Objective: The aim of this study is to prepare oral controlled release (CR) of mucoadhesive alginate microbeads encapsulating fluvastatin by gastroretention technology. Methods: The mucoadhesive microbeads containing fluvastatin were produced using emulsification internal gelation technique. The effect of different variables such as sodium alginate concentration and its combination with other hydrophilic polymers, and the effect of various curing agents on particle size, entrapment efficiency, and in vitro studies were evaluated. Results: There was no marked change in drug entrapment efficiency, and dissolution studies occur during the stability studies of fluvastatin. The in vitro results give data that improvement in the CR of the drug from microbeads compared with marketed tablet. Hence, in this regard, to minimize the frequency of drug administration to reduce side effects. The optimum condition for the preparation of stable alginate beads and produce CR manner was occurred at a higher concentration of combined polymer mixture in equal ratios, i.e., 3% w/v. Infrared spectroscopic study (Fourier transform infrared) confirmed the no incompatibility between drug and other excipients. X-ray diffraction study and differential scanning calorimetry were provided evidence that successful entrapment of drug into the alginates microbeads and drug converted into amorphous nature. The efficiency of mucoadhesion strength of microbeads was determined by wash-off study. Conclusion: The kinetic modeling of the release data indicates drug release from the microbeads follow anomalous transport mechanism and super Case-II transport mechanism. Drug release is a function of pH dependent and controlled drug release depends on type and concentration of polymer blend and curing agents. The release kinetics of drug from the alginate beads followed zero order.
Objective: The aim of the current study is to prepare and lovastatin-loaded alginate microbeads were prepared using emulsification gelation internal method by the use of different cross-linking agents, polymer effect in different concentrations on drug release and its combination with hydrophilic polymers on drug release. Methods: The effect of sodium alginate concentration and its combination with other hydrophilic polymers on particle size and shape, scanning electron microscopy (SEM) studies, entrapment efficiency, Fourier transform infrared (FTIR) analysis (FTIR), differential scanning calorimetry (DSC) studies, and X-ray diffraction (XRD) studies conducted to determine compatibility of drug and used excipients and in vitro drug release was studied. The efficiency of mucoadhesion strength of microbeads is determined by wash-off study. Results: The optimum condition for preparation alginate beads and produces sustained release manner was occurred at 3% polymer mixture. Infrared spectroscopic study confirmed the presence of compatibility between drug-polymer additives, good drug entrapment, and SEM studies prove microbeads were in spherical and rough particles. XRD and DSC were used to confirm successful entrapment of drugs into the alginates microbeads. The in vitro release profile could be altered notably by changing formulation parameters to give a sustained release of drug from the microbeads. Conclusion: The kinetic modeling of the release data indicate that drug release from the microbeads follow anomalous transport mechanism and super Case-II transport mechanism and drug release is controlled by both swelling and relaxation of the polymer chains. It was found to be drug release is pH dependent. This will help in overcoming the drawbacks of lovastatin with a short half-life, improves the bioavailability. The release kinetics of drug from the alginate beads followed zero order.
Lornoxicam is a non-steroidal anti-inflammatory drug, indicated in the treatment of osteoarthritis and rheumatoid arthritis. Lornoxicam is a poor water-soluble drug and hence possesses dissolution limited bioavailability. The aim of the current research work was to develop and characterize orodispersible films of Lornoxicam to enhance its bioavailability by employing Quality-by-Design (QbD) approach. Solvent casting method was used to formulate the Lornoxicam mouth dissolving films. Three formulation factors viz. amount of polymer, amount of PEG 400 and type of polymer were varied at different levels. The responses selected were disintegration time and percent drug dissolved after 5mins. Under the response surface methodology, historical data design was employed to perform the statistical analysis using Design Expert software. The developed films were found to have good elasticity, folding endurance and favorable tensile strength. The disintegration time was found to be 9 to 17 seconds and drug dissolved after 5 minutes was 49 to 95%. The statistical analysis of the results by ANOVA elucidated that there was a significant effect of all the formulation factors on the selected responses (p
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