ArticlePloS one2024
Solid dispersion systems for enhanced dissolution of poorly water-soluble candesartan cilexetil: In vitro evaluation and simulated pharmacokinetics studies.
Article in PloS one, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.
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Who cites it
7 citing papers in PubMed.
- Enhancing Doxorubicin Bioavailability via Dissolving Microneedles: Roles of Drug Loading and Administration Force.AAPS PharmSciTech · 2026Article
- Design and evaluation of a novel expandable gastroretentive film for sustained Metoprolol release.PloS one · 2026Article
- Design, Molecular Docking,Current pharmaceutical design · 2026Article
- Combined Experimental and Computational Approaches for Ternary Solid Dispersions to Enhance the Oral Bioavailability of Penfluridol.Pharmaceutics · 2025Article
- Surfactant-Enriched Cross-Linked Scaffold as an Environmental and Manufacturing Feasible Approach to Boost Dissolution of Lipophilic Drugs.Pharmaceutics · 2025Article
- Industrial Sustainable Decrystallizing Formulation to Enhance Dissolution of Candesartan Cilexetil: Overcoming Limitations of Traditional Solid Dispersion Approaches.Pharmaceutics · 2025Article
- Development of Candesartan Cilexetil-sodium Carbonate Anhydrate-mesoporous Silica Solid Dispersion in Polymer-free System.Pharmaceutical research · 2025Article
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3 authors.
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Abstract
backgroundCandesartan cilexetil (CC) is a selective angiotensin II receptor antagonist widely used to treat hypertension. CC is a substrate of P-glycoprotein (P-gp), causing its efflux to the intestinal lumen. It is also practically insoluble in water and has low oral bioavailability (14%). Thus, the current study aims to improve the in vitro dissolution of CC by developing solid dispersion systems (SDSs) and corroborating the in vitro results using a simulated pharmacokinetics study.
methodsThe SDSs were prepared using polyvinyl pyrrolidone (PVP) as a water-soluble polymer, Eudragit E100 (EE100) as a pH-dependent soluble carrier, and a combination of these two polymers. The saturation solubility and the dissolution rate studies of the prepared systems in three dissolution media were performed. The optimized system SE-EE5 was selected for further investigations, including DSC, XRD, FTIR, FESEM, DLS, TSEM, IVIVC convolution study, and stability studies.
resultsThe solubility of CC significantly increased by a factor of 27,037.344 when formulated as a solid dispersion matrix using EE100 at a ratio of 1:5 (w/w) drug to polymer (SE-EE5 SD), compared to the solubility of the pure drug. The mechanism of solubility and dissolution rate enhancement of CC by the optimized SDS was found to be via the conversion of the crystalline CC into the amorphous form as well as nanoparticles formation upon dissolution at a pH below 5. The instrumental analysis tests showed good compatibility between CC and EE100 and there was no chemical interaction between the drug and the polymer. Moreover, the stability tests confirmed that the optimized system was stable after three months of storage at 25°C.
conclusionThe utilization of the solid dispersion technique employing EE 100 polymer as a matrix demonstrates significant success in enhancing the solubility, dissolution, and subsequently, the bioavailability of water-insoluble drugs like CC.
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