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Assessing the Impact of Mesoporous, Co-Amorphous, and Polymer-Based Systems on Cefdinir's Dissolution and Stability
Raghad Al Nuss1, Mohamad Anas Al Tahan2, Hind El-Zein3
1Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmacy, Arab International University, Daraa, Syria.
Formulating poorly soluble drugs like cefdinir using amorphisation strategies significantly enhances dissolution and oral bioavailability. Mesoporous silica dispersions offer superior long-term stability for Biopharmaceutics Classification System Class IV compounds.
Area of Science:
- Pharmaceutical Sciences
- Drug Delivery
- Materials Science
Background:
- Biopharmaceutics Classification System (BCS) Class IV drugs exhibit poor solubility and permeability, limiting oral bioavailability.
- Enhancing drug dissolution is crucial for improving bioavailability and therapeutic efficacy of poorly soluble compounds.
- Amorphisation strategies offer potential solutions for overcoming solubility challenges in drug formulation.
Purpose of the Study:
- To formulate cefdinir, a BCS Class IV drug, using three amorphisation strategies: solid dispersions, mesoporous silica dispersions, and co-amorphous systems.
- To evaluate the impact of these formulations on drug stability and dissolution profiles.
- To assess the long-term physical stability of the amorphous systems under various storage conditions.
Main Methods:
- Formulation of cefdinir using spray drying and solvent immersion techniques.
- Characterization of amorphous systems using differential scanning calorimetry (DSC), polarized light microscopy (PLM), and powder X-ray diffraction (PXRD).
- Dissolution studies and physical stability assessments under different storage conditions (temperature and humidity).
Main Results:
- All amorphised formulations demonstrated significantly enhanced cefdinir release compared to crystalline cefdinir.
- Solid dispersion and co-amorphous systems showed the greatest improvement in dissolution rates and maintained supersaturation.
- Mesoporous silica dispersions exhibited superior long-term stability, retaining >95% drug content and amorphous structure for 6 months across tested conditions.
Conclusions:
- Amorphisation strategies effectively enhance dissolution and bioavailability of BCS Class IV drugs.
- Mesoporous silica dispersions provide excellent physical stability for amorphous drugs due to pore confinement.
- Balancing dissolution enhancement with solid-state stability is key for rational formulation design of poorly soluble drugs.
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