Design and In Vitro Evaluation of Eudragit-Based Extended Release Diltiazem Microspheres for Once- and Twice-Daily Administration: The Effect of Coating on Drug Release Behavior
Journal Title: Turkish Journal of Pharmaceutical Sciences - Year 2019, Vol 16, Issue 3
Abstract
Objectives: The aim of this investigation was to develop an extended release formulation of diltiazem hydrochloride (DL) for once- and twice-daily administration, based on Eudragit (Eud) RL and RS microspheres using emulsion solvent evaporation. Materials and Methods: Formulations with different drug–polymer concentrations were produced and characterized in terms of yield, encapsulation efficiency (EE), particle size, and surface morphology. The drug release and thermal behavior of the microspheres were also investigated. Selected microspheres were then coated with Eud RS by continuous solvent evaporation, in order to modify the microspheres’ properties and burst release. Results: According to the results, the EE was in the range of 56%-93% for uncoated microspheres. The mean particle size of microspheres was different from 470 to above 1000 μm, based on various formulation variables. No difference was observed between the mean size of particles prepared with Eud RL and Eud RS. Microspheres showed sustained release behavior, which was affected by the drug:polymer ratio as well as particle size. Coating the microspheres not only improved the EE values (82%-92%) but also reduced the mean dissolution rate as well as the burst release. Conclusion: Microspheres prepared with DL:Eud RL ratios of 1:3 and 1:4 showed release profiles in accordance with the USP criteria for a DL extended release product for dosing every 12 and 24 h, respectively.
Authors and Affiliations
Noushin BOLOURCHIAN, Maryam BAHJAT
Keywords
Related Articles
- EP ID EP604422
- DOI 10.4274/tjps.galenos.2018.24861
- Views 170
- Downloads 0
Assessment of Vitronectin, Soluble Epithelial-Cadherin and TGF-β1 as a Serum Biomarker with Predictive Value for Endometrial and Ovarian Cancers
Objectives: Extracellular matrix components, including vitronectin (VN), soluble epithelial-cadherin (sE-cadherin) and transforming growth factor-beta 1 (TGF-β1), play a key role in the invasion and metastasis of cancer....
Antiplasmodial Activity of the n-Hexane Extract from Pleurotus ostreatus (Jacq. ex. Fr) P. Kumm.
Objectives: Several mushrooms species have been reported to be nematophagous and antiprotozoan. This study reported the antiplasmodial and cytotoxic properties of the n-hexane extract from the edible mushroom Pleurotus o...
Synthesis and Evaluation of Vanillin Derivatives as Antimicrobial Agents
Objectives: The present work involves the synthesis of novel acetyl vanillin derivatives and evaluation for their anti-microbial potential against Escherichia coli. Materials and Methods: The titled compounds were prep...
Comparative Anatomical Studies on Three Endemic Ononis L. (Leguminosae) Species Growing in Turkey
Objectives: The leaf and stem anatomical characteristics of three endemic Ononis L. (Leguminosae) species were studied for the first time for the evaluated in terms of systematic of similarities and differences in these...
An In Vitro Study on the Cytotoxicity and Genotoxicity of Silver Sulfide Quantum Dots Coated with Meso-2,3-dimercaptosuccinic Acid
Objectives: Silver sulfide (Ag2S) quantum dots (QDs) are highly promising nanomaterials in bioimaging systems due to their high activities for both imaging and drug/gene delivery. There is insufficient research on the to...