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1.
Pest Manag Sci ; 73(6): 1148-1153, 2017 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-27608288

RESUMEN

BACKGROUND: Owing to the difficulty in reaching targets during pesticide applications on guava trees, it is important to evaluate new technologies that may improve pest management. In electrostatic spraying, an electric force is added to the droplets to control their movements such that they are efficiently directed to the target. The present study evaluated the performance of electrostatic and non-electrostatic spraying in the control of the guava psyllid, the deposition of the spray mixture on the leaves and the losses to the soil. RESULTS: The deposition of the spray mixture was up to 2 times greater when using electrostatic spraying in comparison with non-electrostatic application. The losses of the spray mixture to the soil were up to 4 times smaller with the electrostatic spraying. Electrostatic spraying had better control of the psyllid. CONCLUSION: It was possible to reduce the volume rate of application with electrostatic spraying without adversely affecting the control of the guava psyllid. © 2016 Society of Chemical Industry.


Asunto(s)
Hemípteros , Control de Insectos/instrumentación , Insecticidas , Psidium , Animales , Neonicotinoides , Nitrocompuestos , Residuos de Plaguicidas , Hojas de la Planta , Árboles
2.
Eur J Pharm Biopharm ; 93: 205-13, 2015 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-25748796

RESUMEN

This work aims at studying the efficacy of a series of novel biocompatible, serine-based surfactants as chemical permeation enhancers for two different local anesthetics, tetracaine and ropivacaine, combining an experimental and computational approach. The surfactants consist of gemini molecules structurally related, but with variations in headgroup charge (nonionic vs. cationic) and in the hydrocarbon chain lengths (main and spacer chains). In vitro permeation and molecular dynamics studies combined with cytotoxicity profiles were performed to investigate the permeation of both drugs, probe skin integrity, and rationalize the interactions at molecular level. Results show that these enhancers do not have significant deleterious effects on the skin structure and do not cause relevant changes on cell viability. Permeation across the skin is clearly improved using some of the selected serine-based gemini surfactants, namely the cationic ones with long alkyl chains and shorter spacer. This is noteworthy in the case of ropivacaine hydrochloride, which is not easily administered through the stratum corneum. Molecular dynamics results provide a mechanistic view of the surfactant action on lipid membranes that essentially corroborate the experimental observations. Overall, this study suggests the viability of these serine-based surfactants as suitable and promising delivery agents in pharmaceutical formulations.


Asunto(s)
Amidas/administración & dosificación , Anestésicos Locales/administración & dosificación , Serina/administración & dosificación , Absorción Cutánea/efectos de los fármacos , Piel/efectos de los fármacos , Tensoactivos/administración & dosificación , Tetracaína/administración & dosificación , Administración Cutánea , Amidas/química , Amidas/metabolismo , Anestésicos Locales/química , Anestésicos Locales/metabolismo , Animales , Células Cultivadas , Química Farmacéutica , Queratinocitos/efectos de los fármacos , Queratinocitos/metabolismo , Queratinocitos/ultraestructura , Cinética , Microscopía Electrónica de Rastreo , Modelos Biológicos , Simulación de Dinámica Molecular , Estructura Molecular , Permeabilidad , Ropivacaína , Serina/análogos & derivados , Serina/química , Serina/toxicidad , Piel/metabolismo , Piel/ultraestructura , Relación Estructura-Actividad , Tensoactivos/química , Tensoactivos/toxicidad , Porcinos , Tecnología Farmacéutica/métodos , Tetracaína/química , Tetracaína/metabolismo
3.
J Pediatr (Rio J) ; 79(5): 455-60, 2003.
Artículo en Portugués | MEDLINE | ID: mdl-14557847

RESUMEN

OBJECTIVE: To evaluate if mid-upper arm circumference (MUAC) can be used for obesity screening in preschool children. METHODS: 1,090 children aged from 12 to 59.99 months were studied. Personal information, weight, height and MUAC were obtained. Sensitivity and specificity to detect obese children were calculated for MUAC to age and MUAC to height z scores. Obesity was defined as weight to height z score >2. RESULTS: 6.6% of the children had a weight to height z score >2. The best association between sensitivity (76.5%) and specificity (77.9%) to detect obese children for MUAC to age was obtained with a z score of 0.7. In terms of MUAC to height, the best association between sensitivity (79.4%) and specificity (77.6%) to detect obese children was obtained with a 0.6 score. CONCLUSIONS: MUAC to height z score was not advantageous for obesity screening when compared to MUAC to age z score. MUAC to age z score seems to be an adequate alternative method for obesity screening in preschool children.


Asunto(s)
Antropometría/métodos , Brazo/anatomía & histología , Tamizaje Masivo/métodos , Estado Nutricional , Obesidad/diagnóstico , Distribución por Edad , Estatura , Peso Corporal , Preescolar , Femenino , Humanos , Lactante , Masculino , Sensibilidad y Especificidad
4.
Int J Pharm ; 466(1-2): 349-58, 2014 May 15.
Artículo en Inglés | MEDLINE | ID: mdl-24657142

RESUMEN

This work provides a new insight on fundamental principles of the interaction mechanism between two forms of tetracaine - a potent local anesthetic - both in neutral (TC) and ionized (TC(+)) states, with beta- (ß-CD) and hydroxypropyl-beta-cyclodextrin (HP-ß-CD), and how such interactions affect the transport of tetracaine, at different concentrations, across a model membrane. The kinetics and mechanism of TC release from HPMC gels is also evaluated giving an insight on the role of cyclodextrin on the tetracaine transport. HPLC, fluorescence and NMR spectroscopies provided solid physicochemical knowledge of these systems and in vitro studies were performed to obtain relevant data on the transport and mechanism parameters. HPLC and fluorescence spectroscopy data revealed that tetracaine interacts with both cyclodextrins on a 1:1 stoichiometry but it is observed that neutral tetracaine forms more stables complexes (ca. 1050 M(-1) for both cyclodextrins) than in its ionized form (628 and 337 M(-1) for ß-CD and HP-ß-CD respectively). Despite of that, no host-guest interactions take place as seen by ROESY. This study clearly demonstrates that both forms of tetracaine are successfully released from the formulations at a controlled rate, following a Super-Case transport mechanism and the transport of tetracaine can be tuned by using cyclodextrins.


Asunto(s)
Anestésicos Locales/química , Tetracaína/química , beta-Ciclodextrinas/química , Cromatografía Líquida de Alta Presión , Concentración de Iones de Hidrógeno , Espectroscopía de Resonancia Magnética , Membranas Artificiales , Permeabilidad , Solubilidad , Espectrometría de Fluorescencia , Agua/química
5.
Int J Pharm ; 474(1-2): 212-22, 2014 Oct 20.
Artículo en Inglés | MEDLINE | ID: mdl-25108047

RESUMEN

The aim of this study is to investigate the efficacy of new, biocompatible, lysine-based surfactants as chemical permeation enhancers for two different local anesthetics, tetracaine and ropivacaine hydrochloride, topically administered. Results show that this class of surfactants strongly influences permeation, especially in the case of the hydrophilic and ionized drug, ropivacaine hydrochloride, that is not easily administered through the stratum corneum. It is also seen that the selected permeation enhancers do not have significant deleterious effects on the skin structure. A cytotoxicity profile for each compound was established from cytotoxicity studies. Molecular dynamics simulation results provided a rationale for the experimental observations, introducing a mechanistic view of the action of the surfactants molecules upon lipid membranes.


Asunto(s)
Anestésicos Locales/administración & dosificación , Sistemas de Liberación de Medicamentos , Lisina/química , Absorción Cutánea , Piel/metabolismo , Tensoactivos/administración & dosificación , Tensoactivos/química , Administración Cutánea , Amidas/administración & dosificación , Amidas/química , Amidas/farmacología , Anestésicos Locales/química , Anestésicos Locales/farmacología , Animales , Materiales Biocompatibles/administración & dosificación , Materiales Biocompatibles/química , Materiales Biocompatibles/farmacología , Supervivencia Celular/efectos de los fármacos , Células HEK293 , Humanos , Lisina/administración & dosificación , Simulación de Dinámica Molecular , Estructura Molecular , Permeabilidad/efectos de los fármacos , Ropivacaína , Piel/efectos de los fármacos , Porcinos , Tetracaína/administración & dosificación , Tetracaína/química , Tetracaína/farmacología
6.
AAPS J ; 15(4): 1119-27, 2013 Oct.
Artículo en Inglés | MEDLINE | ID: mdl-23959685

RESUMEN

The purpose of this study was to determine the ability and the safety of a series of alkylammonium C12-gemini surfactants to act as permeation enhancers for three model drugs, namely lidocaine HCl, caffeine, and ketoprofen. In vitro permeation studies across dermatomed porcine skin were performed over 24 h, after pretreating the skin for 1 h with an enhancer solution 0.16 M dissolved in propylene glycol. The highest enhancement ratio (enhancement ratio (ER)=5.1) was obtained using G12-6-12, resulting in a cumulative amount of permeated lidocaine HCl of 156.5 µg cm−2. The studies with caffeine and ketoprofen revealed that the most effective gemini surfactant was the one with the shorter spacer, G12-2-12. The use of the latter resulted in an ER of 2.4 and 2.2 in the passive permeation of caffeine and ketoprofen, respectively. However, Azone was found to be the most effective permeation enhancer for ketoprofen, attaining a total of 138.4 µg cm−2 permeated, 2.7-fold over controls. This work demonstrates that gemini surfactants are effective in terms of increasing the permeation of drugs, especially in the case of hydrophilic ionized compounds, that do not easily cross the stratum corneum. Skin integrity evaluation studies did not indicate the existence of relevant changes in the skin structure after the use of the permeation enhancers, while the cytotoxicity studies allowed establishing a relative cytotoxicity profile including this class of compounds, single chain surfactants, and Azone. A dependence of the toxicity to HEK and to HDF cell lines on the spacer length of the various gemini molecules was found.


Asunto(s)
Benzoatos/química , Benzoatos/metabolismo , Compuestos de Amonio Cuaternario/química , Compuestos de Amonio Cuaternario/metabolismo , Absorción Cutánea/fisiología , Tensoactivos/química , Tensoactivos/metabolismo , Animales , Benzoatos/administración & dosificación , Sinergismo Farmacológico , Técnicas de Cultivo de Órganos , Compuestos de Amonio Cuaternario/administración & dosificación , Absorción Cutánea/efectos de los fármacos , Relación Estructura-Actividad , Porcinos
7.
Eur J Pharm Biopharm ; 80(3): 663-73, 2012 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-22137964

RESUMEN

The present work reports the evaluation of three nonionic ether-monohydroxyl surfactants (C(12)E(1), C(12)E(5,) and C(12)E(8)) as skin permeation enhancers in the transdermal drug delivery of two drugs: ondansetron hydrochloride and diltiazem hydrochloride, formulated as hydrogels. The enhancers are used alone, or in combination with iontophoresis (0.3 mA - 8h). After 1h of pre-treatment with 0.16 M enhancer solutions in propylene glycol (PG), passive and iontophoretic 24 h in vitro studies across dermatomed porcine skin were performed using vertical Franz diffusion cells. Data obtained showed that the nonionic surfactant C(12)E(5) was the most effective permeation enhancer, both for the passive process as well as for samples subjected to iontophoresis, resulting in cumulative amounts of ondansetron HCl after 24h of approximately 93 µg/cm(2) and 336 µg/cm(2), respectively. Data obtained using diltiazem HCl showed a similar trend. The use of the nonionic surfactant C(12)E(5) resulted in higher enhancement ratios (ER) in passive studies, but C(12)E(8) yielded slightly higher values of drug permeated (2678 µg/cm(2)) than C(12)E(5) (2530 µg/cm(2)) when iontophoresis was also employed. Skin integrity studies were performed to assess potential harmful effects on the tissues resulting from the compounds applied and/or from the methodology employed. Skin samples used in permeation studies visualized by light microscopy and Scanning Electron Microscopy (SEM) at different levels of magnification did not show significant morphological and structural changes, when compared to untreated samples. Complementary studies were performed to gain information regarding the relative cytotoxicity of the penetration enhancers on skin cells. MTS assay data using human epidermal keratinocytes (HEK) and human dermal fibroblasts (HDF) indicated that HEK are more sensitive to the presence of the enhancers than HDF and that the toxicity of these compounds is enhancer molecular weight dependent.


Asunto(s)
Diltiazem/administración & dosificación , Diltiazem/química , Ondansetrón/administración & dosificación , Ondansetrón/química , Tensoactivos/química , Administración Cutánea , Animales , Células Cultivadas , Química Farmacéutica/métodos , Difusión , Diltiazem/farmacología , Sistemas de Liberación de Medicamentos/métodos , Fibroblastos/efectos de los fármacos , Humanos , Hidrogeles/administración & dosificación , Hidrogeles/química , Iontoforesis/métodos , Queratinocitos/efectos de los fármacos , Ondansetrón/farmacología , Permeabilidad , Propilenglicol/química , Piel/metabolismo , Absorción Cutánea , Soluciones/química , Porcinos
8.
Int J Pharm ; 421(1): 53-62, 2011 Dec 12.
Artículo en Inglés | MEDLINE | ID: mdl-21963468

RESUMEN

We investigated the enhancement effect of chemical enhancers and iontophoresis on the in vitro transdermal and transbuccal delivery of lidocaine HCl (LHCl), nicotine hydrogen tartrate (NHT), and diltiazem HCl (DHCl) using porcine skin and buccal tissues. Dodecyl 2-(N,N-dimethylamino) propionate (DDAIP), dodecyl-2-(N,N-dimethylamino) propionate hydrochloride (DDAIP HCl), N-(4-bromobenzoyl)-S,S-dimethyliminosulfurane (Br-iminosulfurane), and azone (laurocapram) were used as chemical enhancers. The study results showed that the application of iontophoresis at either 0.1 mA or 0.3 mA significantly enhanced transdermal and transmucosal delivery of LHCl, NHT and DHCl. It was also demonstrated that iontophoresis had a more pronounced enhancement effect on transdermal delivery than on transbuccal delivery of LHCl, NHT and DHCl. In addition, DDAIP HCl was found to be the most effective enhancer for transbuccal delivery of LHCl and NHT.


Asunto(s)
Diltiazem/administración & dosificación , Iontoforesis , Lidocaína/administración & dosificación , Nicotina/administración & dosificación , Absorción Cutánea , Administración Bucal , Administración Cutánea , Alanina/administración & dosificación , Alanina/análogos & derivados , Alanina/química , Animales , Azepinas/administración & dosificación , Azepinas/química , Diltiazem/farmacocinética , Sistemas de Liberación de Medicamentos , Técnicas In Vitro , Lidocaína/farmacocinética , Mucosa Bucal/metabolismo , Nicotina/farmacocinética , Piel/metabolismo , Compuestos de Azufre/administración & dosificación , Compuestos de Azufre/química , Porcinos
9.
J Colloid Interface Sci ; 327(2): 333-40, 2008 Nov 15.
Artículo en Inglés | MEDLINE | ID: mdl-18804777

RESUMEN

In this work we present an analysis of the thermal behavior of hydroxypropylmethyl cellulose aqueous solutions, from room temperature to higher temperatures, above gelation. We focus on significant aspects, essentially overlooked in previous work, such as the correlation between polymer hydrophobicity and rheological behavior, and the shear effect on thermal gelation. Micropolarity and aggregation of the polymer chains were monitored by both UV/vis and fluorescence spectroscopic techniques, along with polarized light microscopy. Gel formation upon heating was investigated using rheological experiments, with both large strain (rotational) tests at different shear rates and small strain (oscillatory) tests. The present observations allow us to compose a picture of the evolution of the system upon heating: firstly, polymer reptation increases due to thermal motion, which leads to a weaker network. Secondly, above 55 degrees C, the polymer chains become more hydrophobic and polymer clusters start to form. Finally, the number of physical crosslinks between polymer clusters and the respective lifetimes increase and a three-dimensional network is formed. This network is drastically affected if higher shear rates, at non-Newtonian regimes, are applied to the system.


Asunto(s)
Geles/química , Metilcelulosa/análogos & derivados , Interacciones Hidrofóbicas e Hidrofílicas , Derivados de la Hipromelosa , Metilcelulosa/química , Microscopía de Polarización , Oscilometría , Pirenos/química , Reología , Soluciones/química , Espectrometría de Fluorescencia , Temperatura , Viscosidad , Agua/química
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