Synthesis and Characterization of Surface‐Hydrophobic Ion‐Exchange Microspheres and the Effect of Coating on Drug Release Rate

Because Eplerenone (EPL) is a Biopharmaceutical Classification System (BCS) class-II drug and is prone to extensive liver degradation, it suffers from poor bioavailability after oral administration. This work aimed to prepare liquisolids loaded with EPL-nanoemulsions (EPL-NEs) that have a higher drug release rate and improved bioavailability by the oral route. Based on solubility studies, mixtures of Triacetin (oil) and Kolliphor EL/PEG 400 surfactant/co-surfactant (Smix) in different ratios were used to prepare EPL-NE systems, which were characterized and optimized for droplet size, zeta potential, polydispersity index (PDI), and drug content. Systems were then loaded onto liquisolid formulations and fully evaluated. A liquisolid formulation with better drug release and tableting properties was selected and compared to EPL-NEs and conventional EPL oral tablets in solid-state characterization studies and bioavailability studies in rabbits. Only five NEs prepared at 1:3, 1:2, and 3:1 Smix met the specified optimization criteria. The drug release rate from liquisolids was significantly increased (90% within 45 minutes). EPL-NE also showed significantly improved drug release but with a sustained pattern for four hours. Liquisolid bioavailability reached 2.1 and 1.2 relative to conventional tablets and EPL-NE. This suggests that the EPL-NE liquisolid is a promising oral delivery system with a higher drug release rate, enhanced absorption, decreased liver degradation, and improved bioavailability.

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Application of a Binary Polymer System in Drug Release Rate Modulation. 1. Characterization of Release Mechanism

Journal of Pharmaceutical Sciences ◽

10.1021/js960302s ◽

1997 ◽

Vol 86 (3) ◽

pp. 316-322 ◽

Cited By ~ 74

Author(s):

Hyunjo Kim ◽

Reza Fassihi

Keyword(s):

Drug Release ◽

Release Rate ◽

Polymer System ◽

Release Mechanism ◽

Drug Release Rate ◽

Rate Modulation ◽

Binary Polymer

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Synthesis and characterization of hydroxyapatite-alginate nanostructured composites for the controlled drug release

Materials Chemistry and Physics ◽

10.1016/j.matchemphys.2018.06.071 ◽

2018 ◽

Vol 217 ◽

pp. 228-234 ◽

Cited By ~ 11

Author(s):

Leonid F. Sukhodub ◽

Liudmyla B. Sukhodub ◽

Olena Litsis ◽

Yuriy Prylutskyy

Keyword(s):

Drug Release ◽

Controlled Drug Release ◽

Synthesis And Characterization ◽

Nanostructured Composites

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Microorganism-based monodisperse microcapsules: encapsulation of the fungicide tebuconazole and its controlled release properties

RSC Advances ◽

10.1039/c5ra01629k ◽

2015 ◽

Vol 5 (32) ◽

pp. 25164-25170 ◽

Cited By ~ 6

Author(s):

Bo Zhang ◽

Teng Zhang ◽

Quanxi Wang ◽

Tianrui Ren

Keyword(s):

Controlled Release ◽

Powdery Mildew ◽

Drug Release ◽

Release Rate ◽

Drug Release Rate ◽

Burst Effect ◽

Initial Burst ◽

Release System ◽

Controlled Release System ◽

Monodisperse Microcapsules

A controlled release system was prepared, it based on UF modified PCC cells in which TEB are loaded into cells. It can control the drug release rate, depress the initial “burst effect”, and was efficacious in controlling wheat powdery mildew.

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