to be coated on pre-treated medical grade stainless steel 316L (SS316L) using an electrodeposition technique. Polyaniline (PANI) was incorporated within the microcapsules to drive the formation of microcapsule coating. The electrodeposition was performed at different current densities (1-3 mA) and different deposition times (20-60 s). The chemical composition, morphology and wettability of the microcapsule coatings were characterized through attenuated total reflectance-Fourier transform infrared spectroscopy (ATR-FTIR), scanning electron microscopy (SEM) and contact angle analyses. The changes of electrolyte colors, before and after the electrodeposition were also observed. The addition of PANI has formed low wettability and uniform microcapsule coatings at 2 mA current density and 40 s deposition time. Reduction in the current density or deposition time caused less attachment of microcapsule coatings with high wettability records. While prolonging either one parameter has led to debris formation and melted microcapsules with non-uniform wettability measurements. The color of electrolytes was also changed from milky white to dark yellow when the current density and deposition time increased. The application of tolerable current density and deposition time is crucial to obtain a uniform microcapsule coating, projecting a controlled release of encapsulated drug.


Assuntos
Compostos de Anilina/química , Materiais Revestidos Biocompatíveis/química , Galvanoplastia/métodos , Panax/química , Copolímero de Ácido Poliláctico e Ácido Poliglicólico/química , Aço Inoxidável/química , Cápsulas , Composição de Medicamentos/instrumentação , Composição de Medicamentos/métodos , Galvanoplastia/instrumentação , Desenho de Equipamento , Próteses e Implantes
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