Development and Evaluation of Transdermal Patches of Quetiapine fumerate for the treatment of psychosis

The aim of the present study was to formulate and evaluate the transdermal patches of an antipsychotic drug Quetiapine fumerate (QF) for the treatment of psychosis and schizophrenia. The transdermal patches was prepared by the solvent evaporation method using hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose (EC) in five different ratios 1:0, 2:1, 1:1, 1:2, 0:1. The PEG-400 and DMSO were used as plasticizers and permeation enhancer respectively to enhance the permeability of the drug. The FTIR studies showed no evidence of incompatibility between the drug and the polymers. The prepared patches were evaluated for various parameters like thickness, weight variation, folding endurance, percentage moisture uptake, percentage moisture content, drug content and in-vitro drug release. The results concluded that the formulation F2 (with HPMC and EC in 2:1 ratio) showed 80.89% in drug release during in-vitro studies after 24 hours. With the incorporation of PEG-400 and DMSO smooth, transparent and flexible film were produced

Formulación de microesferas mucoadherentes de rosiglitazona maleato y su evaluación in vitro usando técnica de gelificación ionotrópica

Aim: The objective of the present study is to design and evaluate mucoadhesive microspheres for oralcontrolled release.Materials and Method: Rosiglitazone maleate microspheres with a coat consisting of alginate and a mucoadhesivepolymer sodium carboxymethylcellulose, carbopol 934P and hydroxypropylmethylcellulosewere prepared by an orifice-ionic gelation process. The microspheres were evaluated for FTIR studies,morphology, particle size, micromeritic properties, percentage entrapment efficiency, in-vitro wash-offtest and in-vitro release studies.Results: The resulting microspheres were spherical and free flowing. The percent entrapment efficiencywas 68.2 to 85.6%. The microspheres exhibited good mucoadhesive property in the in vitro wash-off test.Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h durationof time depending on the composition of coat.Conclusions: The prepared mucoadhesive microspheres are thus suitable for oral controlled release ofRosiglitazone maleate and thereby help in the management of type II diabetes mellitus.Objetivo. El objetivo del presente estudio es diseñar y evaluar las microesferas mucoadherentes de liberacióncontrolada para uso oral.Material y métodos. Las microesferas de rosiglitazona maleato con una capa de alginato y polímerosmucoadherentes de carboximetilcelulosa de sodio, carbopol 934P e hidroxipropilmetilcelulosa fueronelaboradas por un proceso de gelificación iónica de orificio. Las microesferas se evaluaron medianterayos infrarrojos con transformado de Fourier, se estudio la morfología, el tamaño de partícula, las propiedades«micromeritics», el porcentaje de eficacia de entrapamiento, la prueba in vitro de «wash-off» yestudios in vitro de liberación.Resultados. Las microesferas que resultaban eran esféricas y de flujo libre. La eficiencia de captura fuede 68,2 a 85,6%. Las microesferas exhibieron buena propiedad mucoadherentes en el ensayo in vitro delavado. La liberación lde las microesferas mucoadherentes de Rosiglitazona fue lento y se prolongadomás de 12 h dependiendo de la composición de la capa.Conclusiones. Las microesferas preparadas con mucoadherentes son convenientes para la liberaciónoral controlada de rosiglitazona maleato y así ayudar en el tratamiento de la diabetes mellitus tipo II

DESIGN AND OPTIMIZATION OF SOLID LIPID NANOPARTICLES (SLNs) OF ZOLMITRIPTAN FOR THE MANAGEMENT OF MIGRAINE

Solid lipid nanoparticles (SLNs) of zolmitriptan were produced by solvent emulsification-diffusion technique. Soya lecithin and poloxamer 188 were used as surfactants and stabilizers of the particles. The formulations were optimized for independent variables (amount of stearic acid, amount of lecithin and homogenization time) in order to achieve desired particle size with maximum percent entrapment efficiency (% EE). Prepared SLNs were characterized by transmission electron microscopy (TEM), atomic force microscopy (AFM) and zeta potential measurements. To achieve our goal, eight formulations (F1–F8) of SLNs were prepared by solvent injection technique and optimized by 23 full-factorial design. The responses of the design were analyzed using Minitab 15. On the basis of software analysis, formulation F8 was selected as optimized formulation and was evaluated for the independent parameters. Optimized formulation showed particle size of 340nm, percent entrapment efficiency (EE) of 81.36 and 79.11% of in-vitro drug release after 24h. The release kinetics of the optimized formulation best fitted the Higuchi model.Key words: solid lipid nanoparticles, zolmitriptan, solvent emulsificationdiffusion technique, in-vitro release

Development and Evaluation of Transdermal Patches of Quetiapine fumerate for the treatment of psychosis

The aim of the present study was to formulate and evaluate the transdermal patches of an antipsychotic drug Quetiapine fumerate (QF) for the treatment of psychosis and schizophrenia. The transdermal patches was prepared by the solvent evaporation method using hydroxy propyl methyl cellulose (HPMC) and ethyl cellulose (EC) in five different ratios 1:0, 2:1, 1:1, 1:2, 0:1. The PEG-400 and DMSO were used as plasticizers and permeation enhancer respectively to enhance the permeability of the drug. The FTIR studies showed no evidence of incompatibility between the drug and the polymers. The prepared patches were evaluated for various parameters like thickness, weight variation, folding endurance, percentage moisture uptake, percentage moisture content, drug content and in-vitro drug release. The results concluded that the formulation F2 (with HPMC and EC in 2:1 ratio) showed 80.89% in drug release during in-vitro studies after 24 hours. With the incorporation of PEG-400 and DMSO smooth, transparent and flexible film were produced

ANTIMICROBIAL ACTIVITY AND PHYTOCHEMICAL SCREENING OF LEAVES EXTRACT OF MORINDA PUBESCENS LINN. PLANT

The ethanolic extracts of leaves of Morinda pubescens Linn. were explored for their phytochemical constituents and antimicrobial activity. The preliminary evaluation of ethanolic extract exhibited appreciable antimicrobial activity on the tested pathogenic bacterial isolates at a concentration of 100mg/g and displayed inhibitory potency (20-22mm) in diameter on the tested bacterial isolates. Phenol and alkaloids was found to be present in the plant parts while highest phenolic constituent was recorded in the leaves extract

Preparation and <i>In-vitro</i> Evaluation of Metformin Microspheres Using Non-Aqueous Solvent Evaporation Technique

Purpose: To prepare and evaluate metformin microspheres for prolonged release. Methods: Metformin microspheres were prepared by non-aqueous solvent evaporation method using various polymers, including ethylcellulose (EC), hydroxypropyl methylcellulose (HPMC), carbopol 934P (CA) and chitosan (CH). The effect of process variables, viz, drug/polymer ratio, stirring rate and type of polymer on the mean particle size, drug entrapment efficiency, yield, drug content, micromeritic properties and drug release of the microspheres were studied. Results: It was observed that as the stirring speed increased from 600 to 1800 rpm, microsphere size decreased and hence drug release rate increased. Drug release rate at 1:2 drug: polymer for microspheres produced at a stirring rate of 1200 rpm was in the following order: carbopol 934P > HPMC > ethyl cellulose > chitosan. The formulations containing carbopol 934P (CA3) and HPMC (HPMC3) released drug faster than chitosan microspheres (CH3). Conclusion: Amongst the developed microspheres, CH3 formulation (with chitosan as the polymer) exhibited maximum prolonged drug release at gastrointestinal pH or at least 15 h. This oral sustained metformin formulation could potentially improve the bioavailability of the drug as well as patient compliance

Formulation of mucoadhesive microspheres of rosiglitazone maleate and its in vitro evaluation using ionotropic gelation technique

Aim: The objective of the present study is to design and evaluate mucoadhesive microspheres for oral controlled release. Materials and Method: Rosiglitazone maleate microspheres with a coat consisting of alginate and a mucoadhesive polymer sodium carboxymethylcellulose, carbopol 934P and hydroxypropylmethylcellulose were prepared by an orifice-ionic gelation process. The microspheres were evaluated for FTIR studies, morphology, particle size, micromeritic properties, percentage entrapment efficiency, in-vitro wash-off test and in-vitro release studies. Results: The resulting microspheres were spherical and free flowing. The percent entrapment efficiency was 68.2 to 85.6%. The microspheres exhibited good mucoadhesive property in the in vitro wash-off test. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of coat. Conclusions: The prepared mucoadhesive microspheres are thus suitable for oral controlled release of Rosiglitazone maleate and thereby help in the management of type II diabetes mellitus

Formulación de microesferas mucoadherentes de rosiglitazona maleato y su evaluación in vitro usando técnica de gelificación ionotrópica

Aim: The objective of the present study is to design and evaluate mucoadhesive microspheres for oral controlled release. Materials and Method: Rosiglitazone maleate microspheres with a coat consisting of alginate and a mucoadhesive polymer sodium carboxymethylcellulose, carbopol 934P and hydroxypropylmethylcellulose were prepared by an orifice-ionic gelation process. The microspheres were evaluated for FTIR studies, morphology, particle size, micromeritic properties, percentage entrapment efficiency, in-vitro wash-off test and in-vitro release studies. Results: The resulting microspheres were spherical and free flowing. The percent entrapment efficiency was 68.2 to 85.6%. The microspheres exhibited good mucoadhesive property in the in vitro wash-off test. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of coat. Conclusions: The prepared mucoadhesive microspheres are thus suitable for oral controlled release of Rosiglitazone maleate and thereby help in the management of type II diabetes mellitus.Objetivo. El objetivo del presente estudio es diseñar y evaluar las microesferas mucoadherentes de liberación controlada para uso oral. Material y métodos. Las microesferas de rosiglitazona maleato con una capa de alginato y polímeros mucoadherentes de carboximetilcelulosa de sodio, carbopol 934P e hidroxipropilmetilcelulosa fueron elaboradas por un proceso de gelificación iónica de orificio. Las microesferas se evaluaron mediante rayos infrarrojos con transformado de Fourier, se estudio la morfología, el tamaño de partícula, las propiedades «micromeritics», el porcentaje de eficacia de entrapamiento, la prueba in vitro de «wash-off» y estudios in vitro de liberación. Resultados. Las microesferas que resultaban eran esféricas y de flujo libre. La eficiencia de captura fue de 68,2 a 85,6%. Las microesferas exhibieron buena propiedad mucoadherentes en el ensayo in vitro de lavado. La liberación lde las microesferas mucoadherentes de Rosiglitazona fue lento y se prolongado más de 12 h dependiendo de la composición de la capa. Conclusiones. Las microesferas preparadas con mucoadherentes son convenientes para la liberación oral controlada de rosiglitazona maleato y así ayudar en el tratamiento de la diabetes mellitus tipo II

Preparation and In-vitro Evaluation of Metformin Microspheres Using Non-Aqueous Solvent Evaporation Technique

Purpose: To prepare and evaluate metformin microspheres for prolonged release. Methods: Metformin microspheres were prepared by non-aqueous solvent evaporation method using various polymers, including ethylcellulose (EC), hydroxypropyl methylcellulose (HPMC), carbopol 934P (CA) and chitosan (CH). The effect of process variables, viz, drug/polymer ratio, stirring rate and type of polymer on the mean particle size, drug entrapment efficiency, yield, drug content, micromeritic properties and drug release of the microspheres were studied. Results: It was observed that as the stirring speed increased from 600 to 1800 rpm, microsphere size decreased and hence drug release rate increased. Drug release rate at 1:2 drug: polymer for microspheres produced at a stirring rate of 1200 rpm was in the following order: carbopol 934P > HPMC > ethyl cellulose > chitosan. The formulations containing carbopol 934P (CA3) and HPMC (HPMC3) released drug faster than chitosan microspheres (CH3). Conclusion: Amongst the developed microspheres, CH3 formulation (with chitosan as the polymer) exhibited maximum prolonged drug release at gastrointestinal pH or at least 15 h. This oral sustained metformin formulation could potentially improve the bioavailability of the drug as well as patient compliance

Formulación de microesferas mucoadherentes de rosiglitazona maleato y su evaluación in vitro usando técnica de gelificación ionotrópica

Aim: The objective of the present study is to design and evaluate mucoadhesive microspheres for oral controlled release. Materials and Method: Rosiglitazone maleate microspheres with a coat consisting of alginate and a mucoadhesive polymer sodium carboxymethylcellulose, carbopol 934P and hydroxypropylmethylcellulose were prepared by an orifice-ionic gelation process. The microspheres were evaluated for FTIR studies, morphology, particle size, micromeritic properties, percentage entrapment efficiency, in-vitro wash-off test and in-vitro release studies. Results: The resulting microspheres were spherical and free flowing. The percent entrapment efficiency was 68.2 to 85.6%. The microspheres exhibited good mucoadhesive property in the in vitro wash-off test. Rosiglitazone release from these mucoadhesive microspheres was slow and extended over 12 h duration of time depending on the composition of coat. Conclusions: The prepared mucoadhesive microspheres are thus suitable for oral controlled release of Rosiglitazone maleate and thereby help in the management of type II diabetes mellitus.Objetivo. El objetivo del presente estudio es diseñar y evaluar las microesferas mucoadherentes de liberación controlada para uso oral. Material y métodos. Las microesferas de rosiglitazona maleato con una capa de alginato y polímeros mucoadherentes de carboximetilcelulosa de sodio, carbopol 934P e hidroxipropilmetilcelulosa fueron elaboradas por un proceso de gelificación iónica de orificio. Las microesferas se evaluaron mediante rayos infrarrojos con transformado de Fourier, se estudio la morfología, el tamaño de partícula, las propiedades «micromeritics», el porcentaje de eficacia de entrapamiento, la prueba in vitro de «wash-off» y estudios in vitro de liberación. Resultados. Las microesferas que resultaban eran esféricas y de flujo libre. La eficiencia de captura fue de 68,2 a 85,6%. Las microesferas exhibieron buena propiedad mucoadherentes en el ensayo in vitro de lavado. La liberación lde las microesferas mucoadherentes de Rosiglitazona fue lento y se prolongado más de 12 h dependiendo de la composición de la capa. Conclusiones. Las microesferas preparadas con mucoadherentes son convenientes para la liberación oral controlada de rosiglitazona maleato y así ayudar en el tratamiento de la diabetes mellitus tipo II