Category Archives: Pharmaceutical Technology

Characteristics of erythropoietin-alginate microsphere

J Pharm Pharmacogn Res 6(4): 250-259, 2018.

Original Article | Artículo Original

Influence of crosslinker concentration on the characteristics of erythropoietin-alginate microspheres

[Influencia de la concentración de reticulante en las características de las microesferas de eritropoyetina y alginato]

Dewi M. Hariyadi*, Tutiek Purwanti, Safira Adilla

Department of Pharmaceutics, Faculty of Pharmacy, Universitas Airlangga Jl. Dharmawangsa Dalam 60286 Surabaya, East Java, Indonesia.

*E-mail: dewi-m-h@ff.unair.ac.id

Abstract

Context: Microspheres have several advantages including protecting proteins from degradation and clearance after administration and produce a long-term therapeutic effect. Erythropoietin as a neuroprotectant agent has protein-like properties, which are susceptible to degradation and have low in vivo bioavailability. Microspheres formulations is one of potential drug delivery system for erythropoietin.

Aims: To evaluate the effect of CaCl2 concentration on the characteristics (particle size, morphology, swelling index, and yield) of erythropoietin-alginate microspheres.

Methods: Erythropoietin-alginate microspheres prepared by ionotropic gelation method with aerosolization technique using sodium alginate as polymer and CaCl2 as crosslinker were dried using freeze drying method with maltodextrin as lyoprotectant. The concentrations of alginate used were 2%, and CaCl2 concentrations were 0.5 M(F1), 0.75 M(F2) and 1 M(F3).

Results: Results showed smooth and spherical microspheres for all formula with average particle size were 3.23 ± 0.05 μm (F1); 2.99 ± 0.07 μm (F2); and 2.86 ± 0.03 μm (F3). Mass swelling index at 24 h were 1.25 ± 0.10 (F1), 1.18 ± 0.11 (F2), and 1.11 ± 0.10 (F3); at 30 h were 2.00 ± 1.25 (F1), 1.85 ± 0.14 (F2), and 1.72 ± 0.15 (F3) while particle size swelling index at 24 h were 1.15 ± 0.10 (F1), 1.11 ± 0.10 (F2), and 0.97 ± 0.10 (F3); at 30 h were 1.81 ± 0.09 (F1), 1.73 ± 0.15 (F2), and 1.54 ± 0.14 (F3). Respectively yield percentages were 77.76 ± 6.49, 80.01 ± 3.53, and 82.97 ± 4.22. By using One Way ANOVA, it was found that there were significantly differences between three formulas.

Conclusions: The particle size of formulas decreased by increasing concentration of CaCl2, whereas no significant difference on swelling index and yield from microspheres with increasing CaCl2 concentration simultaneously.

Keywords: Ca-alginate microspheres; characterization; erythropoietin; ionotropic gelation.

Resumen

Contexto: Las microesferas tienen varias ventajas, incluyendo la protección de las proteínas contra la degradación y el aclaramiento después de la administración, y producen un efecto terapéutico a largo plazo. La eritropoyetina como un agente neuroprotector tiene propiedades tipo proteína, que son susceptibles de degradación y tienen baja biodisponibilidad in vivo. Las formulaciones de microesferas es uno de los posibles sistemas de administración de fármacos para la eritropoyetina.

Objetivos: Evaluar el efecto de la concentración de CaCl2 sobre las características (tamaño de partícula, morfología, índice de hinchamiento y rendimiento) de las microesferas de eritropoyetina y alginato.

Métodos: Las microesferas de eritropoyetina-alginato preparadas por el método de gelificación ionotrópica con técnica de aerosolización que usa alginato de sodio como polímero y CaCl2 como reticulante se secaron usando el método de liofilización con maltodextrina como lioprotector. Las concentraciones de alginato usadas fueron del 2%, y las concentraciones de CaCl2 fueron 0.5 M (F1), 0.75 M (F2) y 1 M (F3).

Resultados: Los resultados mostraron que las microesferas lisas y esféricas para todas las fórmulas con un tamaño de partícula promedio eran 3.23 ± 0.05 μm (F1); 2.99 ± 0.07 μm (F2); y 2.86 ± 0.03 μm (F3). El índice de hinchazón masivo a las 24 h fue 1.25 ± 0.10 (F1), 1.18 ± 0.11 (F2) y 1.11 ± 0.10 (F3); a las 30 h fue 2.00 ± 1.25 (F1), 1.85 ± 0.14 (F2) y 1.72 ± 0.15 (F3) mientras que el índice de hinchamiento del tamaño de partícula a las 24 h fue de 1.15 ± 0.10 (F1), 1.11 ± 0.10 (F2) y 0.97 ± 0,10 (F3); a las 30 h fue 1,81 ± 0,09 (F1), 1,73 ± 0,15 (F2) y 1,54 ± 0,14 (F3). Respectivamente los porcentajes de rendimiento fueron de 77.76 ± 6.49, 80.01 ± 3.53 y 82.97 ± 4.22. Los valores presentaron diferencias estadísticamente significativas entre las tres fórmulas.

Conclusiones: El tamaño de partícula de las fórmulas disminuyó al aumentar la concentración de CaCl2, mientras que no hubo una diferencia significativa en el índice de hinchamiento y el rendimiento de las microesferas con el aumento de la concentración de CaCl2 simultáneamente.

Palabras Clave: caracterización; eritropoyetina; gelificación ionotrópica; microesferas de alginato de Ca.

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Citation Format: Hariyadi DM, Purwanti T, Adilla S (2018) Influence of crosslinker concentration on the characteristics of erythropoietin-alginate microspheres. J Pharm Pharmacogn Res 6(4): 250–259.

© 2018 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Comparison of artemether-lumefantrine formulations

J Pharm Pharmacogn Res 6(3): 167-178, 2018.

Original Article | Artículo Original

Comparison of the physicochemical properties and in vivo bioavailability of generic and innovator artemether-lumefantrin tablets in Kumasi, Ghana

[Comparación de las propiedades fisicoquímicas y la biodisponibilidad in vivo de comprimidos genéricos e innovadores arteméter-lumefantrina en Kumasi, Ghana]

Noble Kuntworbe*, Francis A. Acquah, Raphael Johnson, Kwabena Ofori-Kwakye

Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, Kwame Nkrumah University of Science and Technology, PV Obeng Avenue, Tackie Building, PMB, Kumasi, Ghana.

*E-mail: nkuntworbe.pharm@knust.edu.gh, nkunstar@yahoo.co.uk

Abstract

Context: Malarial remains a leading course of death in developing countries. Current treatment protocol involves the use of artemisinin-based combination therapy. In endemic areas, cost of treatment is a concern hence generic prescription is on the high. It is therefore necessary to investigate how equivalent or otherwise the generics are to the innovator brand Coatem®.

Aims: To compare the physicochemical properties and in vivo bioavailability of a locally manufactured generic artemether-lumefantrine tablet formulation and that of the innovator brand sold on the Kumasi market, Ghana.

Methods: The most used locally manufactured generic and the innovator brands were sampled from retail pharmacies. The samples were confirmed by colorimetry. Pharmaceutical equivalence of the brands was determined using compendial tests. In vivo bioavailability study on the two brands was done using a two-period, single dose, cross-over design involving 20 healthy rabbits. Pharmacokinetic parameters (AUC0-72, AUC0-∞, and Cmax) for both brands derived from the study were analysed statistically.

Results: Both the generic and innovator brands passed the physicochemical tests. The artemether component of both brands complied with the pharmacopoeia specification for dissolution testing while the lumefantrine did not. Average bioequivalence was demonstrated per the FDA criterion with the geometric mean ratios and corresponding 90% confidence intervals falling within the acceptable limits of 0.80 – 1.25.

Conclusions: Based on the similarity demonstrated between the two brands, evidence have been shown to support substitutability of the often-expensive innovator brand with the affordable locally produced brand.

Keywords: artemether-lumefantrine; bioequivalence generic-substitution; pharmacokinetics.

Resumen

Contexto: La malaria sigue siendo una causa principal de muerte en los países en desarrollo. El protocolo de tratamiento actual implica el uso de terapia de combinación basada en la artemisinina. En áreas endémicas, el costo del tratamiento es una preocupación y la prescripción genérica está auge. Por lo tanto, es necesario investigar qué tan equivalentes o genéricos son los medicamentos para la marca innovadora Coatem®.

Objetivos: Comparar las propiedades fisicoquímicas y la biodisponibilidad in vivo de una formulación de tableta de artemeter-lumefantrina genérica, fabricada localmente, y la de la marca innovadora vendida en el mercado de Kumasi, Ghana.

Métodos: Se tomaron muestras de las marcas genéricas e innovadoras más utilizadas en las farmacias minoristas. Las muestras fueron confirmadas por colorimetría. La equivalencia farmacéutica de las marcas se determinó mediante pruebas compendiales. El estudio de biodisponibilidad in vivo en las dos marcas se realizó utilizando un diseño cruzado de dosis única de dos períodos en el se utilizaron 20 conejos sanos. Los parámetros farmacocinéticos (AUC0-72, AUC0-∞ y Cmax), para ambas marcas derivadas del estudio, se compararon estadísticamente.

Resultados: Tanto las marcas genéricas como innovadoras pasaron las pruebas fisicoquímicas. El componente de arteméter de ambas marcas cumplió con la especificación de la farmacopea para las pruebas de disolución, mientras que la lumefantrina no lo hizo. La bioequivalencia promedio se demostró según el criterio de la FDA con las razones de medias geométricas y los correspondientes intervalos de confianza del 90% dentro de los límites aceptables de 0,80 a 1,25.

Conclusiones: En base a la similitud demostrada entre las dos marcas, se ha demostrado que las pruebas respaldan la sustitución de la marca innovadora, a menudo cara, con la marca de producción local asequible.

Palabras Clave: arteméter-lumefantrina; farmacocinética; sustitución genérica de bioequivalencia.

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Citation Format: Kuntworbe N, Acquah FA, Johnson R, Ofori-Kwakye K (2018) Comparison of the physicochemical properties and in vivo bioavailability of generic and innovator artemether-lumefantrin tablets in Kumasi, Ghana. J Pharm Pharmacogn Res 6(3): 167–178.

© 2018 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Estabilidad física de bases semisólidas con quitosana

J Pharm Pharmacogn Res 5(5): 288-300, 2017.

Original Article | Artículo Original

Estabilidad física de bases emulsionadas e hidrosolubles con quitosana y acetato de quitosana

[Physical stability of emulsion and hydrophilic gels with chitosan and chitosan acetate]

Nilia De la Paz1, Dania Pérez2, Mirna Fernández2*, Dulce M. Soler3, Yanet Rodríguez3, Antonio Nogueira1

1Centro de Investigación y Desarrollo de Medicamentos (CIDEM). Ave. 26 # 1605 e/ Puentes Grandes y Boyeros. La Habana, Cuba.
2Instituto de Farmacia y Alimentos (IFAL). Universidad de la Habana. Calle 23 No. 21425 e/ 214 y 222. La Habana. Cuba.
3Centro Nacional de Sanidad Agropecuaria (CENSA). Autopista Nacional y Carretera de Tapaste, San José de las Lajas, La Habana, Cuba.

*E-mail: mirnafc@ifal.uh.cu; mirnafc@gmail.com

Abstract

Context: Chitosan has received great attention because it is a functional, biodegradable, renewable and non-toxic biopolymer with multiple pharmaceutical applications, including stabilizing agent.

Aims: To evaluate the physical stability of emulsified bases and hydrophilic gels containing chitosan or chitosan acetate as stabilizing agents.

Methods: Stability of shelf-life formulations at room temperature and in refrigeration was evaluated over a period of 60 days and by thermal stress testing and centrifugal destabilization. The organoleptic characteristics, pH, conductivity and flow behavior were evaluated, the latter through the analysis of the rheograms, the determination of rheological parameters (consistency index, apparent viscosity, creep value and flow index), as well as their comparison statistics. The possible correlations between these parameters and the concentration of the biopolymers were also evaluated.

Results: The bases elaborated with chitosan or its soluble derivative showed adequate physical stability during the study time. The effect of the storage temperature, as well as the type and concentration of the stabilizing agent used was evidenced. Emulsifier combinations provided less stability. A linear correlation between the rheological parameters and the biopolymer concentration was evidenced.

Conclusions: Chitosan and chitosan acetate can be used as emulsifying agents in semi-solid and gelling bases in hydrophilic gels, due to the electrostatic stabilization and the viscosity they contribute to the system in relation to its concentration.

Keywords: chitosan; chitosan acetate; physical stability; semisolid vehicles.

Resumen

Contexto: La quitosana ha recibido gran atención al ser un biopolímero funcional, biodegradable, renovable y no tóxico con múltiples aplicaciones farmacéuticas, entre ellas como agente estabilizante.

Objetivos: Evaluar la estabilidad física de bases emulsionadas y geles hidrofílicos que contienen quitosana o acetato de quitosana como agentes estabilizantes.

Métodos: Se evaluó la estabilidad de las formulaciones en vida de estante, a temperatura ambiente y en refrigeración, en un período de 60 días, mediante pruebas de estrés térmico y desestabilización por centrifugación. Se evaluaron las características organolépticas, pH, conductividad y comportamiento de flujo. A partir del análisis de los reogramas se determinaron parámetros reológicos (índice de consistencia, viscosidad aparente, valor de fluencia e índice de flujo), así como su comparación estadística. Se evaluaron además las posibles correlaciones entre estos parámetros y la concentración de los biopolímeros.

Resultados: Las bases elaboradas con quitosana o su derivado soluble mostraron adecuada estabilidad física durante el tiempo de estudio. Se evidenció el efecto de la temperatura de almacenamiento, así como del tipo y concentración del agente estabilizante empleado. Las combinaciones de emulgentes aportaron menos estabilidad. Se evidenció una correlación lineal entre los parámetros reológicos y la concentración del biopolímero.

Conclusiones: La quitosana y el acetato de quitosana pueden emplearse como agentes emulgentes en bases semisólidas y geles hidrofílicos, debido a la estabilización electrostática y a la viscosidad que aportan al sistema en relación con su concentración.

Palabras Clave: acetato de quitosana; bases semisólidas; estabilidad física; quitosana.

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Citation Format: De la Paz N, Pérez D, Fernández M, Soler DM, Rodríguez Y, Nogueira A (2017) Estabilidad física de bases emulsionadas e hidrosolubles con quitosana y acetato de quitosana. [Physical stability of emulsion and hydrophilic gels with chitosan and chitosan acetate]. J Pharm Pharmacogn Res 5(5): 288–300.

© 2017 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Herbal polymeric nanoformulations to contest depression

J Pharm Pharmacogn Res 5(3): 187-199, 2017.

Original Article | Artículo Original

Nanoparticulated formulations of St. John’s wort (Hypericum perforatum L.) as smart drug delivery system combating depression incited in mice models

[Formulas nanoparticuladas de hierba de San Juan (Hypericum perforatum L.) como sistema inteligente de administración de fármacos para combatir la depresión inducida en modelos de ratones]

Violet Dhayabaran, Anita Margret*

Department of Biotechnology and Bioinformatics, Bishop Heber College, Vayallor Road, Puthur, Tiruchirappalli-620017, Tamilnadu, India.

*E-mail: anitamargret@gmail.com; anita.bt@bhc.edu.in

Abstract

Context: Hypericum perforatum L., commonly known as St. John’s wort, is practised as an alternative medicine against depression. Conversely, its remedial efficacy is indulged by various adverse effects that are recuperated in formulating nanoscaled commercial capsules encased by the biopolymer chitosan. A potential application of nanoencapsulation with regards to polymer enhances a slow controlled release of the targeted drug to achieve the desired delay until the right stimulus is obtained.

Aims: To value synthesizing biopolymeric nanocomposites encapsulating St. John’s wort commercial capsules substantiating it with a study of animal model of depression to endorse the effect of nanocapsulated drug as an effective brain drug.

Methods: The nanoparticulated suspension was prepared by ionic gelation technique and characterized to attest its antidepressant activity by in vivo studies.

Results: The drug binding efficiency was endorsed by FT-IR studies and the nanoparticles were characterized by an average particle size of 211.4 nm with a positive zeta potential of 45.9 mV. The animal despair studies on depression induced mice models displayed a significant difference in the immobility time during force swimming and tail suspension test. The commercial capsules were administed orally (p.o., 50 and 100 mg/kg). The animal despair studies were substantiated with affirmative biochemical assessments like SOD, CAT, GPx, GSH and LPO and compared with control groups.

Conclusions: The outcomes of this work manifest the calibre of St. John’s wort nanocomposites in a lower dosage that can alleviate depression and reduce side effects.

Keywords: biopolymer; chitosan; depression; Hypericum perforatum; nanoparticles.

Resumen

Contexto: Hypericum perforatum L., comúnmente conocida como hierba de San Juan, es usada como una medicina alternativa contra la depresión. Por el contrario, su eficacia terapéutica se acompaña de diversos efectos adversos que se aminoran con la formulación de nanocápsulas con el biopolímero quitosano. Una aplicación potencial de la nanoencapsulación con respecto al polímero mejora una lenta liberación controlada del fármaco dirigido para conseguir el retardo deseado hasta que se obtenga el estímulo correcto.

Objetivos: Evaluar nanocompuestos biopoliméricos sintéticos que encapsulan las cápsulas comerciales de hierba de San Juan que los justifican con un estudio en modelos animales de depresión para endosar el efecto del medicamento nanocapsulado como fármaco eficaz para el cerebro.

Métodos: La suspensión nanoparticulada se preparó mediante una técnica de gelificación iónica y caracterizada por atestiguar su actividad antidepresiva mediante estudios in vivo.

Resultados: La eficacia de unión a fármacos fue respaldada por estudios FT-IR y las nanopartículas se caracterizaron por un tamaño medio de partícula de 211,4 nm, con un potencial zeta positivo de 45,9 mV. Los estudios de desesperación animal en modelos de depresión en ratones mostraron una diferencia significativa en el tiempo de inmovilidad durante la natación forzada y la prueba de suspensión de cola. Las cápsulas comerciales se administraron por vía oral (p.o., 50 y 100 mg/kg). Los estudios de desesperación animal se confirmaron con valoraciones bioquímicas positivas como SOD, CAT, GPx, GSH y LPO y se compararon con los grupos de controles.

Conclusiones: Los resultados de este trabajo manifiestan el calibre de los nanocompuestos de la hierba de San Juan, en una dosis más baja, que puede aliviar la depresión y reducir los efectos secundarios.

Palabras Clave: biopolímero; depresión; Hypericum perforatum; nanopartículas; quitosano.

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Citation Format: Dhayabaran V, Margret A (2017) Nanoparticulated formulations of St. John’s wort (Hypericum perforatum L.) as smart drug delivery system combating depression incited in mice models. J Pharm Pharmacogn Res 5(3): 187–199.

© 2017 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Dibucaine release from chitosan semisolid vehicles

J Pharm Pharmacogn Res 5(2): 96-105, 2017.

Original Article | Artículo Original

In vitro release of dibucaine hydrochloride from chitosan semisolid vehicles: emulsion and hydrophilic gels

[Liberación in vitro del clorhidrato de dibucaína desde vehículos semisólidos con quitosana: emulsionados y geles hidrofílicos]

Nilia de la Paz1, Dania Pérez2, Mirna Fernández2*, Caridad M. García1, Vivian Martínez1, Antonio Nogueira1, Oscar García3

1Centro de Investigación y Desarrollo de Medicamentos (CIDEM). Ave. 26 # 1605 e/ Puentes Grandes y Boyeros. La Habana, Cuba.
2Instituto de Farmacia y Alimentos (IFAL). Universidad de la Habana. Calle 23 No. 21425 e/ 214 y 222. La Habana. Cuba.
3Empresa Laboratorio Farmacéutico Roberto Escudero Díaz. Calle 20 de Mayo No. 540 esq. Marta Abreu. La Habana, Cuba.

*E-mail: mirnafc@ifal.uh.cu

Abstract

Context: Chitosan has received attention as a functional, sustainably renewable, nontoxic and biodegradable biopolymer for pharmaceutical applications.

Aims: To evaluate the release of dibucaine hydrochloride from semisolid vehicles of oil/aqueous type emulsion and aqueous gels, stabilized by using chitosan (CH) or chitosan acetate (CHAc).

Methods: Emulsions were developed by varying the emulsifying agent: polysorbate 80, CH or CHAc and by combining CH with polysorbate 80 or CHAc with polysorbate 80. The hydroxypropylmethyl cellulose F4M was added as a stabilizing agent in gel formulations. The release rates of model drug from semisolid vehicles were measured by using a dialysis sac. Drug release was also quantified by using a validated UV-VIS spectrophotometric method.

Results: The pH values showed minimal changes for emulsion and gel formulations. The drug is a cationic salt, and it is not able to bind polymer cations by electrostatic repulsion. The rheological property of the vehicle type emulsion was adjusted to plastic and pseudo-plastic fluid to the gels. The drug release was independent of the viscosity of vehicles. Dibucaine release from both types of formulation was found to follow a square-root-of-time kinetic model, but a higher rate of release was obtained from gel formulations.

Conclusions: It was shown that chitosan was adsorbed to the surface of polysorbate 80-coated droplets, and that the electrostatic attraction between the non-ionic surfactant and the drug retarded its release from a semisolid system. The multilayer emulsions showed more influence of the release of drug than CH or CHAc single layer emulsion.

Keywords: dibucaine hydrochloride; chitosan; chitosan acetate; release; semisolid vehicles.

Resumen

Contexto: La quitosana ha recibido gran atención al ser un biopolímero funcional, biodegradable, renovable y no tóxico con múltiples aplicaciones farmacéuticas.

Objetivos: Evaluar la liberación del clorhidrato de dibucaína desde vehículos semisólidos emulsionados aceite/agua y geles acuosos, estabilizados con quitosana (CH) o acetato de quitosana (CHAc).

Métodos: Las emulsiones fueron elaboradas variando el agente emulsificante: polisorbato 80, CH o CHAc, o las combinaciones de CH o CHAc con polisorbato 80, respectivamente. La hidroxipropilmetil celulosa F4M se adicionó como viscosante en el gel. La liberación del fármaco modelo, se realizó empleando bolsas de membranas de diálisis. En la cuantificación del fármaco se utilizó un método espectrofotométrico validado.

Resultados: Los valores de pH mostraron variaciones mínimas en los sistemas emulsionados y geles acuosos. Al ser el fármaco una sal catiónica existe repulsión electrostática con el biopolímero. Los vehículos emulsionados mostraron comportamiento de flujo plástico mientras que los geles pseudoplástico. La liberación de la dibucaína fue independiente de la viscosidad de los vehículos semisólidos. El perfil de liberación, desde ambos sistemas, se ajustó al modelo cinético de la raíz cuadrada del tiempo, siendo la velocidad mayor desde los geles acuosos.

Conclusiones: Se demostró que la quitosana fue adsorbida en la superficie de las gotículas cubiertas con polisorbato 80, y la interacción electrostática entre el surfactante no iónico y el fármaco retardó su liberación desde los sistemas semisólidos. Las combinaciones de emulgentes mostraron mayor influencia sobre la liberación del fármaco que los estabilizados con CH o CHAc.

Palabras Clave: acetato de quitosana; clorhidrato de dibucaina; liberación; quitosana; vehículos semisólidos.

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Citation Format: De la Paz N, Pérez D, Fernández M, García CM, Martínez V, Nogueira A, García O (2017) In vitro release of dibucaine hydrochloride from chitosan semisolid vehicles: emulsion and hydrophilic gels. J Pharm Pharmacogn Res 5(2): 96-105.
This article has been cited by:
De la Paz N, Pérez D, Fernández M, Soler DM, Rodríguez Y, Nogueira A (2017) Physical stability of emulsion and hydrophilic gels with chitosan and chitosan acetate. J Pharm Pharmacogn Res 5(5): 288-300. Website

© 2017 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

In vitro studies of glibenclamide microspheres

J Pharm Pharmacogn Res 5(2): 78-87, 2017.

Original Article | Artículo Original

Evaluation of glibenclamide microspheres for sustained release

[Evaluación de microesferas de glibenclamida para liberación sostenida]

Kambham Venkateswarlu*

Department of Pharmaceutics, JNTUA Oil Technological and Pharmaceutical Research Institute, Ananthapuramu, Andhra Pradesh-515001, India.

*E-mail: k.v.pharmacy@jntua.ac.in

Abstract

Context: Sustained release drug delivery systems are more preferred than the conventional drug delivery systems due to its enhanced bioavailability and patient compliance. Earlier studies reported on glibenclamide (GBCM) were not clear and hence, the step has been taken to explore the sustained release drug delivery system of GBCM.

Aims: To evaluate the sustained release microspheres obtained of GBCM.

Methods: Microspheres were prepared by ionic gelation method using the polymers like Eudragit RS 100 and xanthan gum. Polymers can sustain the drug release from microspheres. The prepared microspheres were subjected to micromeritic studies like Carr’s index, Hausner’s ratio and angle of repose.

Results: Micromeritic studies confirmed that the microspheres possessing acceptable flow properties. It was observed from the in vitro release studies, formulations F8 and F9 showed sustained drug release for desired time of 12 h and when compared to F9, formulation F8 showed maximum drug release for 12 h.

Conclusions: Results confirmed the formulation F8 consist of the polymers such as Eudragit RS 100 about 150 mg and xanthan gum about 100 mg showed desired sustained release of 12 h with 96.07% and kinetic studies confirmed that the release from microspheres followed non-Fickian diffusion mechanism. Due to its sustained release property, it could enhance the bioavailability of drug thereby improves the patient compliance and expect better treatment than conventional dosage forms.

Keywords: Eudragit RS 100; glibenclamide; ionic gelation method; sustained release; xanthan gum.

[SUPPLEMENTARY DATA]

Resumen

Contexto: Los sistemas de suministro de fármacos de liberación sostenida son más preferidos que los sistemas convencionales de administración debido a su mejor biodisponibilidad y al cumplimiento del paciente. Los estudios anteriores sobre glibenclamida (GBCM) no fueron claros, por lo que se decidió explorar el sistema de liberación sostenida de fármacos de GBCM.

Objetivos: Evaluar las microesferas de acción sostenida obtenidas de GBCM.

Métodos: Las microesferas se prepararon mediante un método de gelificación iónica con polímeros como Eudragit RS 100 y goma xantano. Los polímeros pudieron sostener la liberación del fármaco a partir de microesferas. Las microesferas preparadas se sometieron a estudios micromeríticos como el índice de Carr, la relación de Hausner y el ángulo de reposo.

Resultados: Los estudios microméríticos confirmaron que las microesferas poseen propiedades de flujo aceptables. Se observó, a partir de los estudios de liberación in vitro, que las formulaciones F8 y F9 mostraron una liberación sostenida del fármaco durante un tiempo deseado de 12 horas y cuando se comparó con F9, la formulación F8 mostró liberación máxima del fármaco durante 12 h.

Conclusiones: Los resultados confirmaron que la formulación F8 constituida de polímeros tales como Eudragit RS 100 (150 mg) y goma xantano (100 mg) mostró una liberación sostenida deseada de 12 h con 96,07% y estudios cinéticos confirmaron que la liberación de microesferas seguía mecanismo de difusión no Fickiano. Debido a su propiedad de liberación sostenida, esta podría mejorar la biodisponibilidad del fármaco, por lo tanto, mejorar el cumplimiento del paciente y se esperaría un mejor tratamiento que las formas de dosificación convencionales.

Palabras Clave: Eudragit RS 100; glibenclamida; goma xantano; liberación sostenida; método de gelificación iónica.

[SUPPLEMENTARY DATA]

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Citation Format: Venkateswarlu K (2017) Evaluation of glibenclamide microspheres for sustained release. J Pharm Pharmacogn Res 5(2): 78-87.
This article has been cited by:
Manyam N, Reddy Budideti KK, Mogili S (2018) Formulation and in-vitro evaluation of nanosponge loaded extended release tablets of trimethoprim. UPI Journal of Pharmaceutical, Medical and Health Sciences 1(1): 78-86. Website
Kambham Venkateswarlu, Manyam Nirosha, Budideti Kishore Kumar Reddy, Badithala Siva Sai Kiran (2017) Effect of directly compressible excipient and treated agar on drug release of clopidogrel oral disintegrating tablets. Therapeutic Delivery 8(8): 615-624. DOI: 10.4155/tde-2017-0019

© 2017 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

Emulsifying systems of raw material grease from Brazil flora

J Pharm Pharmacogn Res 3(5): 130-140, 2015.

Original Article | Artículo Original

Development and evaluation of emulsifying systems of the material grease from Brazilian flora

[Desarrollo y evaluación de sistemas emulsionantes a partir de grasas de la flora brasileña]

Douglas Dourado1,2*, Camilla Barreto1, Rafaela S. Fernandes1, Ian M.R. Blanco1, Danilo Oliveira3, Neila Pereira1, Mateus F. Leite3

1Laboratory of Research of Medicines and Cosmetics, LAPEMEC. Federal University of Bahia. UFBA, Salvador, Brazil. 2Laboratory of Molecular Interactions and Chemical and Photochemical Reactivity, IMRCP. University Paul Sabatier, Toulouse, France. 3Multidisciplinary Institute for Health, Federal University of Bahia, UFBA, Vitoria da Conquista, Brazil.
Abstract

Context: Oils and butter of seed from Brazilian biodiversity are extending the range of innovative products for cosmetics development. They have a fat potential similar to skin composition, leading to the improved performance of these product.

Aims: Improve the emulsions spreadability through prior screening of grease composition and studying the viscosity, and the emulsions accelerated stability.

Methods: Emulsions were formulated using oils from semiarid plants from Bahia: Syagrus coronate, Pachira retusa, and Pachira aquatica, so as to compare them with oils already standard in the production of cosmetics. Spreadability and stability tests were made comparing the results. The same criteria were used with Amazon seed butter: Virola surinamensis, Butyrospermum parkii, Astrocaryum murumuru, Theobroma cacao and Theobroma grandiflorum. For the emulsions screening and performance, a system was developed for oil/ butter, following tests of accelerated stability, viscosity, and spreadability.

Results: The combined system of spreadability was optimized using screening. Emollients containing oleic and palmitic acids, and light chain fatty acids obtained good spreadability. The oil emulsion containing Pachira retusa and Virola surinamensis butter had a higher viscosity.

Conclusions: With high content of fatty acids such as oleic, palmitic or the light chain fatty acids obtain an appropriated appearance, texture, and spreadability for cosmetic use. Thus, oils with a low fatty acid content may be combined with butter that have a high fatty acid content and vice-versa. Analyzing and strategically combining grease composition, one can optimize the performance of cosmetic formulations.

Keywords: Raw material grease; screening; spreadability; viscosity.

Resumen

Contexto: Los aceites y mantecas de semillas de la biodiversidad brasileña están ampliando la gama de productos innovadores para el desarrollo de los cosméticos. Estos tienen una grasa potencial similar a la composición de la piel, dando lugar a la mejora del rendimiento de estos productos.

Objetivos: Mejorar la capacidad de extensión de las emulsiones mediante el cribado previo de la composición de grasa y el estudio de la viscosidad y la estabilidad acelerada de las emulsione.

Métodos: Las emulsiones se formularon utilizando aceites de plantas semiáridas de Bahía: Syagrus coronata, Pachira retusa, Pachira aquatica y mantecas de semillas de la Amazona: Virola surinamensis, Butyrospermum parkii, Astrocaryum murumuru, Theobroma cacao y Theobroma grandiflorum. Para el cribado y el rendimiento de las emulsiones se desarrolló un sistema aceite/manteca, seguido de pruebas de estabilidad acelerada, viscosidad y extensibilidad.

Resultados: Los emolientes que contenían ácidos oleico y palmítico, y ácidos grasos de cadena ligera obtuvieron buena extensibilidad. La emulsión de aceite de Pachira retusa y manteca de Virola surinamensis tuvo una viscosidad más alta.

Conclusiones: Con un alto contenido de ácidos grasos oleico, palmítico o los ácidos grasos de cadena ligera se obtienen apariencia, textura y extensibilidad adecuadas para uso cosmético. Por lo tanto, los aceites (contenido bajo de ácidos grasos) se pueden combinar con la manteca (alto contenido de ácidos grasos) y viceversa. Analizando y combinando estratégicamente la composición de grasa se puede optimizar el rendimiento de las formulaciones cosmética.

Palabras Clave: Cribado; extensibilidad; materia prima grasa; viscosidad.

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Citation Format: Dourado D, Barreto C, Fernandes RS, Blanco IMR, Oliveira D, Pereira N, Leite MF (2015) Development and evaluation of emulsifying systems of the material grease from Brazilian flora. J Pharm Pharmacogn Res 3(5): 130-140.
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de Sousa Coêlho E, Nunes Lopes GL, Martins Pinheiro I, Policarpo de Holanda JN, de Moraes Alves MM,  Carvalho Nogueira N, de Amorim Carvalho FA, Menezes Carvalho AL (2018) Emulgel based on amphotericin B and bacuri butter (Platonia insignis Mart.) for the treatment of cutaneous leishmaniasis: characterization and in vitro assays. Drug Development and Industrial Pharmacy. DOI: 10.1080/03639045.2018.1492610 
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© 2015 Journal of Pharmacy & Pharmacognosy Research (JPPRes)

CO 060: PEGYLATION: AN EFFECTIVE TOOL FOR BIOMASKING

J Pharm Pharmacogn Res 2(Suppl. 1): S36, 2014

Special supplement with the abstract book of LATINFARMA 2013

Oral Communication

CO 060: PEGYLATION: AN EFFECTIVE TOOL FOR BIOMASKING

Ramón JA1, Saez V1, Peniche C1, Hardy E2.

1Center for Biomaterials, University of Havana, P.O. Box 6130, Havana, Cuba. Email: jose@biomat.uh.cu
2Institute for Science and Technology of Materials, University of Havana, Havana, Cuba.
Abstract

Nowadays, a large group of medical treatments are based on new substances. These were obtained due to strong development of science and technology in last few decades and include: (i) proteins and peptides used as replacement therapy and as inhibitors or regulators of the immune system, (ii) materials used in drug delivery systems like phospholipids and biodegradable polymers, and (iii) metals and their alloys, polymers, ceramics and composites of them used in various devices such as prostheses, stents, heart valves, etc.

Unfortunately the behaviour of these materials in the body is sometimes negative for the initial purpose. For example, proteins and peptides have low stability in vivo, a short half-life time and immunogenicity. Among the problems associated with other materials are: a) thrombus formation on artificial surfaces in contact with living tissues, b) damages to the tissues (e.g. vascular weakening produced by the liposomes) and c) recognition and elimination by the reticuloendothelial system of micro/nano-devices used as DDS like liposomes and biodegradable polymer microspheres.

In general, all these phenomena are due to unwanted interactions that occur at the interfaces between biodrugs or synthetic biomaterials and biological medium. Consequently, any agent that mediates this interaction, and become to this in a more “natural” fashion, promotes the acceptance by living organisms of these “foreign bodies”. An ideal substance for this mediation, it might be call “biomasking”, is the polyethylene glycol (PEG).

This presentation is about advantages of PEGylation (conjugation to PEG) for biomasking. PEGylation is a well-established technology used to transform proteins, peptides, small molecules and oligonucleotides into more potent drugs than their corresponding unmodified native molecules. Furthermore, PEGylated liposomes had received approval for improve the delivery of encapsulated drugs, such as the anticancer agent doxorubicin, and PEG-modified polymers (such as nhexadecylcyanoacrylate and PLGA) are studied extensively to obtain enhanced particulate delivery systems.

CO 059: NOVEL PEGYLATION TECHNOLOGIES FOR THE DEVELOPMENT OF NEXT GENERATION BIODRUGS

J Pharm Pharmacogn Res 2(Suppl. 1): S36, 2014

Special supplement with the abstract book of LATINFARMA 2013

Oral Communication

CO 059: NOVEL PEGYLATION TECHNOLOGIES FOR THE DEVELOPMENT OF NEXT GENERATION BIODRUGS

Ikeda Y1, Katamachi J1, Kawasaki H1, Nagasaki Y2.

1Department of Materials Science, Graduate School of Pure and Applied Sciences, University of Tsukuba, Tennodai 1-1-1, Tsukuba, Ibaraki 305-8573, Japan
2 Master’s School of Medical Sciences, Graduate School of Comprehensive Human Sciences, University of Tsukuba, Tennodai 1-1-1, Tsukuba, Ibaraki 305-8573, Japan. E-mail: ikeda@ims.tsukuba.ac.jp
3Satellite Laboratory, International Center for Materials Nanoarchitectonics (MANA), National Institute of Materials Science (NIMS), Tennodai 1-1-1, Tsukuba, Ibaraki 305-8573, Japan.
Abstract

Introduction: PEGylation refers to the covalent attachment of poly(ethylene glycol) on the biomolecules. PEGylation is recognized as a promising method to increase the therapeutic efficacy of medicines in clinical settings. A variety of molecules have been modified with PEG and several PEGylated drugs have been approved in clinical settings. In this presentation, our recent developments of novel PEGylation technologies on biomolecules will be shown.

Material and methods: For the construction of PEGylated oligonucleotide by solid phase synthesis, a novel solid phase which was pre-installed with PEG was prepared. In the case of protein PEGylation, a novel PEG derivative which possesses glutaraldehyde at one end has been synthesized.

Results: Solid phase synthesis of PEGylated oligonucleotide. A novel solid-phase synthesis method for poly(ethylene glycol) (PEG)oligonucleotide conjugates was developed to increase the stability of therapeutic oligonucleotides such as antisense oligonucleotides and siRNA. A prepared solid phase was pre-installed with PEG to provide oligonucleotides modified with PEG at the 3′ terminus. Compared with the conventional liquid-phase synthesis method, the developed solid-phase method is simple and reproducible. PEGylation at the 3′ terminus was confirmed to stabilize not only DNA but also RNA more than PEGylation at the 5′ terminus, which has been widely used thus far. A novel chemistry for the PEGylated protein with a high activity. Several PEGylated proteins have been approved as therapeutic drugs. In many cases, PEGylated protein has been synthesized by the conjugation reaction between PEG possessing activated ester and amine(s) in the protein. This reaction, however, often causes inactivation of PEGylated proteins.

Conclusions: In this report, we present a novel chemistry which enables the PEGylation of proteins under the mild reaction condition. PEGylated protein prepared by the method developed exhibited much higher biological activity than the PEGylated protein prepared by the conventional method.

CO 058: NANOPARTICLES AS DRUG CARRIERS: CHARACTERISTICS AND PERSPECTIVES

J Pharm Pharmacogn Res 2(Suppl. 1): S35, 2014

Special supplement with the abstract book of LATINFARMA 2013

Oral Communication

CO 058: NANOPARTICLES AS DRUG CARRIERS: CHARACTERISTICS AND PERSPECTIVES

Oropesa-Nuñez R1, Jáuregui-Haza U2.

1Centro de Estudios Avanzados de Cuba (CEAC). Carretera San Antonio, Km 1 1/2, Valle Grande, La Lisa, La Habana, Cuba
2Instituto Superior de Tecnologías y Ciencias Aplicadas (InSTEC). Ave. Salvador Allende y Luaces, Plaza de la Revolución, La Habana, Cuba. E-mail: ulises.jauregui@infomed.sld.cu
Abstract

Nanoparticles can copy or modify biological processes because they propose solutions to the old problems associated with solubility, bioavailability, immunocompatibility and cytotoxicity of many traditional drugs. Carbon nanotubes are an example of nanoparticles and nanotechnology due to their small diameters. They can be manipulated chemically and physically. Besides, they are mainly used in nanomedicine as carriers and as excipients to obtain different drug delivery systems. In this work, the state of the art of the research on nanoparticles as drug carriers for medical applications, with emphasis on their properties, determination of physico-chemical properties and carbon nanotubes applications is analyzed. It is demonstrated that drug formulation and administration has been changed with the advances of nanotechnology. The application of nanoparticles in medicine includes their use as carriers through the functionalization or drug encapsulation. With the use of nanoformulations, an important amount of pharmaceuticals have improved their therapeutic action. The biomedical applications of carbon nanotubes have open a way to a new field in therapy and medical diagnosis. The main part of these applications might consist on the implant of nanotubes or functionalized nanotubes in patients. However, the use of carbon nanotubes in medicine depends on the evaluation of their toxicity in humans.