Formulación y evaluación de vesículas de liposomas de baclofeno usando lecitina

I express my sincere regards and respect to RIC and Pharmaceutical Sciences of IKG Punjab Technical University, Jalandhar, for their support and kind cooperationIntroducción: El objetivo principal del presente estudio fue preparar y caracterizar la formulación liposomal de baclofeno para mejorar la efectividad de la formulación aplicada tópicamente. Método: Para la preparación de liposomas, se tomaron diferentes proporciones de lecitina, colesterol y etanol, pero la proporción de fármaco y ácido esteárico se mantuvo constante y se preparó mediante el método de inyección de etanol. Los liposomas se caracterizaron por tamaño de vesícula, forma de vesícula, eficacia de atrapamiento, estudios in vitro, estudios de estabilidad y estudios in vivo. Resultados: El tamaño promedio de partícula del liposoma formulado estuvo en el rango de 3.98 ± 0,45-4,24 ± 0,65 µm y se observaron pequeñas vesículas unilamelares con forma esférica. La eficiencia de atrapamiento de la formulación optimizada fue de 58,67 ± 0,81%. El % máximo de comportamientos acumulativos de liberación de drogas fue 67,66 ± 5,32% después de 10 h. la formulación almacenada a una temperatura de 4 ± 2 ° C muestra una mejor estabilidad (64,19±0,26) en comparación con la temperatura elevada. Se usaron ratones albinos suizos para el estudio in vivo y exhiben actividad relajante muscular en términos de no. de caídas del aparato de varilla giratoria (valor p = 0,001). Conclusiones: la formulación liposomal cargada de baclofeno ha mostrado actividad relajante del músculo esquelético en ratones, lo que sugiere la administración de baclofeno desde los liposomas en el rango terapéutico.Introduction: The main aim of present study was to prepare and characterize liposomal formulation of baclofen to improve the effectiveness of the topically applied formulation. Method: For the preparation of liposomes, different ratio of lecithin, cholesterol and ethanol were taken but ratio of drug and stearic acid were kept constant and prepared by ethanol injection method. Liposomes were characterized for vesicle size, vesicle shape, entrapment efficiency, in vitro studies, stability studies and in vivo studies. Results: The average particle size of formulated liposome was in the range of 3.98±0.45-4.24±0.65 µm and small unilamellar vesicles with spherical in shape observed. Entrapment efficiency of optimized formulation was 58.67±0.81 %. The maximum % cumulative drug release behaviours were 67.66±5.32 % after 10 h. formulation stored in 4±2 °C temperature shows better stability (64.19±0.26) compared to elevated temperature. Swiss albino mice were used for the in vivo study and exhibit muscle relaxant activity in terms of no. of falls from rota rod apparatus (p value =0.001). Conclusions: Baclofen loaded liposomal formulation have shown skeletal muscle relaxant activity in mice suggesting delivery of baclofen from liposomes in the therapeutic range

Methoxsalen loaded chitosan coated microemulsion for effective treatment of psoriasis

Methoxsalen has been used for the treatment of psoriasis. In order to develop alternative formulations for the topical administration of methoxsalen, chitosan coated microemulsion were evaluated as delivery vehicle. Microemulsions were prepared using water, soyabean oil. Egg phosphatidylcholine, ethanol and coated with chitosan. They were characterized for shape and surface morphology, droplet size and size distribution, zeta potential, pH and viscosity. The ability of the system to deliver into the skin was evaluated using dialysis membrane and human cadaver skin. The in vitro permeation data showed that the novel system cumulative amount released was 18.75 % lesser than the microemulsion. These studies clearly show that methoxsalen loaded chitosan-coated microemulsion provides control release of methoxsalen with retention on the skin. Therefore may be appropriate vehicle for topical delivery of methoxsalen.Keywords: Microemulsions; Soyabean; Methoxsalen; Chitosa

Formulation and in vitro characterization of metoprolol tartrate loaded chitosan microspheres

Objetivos: El objetivo principal del presente estudio es el de facilitar la administración intranasal de tartrato de metoprolol (cardioselectivo β1-bloqueante), mediante la formulación de microesferas mucoadhesivas.Métodos: Las microesferas se preparan por precipitación iónica y el método químico de reticulación. Las microesferas se caracterizaron mediante determinación del tamaño de partícula, morfología de la superficie, la eficiencia de atrapamiento, estudio in vitro de la liberación del fármaco y por espectroscopia infrarroja.Resultados: El tamaño de partícula y retención máxima de formulación optimizada (MT 4) fue de 1897 nm y 94,19± 0,015%, respectivamente. La liberación del fármaco in vitro en una solución salina de tampón fosfato (pH=7,4) fue 97,88 ± 0,02% en la formulación de MF1. La tasa de liberación del fármaco puede ser adaptada mediante la manipulación del grado de cristalinidad, la menor cristalinidad favorece una liberación mas lenta. El fármaco empleado puede inducir la escisión de la cadena de polímeros a través de la degradación del nucleófilo. Los resultados de los análisis de infrarrojos no moistraron ningún tipo de alteración producida por el proceso de microencapsulación.Conclusiones: el tartrato de metoprolol liberado en la mucosa nasal es aceptable para conseguir reducir los niveles elevados de presión arterial.Aim: The main objective of present study was to facilitate intranasal delivery of Metoprolol tartrate (cardioselective β1-blocker) by formulating mucoadhesive microspheres.Methods: The microspheres were prepared by ionic precipitation and chemical cross-linking method. Microsphere formulations were characterized for particle size, surface morphology, entrapment efficiency, in vitro drug release and Infrared Spectroscopy.Results: The particle size and maximum entrapment of optimized formulation (MT 4) was found to be 1897 nm, 94.19±0.015 %, respectively. In vitro drug release in phosphate buffer saline (pH 7.4) was maximum (97.88±0.02 %) in formulation MF1. The drug release rate can be tailored by manipulating the degree of crystallinity, reduced crystallinity is favorable when slow release is desired. The drug employed can induce polymer chain scission through nucleophilic degradation. The results of the infrared analysis were in agreement with reference as no new chemical species after the microencapsulation process was observed.Conclusions: To conclude, the drug (metoprolol tartrate) thus released in nasal mucosa will attain therapeutic plasma concentration and reduce elevated blood pressure levels

Sistema de administración de fármacos autoemulsionante: una estrategia para mejorar la biodisponibilidad oral

Objetivo: La vía oral siempre ha sido la ruta preferida de administración de fármacos en muchas enfermedades y hasta hoy es la primera forma investigada en el desarrollo de nuevas formas de dosificación. El principal problema en las formulaciones de fármacos orales es la baja y errática biodisponibilidad, lo que resulta fundamentalmente por la escasa solubilidad en agua, con lo que plantean problemas en su formulación. Para la administración terapéutica de los grupos activos lipófilos (BCS clase II drogas), las formulaciones a base de lípidos están teniendo cada vez más atención. Métodos: Con ese objetivo, a partir de los sitios web de PubMed, HCAplus, Thomson, y sus registros se utilizaron como fuentes principales para llevar a cabo la búsqueda de los artículos de investigación más importantes publicados sobre el tema. A continuación, la información fue analizada cuidadosamente, poniendo de relieve los resultados más importantes en la formulación y desarrollo de sistemas de administración de fármacos auto-emulsionante micro, así como su actividad terapéutica. Resultados: El sistema de administración de fármacos autoemulsionante (SMEDDS) ha ganado más atención debido a la mejorada que permite la reducción de la biodisponibilidad oral en dosis, los perfiles temporales más consistentes de la absorción del fármaco, la orientación selectiva de fármaco (s) hacia la ventana de absorción específica en el tracto gastrointestinal, y la protección del fármaco (s) desde el entorno poco receptivo en el intestino. Conclusiones: Este artículo proporciona una visión completa de SMEDDS como un enfoque prometedor para abordar eficazmente el problema de moléculas poco solubles.Aim: Oral route has always been the favorite route of drug administration in many diseases and till today it is the first way investigated in the development of new dosage forms. The major problem in oral drug formulations is low and erratic bioavailability, which mainly results from poor aqueous solubility, thereby pose problems in their formulation. For the therapeutic delivery of lipophilic active moieties (BCS class II drugs), lipid based formulations are inviting increasing attention. Methods: To that aim, from the web sites of PubMed, HCAplus, Thomson, and Registry were used as the main sources to perform the search for the most significant research articles published on the subject. The information was then carefully analyzed, highlighting the most important results in the formulation and development of self-micro emulsifying drug delivery systems as well as its therapeutic activity. Results: Self-emulsifying drug delivery system (SMEDDS) has gained more attention due to enhanced oral bio-availability enabling reduction in dose, more consistent temporal profiles of drug absorption, selective targeting of drug(s) toward specific absorption window in GIT, and protection of drug(s) from the unreceptive environment in gut. Conclusions: This article gives a complete overview of SMEDDS as a promising approach to effectively deal with the problem of poorly soluble molecules

Novel vesicular approach for topical delivery of baclofen via niosomes

Niosomes have been reported as a possible approach to improve the low skin penetration and bioavailability characteristics shown by conventional topical vehicle for Baclofen (centrally acting skeletal muscle relaxant). Niosomes were prepared by lipid film hydration method using non ionic surfactant (Span 20) and cholesterol in varying molar ratios such as 1:1, 1:2 and 2:1. The prepared systems were characterized for vesicle surface morphology, entrapment efficiency, Osmotic fragility and stability studies. The in vitro drug release behavior was determined by an in-house fabricated dissolution-dialysis apparatus. The skeletal muscle relaxant activity was determined by rota rod method using Swiss albino mice. The average particle size of niosomes was in the range of 3260-3810 nm. The maximum percent drug entrapment was observed with span 20 (89.67 ± 0.46 %). Furthermore, the release profile of baclofen from these niosomes was 68.15 ± 1.7 % (maximum). The formulations kept for stability studies have exhibited percent drug entrapment value of 87.93 ± 0.34 % under refrigerated milieu (4 ± 2 °C). The mice treated with formulations have shown improved muscle relaxation activity which was evident by increased number of falls in rota rod test as compared to plane drug treated mice (p value = 0.001).Colegio de Farmacéuticos de la Provincia de Buenos Aire

EBOLA VIRUS DISEASE AND ITS COMPLICATIONS

In African countries Ebola virus has been responsible for several deaths. In addition to being a global health concern, the virus is also considered a potential biological threat.  Ebola viruses are incompletely understood pathogens that cause severe, often fatal, illnesses in humans and non-human primates. Ebola virus disease affects most of the human being and finally mortality rate increases in that county. Most of the countries are on alert for the ebola virus because peoples have worked within the boundaries of the affected area of Africa. Such people are not permitted to enter in the resident country without proper test at airport or other places.  In this review we have discussed ebola virus disease and  it affects the peoples worldwide. Peer Review History: Article received on- 3 August;    Revised on- 10 September; Accepted on- 15 October , Available online 15 November 2016 Academic Editor: Dr. DANIYAN Oluwatoyin Michael, Obafemi Awolowo University, ILE-IFE, Nigeria, [email protected] UJPR follows the most transparent and toughest ‘Advanced OPEN peer review’ system. The identity of the authors and, reviewers will be known to each other. This transparent process will help to eradicate any possible malicious/purposeful interference by any person (publishing staff, reviewer, editor, author, etc) during peer review. As a result of this unique system, all reviewers will get their due recognition and respect, once their names are published in the papers. We expect that, by publishing peer review reports with published papers, will be helpful to many authors for drafting their article according to the specifications. Auhors will remove any error of their article and they will improve their article(s) according to the previous reports displayed with published article(s). The main purpose of it is ‘to improve the quality of a candidate manuscript’. Our reviewers check the ‘strength and weakness of a manuscript honestly’. There will increase in the perfection, and transparency. Received file:        Reviewer's Comments: Average Peer review marks at initial stage: 5.0/10 Average Peer review marks at publication stage: 7.5/10 Reviewer(s) detail: Dr. Viney Chawla, University Institute of Pharmaceutical Sciences, Baba Farid University of Health Sciences, Sadiq Road, Faridkot-Punjab 151203, [email protected] Dr. Tamer Elhabibi, Suez Canal University, Egypt, [email protected]

Stability indicating method development and validation for simultaneous estimation of atorvastatin calcium and celecoxib in bulk and niosomal formulation by RP-HPLC

The present work describes development and validation of a specific, sensitive, precise and stability-indicating high-performance liquid chromatographic method of analysis of atorvastatin calcium and celecoxib, both as a bulk drug and in niosomal formulation. The analysis has been performed by using Cosmosil-C18 column (4.6 mm´250 mm, 5 m) at 25 °C using acetonitrile: ammonium acetate buffer pH 5.0: methanol (50:25:25 v/v/v) as mobile phase. The detection was carried out at 277nm with a flow rate of 1.0mL/min. The retention times of Atorvastatin calcium and Celecoxib were 6.195 and 3.989min, respectively. The method was validated according to ICH guidelines, for specificity, precision, linearity, accuracy and robustness. Atorvastatin calcium and Celecoxib were subjected to stress conditions of hydrolysis, oxidation, photolysis and thermal degradation. The degradation was observed in oxidation and acid hydrolysis. The linearity for atorvastatin calcium and celecoxib were in the range of 100-500 µg/mL. The recovery study of atorvastatin and celecoxib were found to be in the range of 98.96 - 99.92% and 98.90-100%, respectively. The proposed method was validated and successfully applied to the estimation of Atorvastatin calcium and Celecoxib in combined in-house niosomal formulation.O presente trabalho descreve o desenvolvimento e a validação de método de análise por cromatografia de alta eficiência específico, sensível, preciso e indicador de estabilidade de atorvastatina cálcica e celecoxibe, ambos como fármaco e como formulação niosômica. A análise foi realizada utilizando coluna Cosmosil-C18 (4,6 mm´250 mm, 5 m) a 25 °C, e acetonitrila: tampão acetato de amônio pH 5,0: metanol (50:25:25 v/v/v) como fase móvel. A detecção foi realizada a 277 nm, com fluxo de 1,0 mL/min. Os tempos de retenção de atorvastatina cálcica e de celecoxibe foram 6,195 e 3,989 min, respectivamente. O método foi validado de acordo com as regras da ICH para especificidade, precisão, exatidão e robustez. A atorvastatina cálcica e o celecoxibe foram submetidos a condições de estresse por hidrólise, oxidação, fotólise e degradação térmica. A degradação foi observada por oxidação e hidrólise ácida. Observou-se a linearidade da atorvastatina cálcica e do celecoxibe na faixa de 100-500 µg/mL. A recuperação da atorvastatina e do celecoxibe foi observada na faixa de 98,96-99,92% e 98,90-100%, respectivamente. O método proposto foi validado e aplicado com sucesso para a determinação de atorvastatina cálcica e celecoxibe em formulação niosômica caseira combinada