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Candesartan Cilexetil Formulations in Mesoporous Silica: Preparation, Enhanced Dissolution In Vitro, and Oral
Huijian Guan1, Miao Wang2, Shaowen Yu2
1School of Chemistry, South China Normal University, Key Laboratory of Process Control and Quality Evaluation of Chiral Drugs, Guangdong Provincial Drug Administration, Guangzhou Key Laboratory of Biomedical Analytical Chemistry, Guangzhou 510006, China.
Journal of Pharmaceutical Sciences
|August 2, 2024
Summary
This study enhanced candesartan cilexetil (CC) bioavailability using mesoporous silica carriers. Solid dispersions significantly improved CC dissolution and absorption in rats.
Area of Science:
- Materials Science
- Pharmaceutical Sciences
- Drug Delivery
Background:
- Candesartan cilexetil (CC) is an effective antihypertensive drug.
- Poor solubility and low bioavailability limit CC's therapeutic potential.
Purpose of the Study:
- To develop novel solid dispersions of CC using mesoporous silica carriers.
- To enhance the dissolution and bioavailability of CC.
Main Methods:
- Solid dispersions were prepared using solvent immersion with mesoporous silica (Syloid XDP 3150, Syloid AL-1 FP) and amino-modified silica carriers.
- Characterization involved XRD, FTIR, DSC, SEM, and ssNMR.
- In vitro dissolution and in vivo pharmacokinetic studies in rats were conducted.
Main Results:
- CC transitioned from crystalline to amorphous state within silica carriers.
- The CC-XDP 3150 solid dispersion showed 1.88-fold greater cumulative CC release compared to pure CC.
- Relative bioavailability increased to 326% for CC-XDP 3150 and 238% for CC-N-XDP 3150 in rats.
Conclusions:
- Mesoporous silica carriers effectively enhance CC dissolution and bioavailability.
- Carrier properties like pore size and surface characteristics significantly impact drug loading, dissolution, and absorption.
- This research offers valuable insights for developing mesoporous silica-based delivery systems for poorly water-soluble drugs.
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