Sustained Release Solid Dispersions of Pentoxyfylline: Formulation and Optimization

Objective: The purpose of the study is to formulate and optimize sustained release solid dispersions of pentoxyfylline using a combination of eudragit polymers and ethyl cellulose. Methods: Solid dispersions were formulated by solvent evaporation method.Preliminary batches were formulated using various drug to polymer ratio; with eudragit S100 and L100 (1:1 to 1:5 ratio), and with ethyl cellulose(1:1 to 1:3 ratio) and evaluated for solubility analysis. Based on results of preliminary batches, Box Behnken design was further applied and three factors (X1- concentration of Eudragit S100, X2- concentration of Eudragit L100, X3- concentration of Ethyl Cellulose) were selected with three levels (+1, 0, -1). Multiple linear regression was applied to generate polynomial equations and statistical evaluation. Prepared solid dispersions were investigated for sustained release properties via in vitro dissolution studies. Fourier transform infrared spectroscopic analysis (FTIR), X-ray diffraction analysis (X-RD), Differential scanning calorimetry (DSC) studies were carried out to evaluate drug polymer interactions. Scanning Electron Microscopy (SEM) analysis of optimized solid dispersion was carried out to evaluate surface morphology of the particles. Results: Batch F5 showed maximum sustained release (65.46% in 24 h) characteristics out of all solid dispersions. DSC studies indicated drug integrity when mixed with the polymeric carriers. FTIR and X-RD studies also ruled out any drug polymer interaction. A change in crystalline habit was observed in solid dispersion particles (F5 batch) as seen in SEM micrographs. Polynomial mathematical model generated using multiple regression analysis was found to be statistically significant (p<0.05). Conclusion: Release retarding effect was found to be dependent on polymer concentration. Therefore, an optimized combination may lead to better sustaining effect

QbD-based optimization of guar gum suspension medium for optimum pourability and sedimentation volume

A stable, adequately pourable guar-gum suspension medium has been developed by using the QbD approach. For this, the QTPP is defined followed by its subset CMA (guar gum and sucrose concentration). The CQA are viscosity and sedimentation volume. The target range for viscosity is 99 - 101.3 cps and sedimentation volume 0.98-1 for preparing the optimized suspension. To achieve this optimization, the central composite design has been opted which would fit well to the quadratic model. The quadratic equations and the ANOVA results are validated. The analysis phase of graphical and numerical optimization suggested that 0.1g of guar-gum and 20g of sucrose can achieve an optimized viscosity and sedimentation volume suspension. This contour plots and surface plots are utilized to check the combined interaction of the variables. The checkpoint analysis reveal appropriate percentage variance, which signify the predictive ability of the developed model and validated the design for an optimum suspension. Further, scale-up and stability studies will verify the projected promising results which may be scaled up for its applications in pharmaceutical, food and chemical industries

UV Method Development and Validation of Ellagic Acid for its Rapid Quantitative Estimation

Development and validation of a simple UV- Spectroscopy method was done for the quantitative analysis of Ellagic Acid (EA). The stock solution of 50μg/ml was prepared and scanned, for which absorption maxima was found to be 277nm. Further dilutions to different concentrations (1-5μg/ml) were prepared and analyzed at 277nm. The method so developed was validated as per ICH guidelines for: linearity, robustness, precision, accuracy, limit of detection and quantification. The Lambert- Beer’s law is followed in the range (1-5μg/ml) with correlation coefficient value 0.9994. It was observed that the method is precise and accurate for EA analysis with good recovery percent of 94.47% to 106.83%. The method developed was further employed for determining the entrapment efficiency of ellagic acid and its release from its nanoparticle dosage form. The method may be utilized for determining the concentration of EA when present as formulation and in combination with other drugs

QbD-based optimization of guar gum suspension medium for optimum pourability and sedimentation volume

223-230A stable, adequately pourable guar-gum suspension medium has been developed by using the QbD approach. For this, the QTPP is defined followed by its subset CMA (guar gum and sucrose concentration). The CQA are viscosity and sedimentation volume. The target range for viscosity is 99 - 101.3 cps and sedimentation volume 0.98-1 for preparing the optimized suspension. To achieve this optimization, the central composite design has been opted which would fit well to the quadratic model. The quadratic equations and the ANOVA results are validated. The analysis phase of graphical and numerical optimization suggested that 0.1g of guar-gum and 20g of sucrose can achieve an optimized viscosity and sedimentation volume suspension. This contour plots and surface plots are utilized to check the combined interaction of the variables. The checkpoint analysis reveal appropriate percentage variance, which signify the predictive ability of the developed model and validated the design for an optimum suspension. Further, scale-up and stability studies will verify the projected promising results which may be scaled up for its applications in pharmaceutical, food and chemical industries

Anti-inflammatory, Analgesic and Antiulcer properties of Porphyra vietnamensis

Objectives: Aim of the present work was to investigate the anti-inflammatory, analgesic and antiulcer effects of red seaweed Porphyra vietnamensis (P. vietnamenis). Materials and Methods: Aqueous (POR) and alcoholic (PE) fractions were successfully isolated from P. vietnamenis. Further biological investigations were performed using a classic test of paw edema induced by carrageenan, writhing induced by acetic acid, hot plate method and naproxen induced gastro-duodenal ulcer. Results: Among the fractions POR showed better activity.  POR and PE significantly (p < 0.05) reduced carrageenan induced paw edema in a dose dependent manner. In the writhing test POR significantly (p < 0.05) reduced abdominal writhes than PE.  In hot plate method POR showed better analgesic activity than PE. POR showed comparable ulcers reducing potential (

Significance of Algal Polymer in Designing Amphotericin B Nanoparticles

Development of oral amphotericin B (AmB) loaded nanoparticles (NPs) demands a novel technique which reduces its toxicity and other associated problems. Packing of AmB in between two oppositely charged ions by polyelectrolyte complexation technique proved to be a successful strategy. We have developed a novel carrier system in form of polyelectrolyte complex of AmB by using chitosan (CS) and porphyran (POR) as two oppositely charged polymers with TPP as a crosslinking agent. Initially POR was isolated from Porphyra vietnamensis followed by the fact that its alkali induced safe reduction in molecular weight was achieved. Formulation was optimized using three-factor three-level (33) central composite design. High concentration of POR in NPs was confirmed by sulfated polysaccharide (SP) assay. Degradation and dissolution studies suggested the stability of NPs over wide pH range. Hemolytic toxicity data suggested the safety of prepared formulation. In vivo and in vitro antifungal activity demonstrated the high antifungal potential of optimized formulation when compared with standard drug and marketed formulations. Throughout the study TPP addition did not cause any significant changes. Therefore, these experimental oral NPs may represent an interesting carrier system for the delivery of AmB