Formulation and evaluation of carvedilol microcapsules using Eudragit NE30D and sodium alginate

Inclusion complexes of carvedilol(CR) with hydroxyl propyl beta-cyclodextrin (HPBCD) was prepared using co-grinding technique. Then, the inclusion complex was microencapsulated using combinations of Eudragit NE30D (EU) and sodium alginate (SA) utilizing orifice gelation technique. The formulations were analysed by using Scanning electron microscopy (SEM), Fourier Transform Infrared spectroscopy (FTIR), Differential scanning Calorimetry (DSC) and X-ray diffractometer (XRD) and also evaluated for particle size, encapsulation efficiency, production yield, swelling capacity, mucoadhesive properties, zeta potential and drug release. The microcapsules were smooth and showed no visible cracks and extended drug release of 55.2006% up to 12 hours in phosphate buffer of pH 6.8, showing particle size within the range of 264.5-358.5 µm, and encapsulation efficiency of 99.337±0.0100-66.2753±0.0014%.The in vitro release data of optimized batch of microcapsules were plotted in various kinetic equations to understand the mechanisms and kinetics of drug release, which followed first order kinetics, value of "n" is calculated to be 0.459 and drug release was diffusion controlled. The mice were fed with diet for inducing high blood pressure and the in vivo antihypertensive activity of formulations was carried out administering the optimized formulations and pure drug separately by oral feeding and measured by B.P Monwin IITC Life Science instrument and the results indicated that the bioavailability of carvedilol was increased both in vitro and in vivo with the mucoadhesive polymers showing primary role in retarding the drug release.Prepararam-se complexos de carvedilol (CR) com hidroxipropil beta-ciclodextrina (HPBCD), utilizando a técnica de co-moagem. O complexo de inclusão foi microencapsulado empregando-se associações de Eudragit NE30D (EU) e alginato de sódio (AS), utilizando a técnica de gelificação de orifício. As formulações foram analisadas utilizando-se microscopia eletrônica de varredura (SEM), espectroscopia no infravermelho com Transformada de Fourier, calorimetria diferencial de varredura (DSC) e difratometria de raios X (XDR) e, também, avaliadas por tamanho de partícula, eficiência de encapsulação, rendimento de produção, capacidade de inchamento, propriedades mucoadesivas, potencial zeta e liberação do fármaco. Obtiveram-se microcápsulas lisas e sem fendas visíveis, com liberação prolongada do fármaco de 55,2006% em 12 horas em tampão fosfato pH 6,8, com tamanho de partículas na faixa de 264,5-358,5 mm e eficiência de encapsulação de 99,3337±0,0100-66,2753±0,0014%. Os dados de liberação in vitro de lote otimizado de microcápsulas foram plotados em várias equações cinéticas para se entender os mecanismos e a cinética de liberação do fármaco, que é de primeira ordem, o valor de "n" foi de 0,459 e a liberação do fármaco foi por difusão controlada. Os camundongos foram alimentados com dieta para induzir pressão sanguínea alta e a atividade anti-hipertensiva in vivo das formulações foi obtida por administração de formulações otimizadas e fármaco puro, separadamente, por via oral e medida pelo equipamento BP Monwin IITC Life Science. Os resultados mostraram que a biodisponibilidade do carvedilol aumentou tanto in vitro quanto in vivo com os polímeros mucoadesivos, mostrando papel principal no retardamento da liberação do fármaco

A Statistical Approach Towards Development and Optimization of Conventional Immediate Release Tablet of Nimorazole by Wet Granulation Technique: Conventional immediate release tablet of nimorazole by wet granulation technique

Till date, most of the drugs have been given in conventional immediate release dosage form. Nimorazole is an anticancer drug, used as a hypoxic radiosensitizer in patients undergoing radiotherapy and no formulation has been available in the market till now. Hence, for the purpose to develop an immediate release dosage form, a statistical optimization process has been employed to quantify the effect of two primary excipient MCC and maize starch on its immediate release characteristics. A series of combinations by varying the composition of the two excipients were prepared and their effect on tablet property such as disintegration time, hardness and friability were analyzed using statistical design software. An optimized formulation generated by the software, was evaluated for tablet properties and drug-excipient compatibility study was carried out by FT-IR analysis and DSC thermogram analysis. A SEM image of the granules was recorded to study surface morphology. A 70:50 combination of MCC and starch was found to be the best optimized formulation for an immediate release tablet without affecting its hardness and stability. Disintegration time increased with increasing amount of starch, but decreased with increasing amount of MCC. The low prediction error observed during evaluation of the final formulation indicated the high prognostic capability of the RSM methodology. FT-IR and DSC study confirmed the compatibility of the drug with excipients

Fabrication and Evaluation of Physically Crosslinked Stimuli Sensitive Polymeric Blend of Pva-Gelatin as Drug Delivery System by Freeze Thaw Cycles: Crosslinked Stimuli Sensitive Polymeric Blend by Freeze Thaw Cycles

Vacuum dried Metronidazole hydrochloride (MTZ) loaded Crosslinked polymeric blend of Poly (vinyl) alcohol (PVA) and Gelatin (GE) in different ratios by 30 freeze/thaw cycles (FTC) tested for stimuli sensitivity and crosslinking at various pH, temperature, ionic concentration and oscillatory test along with dye absorption test showed maximum swelling in alkaline pH and decreased swelling with increased ionic concentration. Digital scanning calorimetry (DSC) thermo grams of the blank crosslinked sample showed a sharp endothermic peak at 160.57 0C and MTZ loaded samples showed two sharp endothermic peaks at 159.95 0C and 324.74 0C indicating the entrapment of drug in the polymeric network. Scanning electron microscopy (SEM) showed the rough polymeric texture. Fourier Transformation Infrared Spectroscopy (FTIR) confirmed the presence of new peaks in the cross-linked and drug-loaded sample. In-vitro drug release studies showed 98.253% ± 0.363 and 92.248% ± 0.244 releases in the first 6 hours. Biodegradability and bactericidal studies of the blank film indicated that the crosslinked sample is biodegradable and does not inhibit any microbial growth