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Ibrahim, BA, Hussein, NR, Omer, HK, Elhissi, A and Khan, I (2025) Enhancing Gliclazide Solubility Using Solid Dispersions with Carboxymethyl Chitosan and Polyvinylpyrrolidone K30 as Polymeric Carriers. Drug Development and Industrial Pharmacy. pp. 1-16. ISSN 0363-9045
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Abstract
Background Gliclazide (Glz) is a second-generation sulfonylurea antidiabetic drug, used to treat type II diabetes mellitus. Glz is a class II drug according to the biopharmaceutic classification system (BCS), indicating that it has high permeability and poor aqueous solubility. Objective This study aimed to improve the solubility of Glz via the solid dispersion method. Methods Solid dispersions of the drug were formulated using carboxymethyl chitosan (CMch) and polyvinyl pyrrolidone K30 (PVP K30) in varying drug to carrier ratios (1:1, 1:3, and 1:5 w/w) using kneading and solvent evaporation methods. The solubility of Glz solid dispersions was compared with the pure Glz and co-grounded mixtures of the drug. Results Both carriers exhibited a noticeable increment in solubility and dissolution rate compared to the drug alone. Glz: CMch (1:5 w/w ratio) formulation made by the kneading method exhibited an increased solubility by approximately nine folds (337.79 ± 4.22 µg/ml) as compared to Glz alone (38.74 ± 4.69 µg/ml). However, the greatest improvement in drug dissolution rate was observed in the dispersion made with 1:5 w/w drug to PVP K30 using the solvent evaporation method, and the percentage drug release reached 100% after 30 min. Solid dispersions characterization manifested the compatibility between the drug and carriers, with alteration in particle morphology, and reduction in drug crystallinity. Conclusion Overall, solid dispersion using CMch has shown to be an excellent approach for enhancing the solubility and dissolution of the class II drug Glz.
| Item Type: | Article |
|---|---|
| Uncontrolled Keywords: | 3206 Medical Biotechnology; 32 Biomedical and Clinical Sciences; 5.1 Pharmaceuticals; 1115 Pharmacology and Pharmaceutical Sciences; 3214 Pharmacology and pharmaceutical sciences |
| Subjects: | R Medicine > RC Internal medicine R Medicine > RS Pharmacy and materia medica |
| Divisions: | Pharmacy and Biomolecular Sciences |
| Publisher: | Taylor and Francis Group |
| Date of acceptance: | 11 May 2025 |
| Date of first compliant Open Access: | 29 May 2025 |
| Date Deposited: | 29 May 2025 10:21 |
| Last Modified: | 29 May 2025 10:30 |
| DOI or ID number: | 10.1080/03639045.2025.2506651 |
| URI: | https://researchonline.ljmu.ac.uk/id/eprint/26456 |
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