Microencapsulation of ibuprofen and Eudragit (R) RS 100 by the emulsion solvent diffusion technique
ABSTRACT The emulsion solvent diffusion was employed to prepare modified release microspheres of ibuprofen. The technique was optimised for the following processing variables: the absence/presence of baffles in the reaction vessel, agitation rate and drying time. Thereafter, the influence of various formulation factors on the microencapsulation efficiency, in vitro drug release and micromeritic properties was examined. The variables included the methacrylic polymer, Eudragit(R) RS 100, ibuprofen content and the volume of ethanol used during microencapsulation. The results obtained were then interpreted on a triangular phase diagram to map the region of microencapsulation, as well as those formulations that yielded suitable modified release ibuprofen microspheres.
SourceAvailable from: Khaled Al-Tahami[Show abstract] [Hide abstract]
ABSTRACT: Objective: Ketoprofen is a nonsteroidal anti-inflammatory drug which could benefit if fabricated in a sustained delivery system. This work aims to develop the sustained release delivery system for ketoprofen using natural polymers. Methods: Alginate microspheres were prepared employing crosslinking method employing calcium chloride. The formation and compatibility of microspheres was confirmed by FT-IR. The formed microspheres were evaluated for percentage yield, drug content, drug loading, and encapsulation efficiency. In vitro release studies were carried out in phosphate buffer (pH 7.4). Results: FT-IR spectra exhibited the successful compatible encapsulation of ketoprofen in alginate microsphers. The formed microspheres exhibited good drug loading and encapsulation efficiency. The drug release was sustained over a period of 8 hours. There was a better release profile in phosphate buffer in formulations containing 3:1 polymer to drug ratio. Conclusion: It was feasible to prepare alginate-based microspheres capable of sustaining ketoprofen release over an extended period of time.
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ABSTRACT: Aim: The aim of this research is to prepare and evaluate alginate microspheres of prolonged delivery of a model drug, Risperidone. Methods: Alginate microspheres containing Risperidone were prepared employing cross-linking method by calcium chloride. The formed microspheres were evaluated for percentage yield, drug content, drug loading, and encapsulation efficiency. In vitro release studies were carried out in phosphate buffer (pH 7.4). Results: The formed microspheres exhibited good drug loading and encapsulation efficiency. The drug release was sustained over a period of 8 hours. Conclusions: The fabricated Risperidone microspheres showed extended drug release, which could improve the therapeutic agent bioavailability and increase patient compliance. The delivery system developed can potentially serve for the delivery of many therapeutic agents.
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ABSTRACT: Polymeric microspheres containing aceclofenac were prepared by single emulsion (oil-in-water) solvent evaporation method using response surface methodology (RSM). Microspheres were prepared by changing formulation variables such as the amount of Eudragit® RS100 and the amount of polyvinyl alcohol (PVA) by statistical experimental design in order to enhance the encapsulation efficiency (E.E.) of the microspheres. The resultant microspheres were evaluated for their size, morphology, E.E., and in vitro drug release. The amount of Eudragit® RS100 and the amount of PVA were found to be significant factors respectively for determining the E.E. of the microspheres. A linear mathematical model equation fitted to the data was used to predict the E.E. in the optimal region. Optimized formulation of microspheres was prepared using optimal process variables setting in order to evaluate the optimization capability of the models generated according to IV-optimal design. The microspheres showed high E.E. (74.14±0.015% to 85.34±0.011%) and suitably sustained drug release (minimum; 40% to 60%; maximum) over a period of 12h. The optimized microspheres formulation showed E.E. of 84.87±0.005 with small error value (1.39). The low magnitudes of error and the significant value of R(2) in the present investigation prove the high prognostic ability of the design. The absence of interactions between drug and polymers was confirmed by Fourier transform infrared (FTIR) spectroscopy. Differential scanning calorimetry (DSC) and X-ray powder diffractometry (XRPD) revealed the dispersion of drug within microspheres formulation. The microspheres were found to be discrete, spherical with smooth surface. The results demonstrate that these microspheres could be promising delivery system to sustain the drug release and improve the E.E. thus prolong drug action and achieve the highest healing effect with minimal gastrointestinal side effects. Copyright © 2014 Elsevier B.V. All rights reserved.Materials Science and Engineering C 03/2015; 48:197-204. DOI:10.1016/j.msec.2014.12.008 · 2.74 Impact Factor