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

STABILITY INDICATING REVERSED PHASE-HIGH PERFORMANCE LIQUID CHROMATOGRAPHY METHOD DEVELOPMENT AND VALIDATION FOR SIMULTANEOUS DETERMINATION OF RELATED SUBSTANCES OF CITICOLINE AND PIRACETAM IN PHARMACEUTICAL DOSAGE FORM

ABSTRACTObjective: A high-performance liquid chromatography (HPLC) method was developed and validated to determine stability indicating method ofPiracetam and Citicoline in a tablet dosage.Methods: The separation was made using Inertsil C18, 250 × 4.6 mm, 5 µm column, mobile phase used contained phosphate buffer and acetonitrilein the gradient mode at wavelength of 205 nm for Piracetam and 280 nm for Citicoline on a PDA detector.Results: The method showed good linearity for, respectively related substances of Citicoline and Piracetam with correlation coefficients in the rangeof 0.29-623 µg/mL and 0.48-1030 µg/mL, respectively. Method accuracy was assessed at three levels; the recovery ranged between 100.0% and 102%for Citicoline and for Piracetam between 94.3% and 109.1%. Limit of detection and quantification for Citicoline was 0.07 µg/mL - 0.25 µg/ml and forPiracetam 0.12 µg/mL - 0.41 µg/ml. The solution was found to be stable within 27 hrs at room temperature.Conclusion: The method was demonstrated to be robust and simple, and suitable for industrial application for determination of related substancesin the pharmaceutical preparation.Keywords: Piracetam, Citicoline, Assay, Reversed phase-high performance liquid chromatography

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

Formulation and evaluation of floating microspheres of losartan potassium using sodium alginate and HPMC by solvent evaporation method

Hollow multі-unіt mіcrospheres were prepared by a solvent dіffusіon technіque іn emulsіon wіth a drug and an acrylіc polymer. These were dіssolved іn a mіxture of ethanol-dіchloromethane and poured іnto an aqueous solutіon of PVA wіth stіrrіng to form emulsіon droplets. The rate of drug release іn mіcro balloons was controlled by changіng the ratіo of polymer to drug. The mіcroballoons were floatіng іn vіtro for 12-24 hours when submerged іn aqueous medіa. Radіographіc studіes showed that mіcroballons admіnіstered orally to humans were dіspersed іn the upper part of the stomach and were held there for 3 hours agaіnst perіstaltіc movement. Floating Microspheres of Losartan potassium were formed by Solvent Evaporation method .The formulas LP7 of Losartan Potassium Floating Microspheres shows a very good drug release profiles and shown better sustained action till the end of last hour (24th hrs). It will improve patient compliance and increase in bioavailability which give better approach to treat hypertensive condition and the angiotensin receptor blocking action of Losartan lower the long term complications of Hypertension and reduce the risk of heart failure, CHF, Myocardial Infarction and also vascular damage in blood vessels and kidney. Keywords: Losartan Potassium, Floating microspheres, Drug Entrapment, In-vitro drug release

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

Formulation and evaluation of floating microspheres of lovastatin using Eudragit-E and ethyl cellulose by solvent evaporation method

Hollow multі-unіt mіcrospheres were prepared by a solvent dіffusіon technіque іn emulsіon wіth a drug and an acrylіc polymer. These were dіssolved іn a mіxture of ethanol-dіchloromethane and poured іnto an aqueous solutіon of PVA wіth stіrrіng to form emulsіon droplets. The rate of drug release іn mіcro balloons was controlled by changіng the ratіo of polymer to drug. The mіcroballoons were floatіng іn vіtro for 12-24 hours when submerged іn aqueous medіa. Radіographіc studіes showed that mіcroballons admіnіstered orally to humans were dіspersed іn the upper part of the stomach and were held there for 3 hours agaіnst perіstaltіc movement. Floating Microspheres of Lovastatin were formed by Solvent Evaporation method .The formulas LV7 of Lovastatin Floating Microspheres shows a very good drug release profiles and shown better sustained action till the end of last hour (24th hrs). It will improve patient compliance and increase in bioavailability which give better approach to treat hypertensive condition and the antihyperlipidemic action of Lovastatin lower the long term complications of Hypertension and reduce the risk of heart failure, CHF, Myocardial Infarction and also vascular damage in blood vessels and kidney. Keywords: Lovastatin, Floating microspheres, Drug Entrapment, In-vitro drug release

Inulin: A promising carrier for controlled and targeted drug delivery system

The delivery of a drug to the preferred site of action is referred to as drug targeting. The benefits of drug targeting are a reproducible and controlled release rate of the therapeutic compound, which forestalls overdose. Due to the potential to treat colonic diseases with minimum side effects, colon targeting has become of high interest over the last decades. Inulin was investigated for its potential as encapsulation material regarding its enzymatic degradability and its drug release behaviour. Inulin is a polysaccharide with a widespread range of therapeutic uses such as a carrier in a drug delivery vehicle, as a diagnostic/analytical tool or as a dietary fibre with additional health benefits. In the main, much research has focused on inulin as a drug delivery carrier for colon-specific drug delivery. The justification for this is its potential to survive in the stomach’s acidic environment. This unique stability and strength are utilized in many ways to deliver drugs safely to the colon, where they can be easily absorbed through the gut epithelium into the blood. There are also some proofs that inulin’s prebiotic features also lead to health benefits, mainly for patients with inflammatory bowel disease or in the prevention of colonic cancer. Inulin based hydrodynamic research will be useful to discover the potential of inulin

Thin Films: A Promising Approach for Drug Delivery System

The prime goal of drug delivery through drug carrier system to the specific target site at the suitable concentration for therapeutic action. Recently thin films are acquiring attention as drug carrier and various scientists are working on the formulation and development of thin films as a novel drug delivery system. Because of its capacity to safely load medications and release them in a regulated manner, thin films have attracted increasing interest in the field of drug delivery, which improves drug efficacy. They are more patient compliance and alternative to oral drug delivery employing self-application, prolonged action and easily terminate if drug toxicity is produced. Oral, buccal, sublingual, ocular, and transdermal routes have all been employed to deliver this delivery mechanism for both systemic and local effects. The development of thin films comprises of various methods with keeping in mind the anatomical and physiological constraints, physicochemical properties and types of drug substance and use of various polymers (matrix, hydrophilic and hydrophobic) as well as the characterisation methods with recent trends