Investigation reveals improved solubility of camptothecin in liposomes, suggesting enhanced drug delivery for anticancer therapy.
Camptothecin (CPT) is a potent topoisomerase I inhibitor with promising anticancer potential. However, its poor solubility and stability present major obstacles in pharmaceutical formulations. Rutin, a plant-derived quercetin glycoside, also exhibits anticancer activity but suffers from limited solubility. This study explores a novel combination of CPT and Rutin in a liposomal drug delivery system. To enhance CPT solubility and encapsulation, hydroxypropyl-β-cyclodextrin (HPβCD) complexation was employed. High-performance liquid chromatography (HPLC) with UV detection was used for analysis. The CPT-HPβCD complex was prepared via different methods and characterized by Differential Scanning Calorimetry (DSC), Fourier Transform Infrared (FTIR) Spectroscopy, and Nuclear Magnetic Resonance (NMR). Liposomes loaded with Rutin and CPT-HPβCD were formulated and evaluated for size, charge, encapsulation efficiency, and in vitro release. Results showed that the solubility of CPT was significantly increased from 1.09µM to a range of (1.68-8.5) µM using different concentrations of HPβCD. Characterization proved the formation of the complex and the kneading method of preparation was found to be superior to other methods like solvent evaporation with an encapsulation efficiency of 64.6 ± 2.5%. The prepared Liposomes showed particle size around 20 nm with negative charge and 60 % cumulative release of rutin from the liposomes was achieved and CPT up to 60% compared to 10 % from the formula 1 (without complexation) with controlled release pattern.
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Ahmed et al. (2025) studied this question.
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