Enhanced anticancer activity of drug nanoparticles formulated with β-cyclodextrin

Abstract

Camptothecin (CPT) is a potent chemotherapeutic agent that shows a broad spectrum of anticancer activities. However, it is clinically inactive because of poor aqueous solubility, rapid aqueous hydrolysis, and unexpected side effects. Three strategies have extensively been adopted to improve its dissolution rate including reduction of drug particle size to a nanoscale, use of an amorphous state, and the formation of inclusion compounds. In our study, we combined these three strategies together by constructing CPT nanoparticles by creating an inclusion complex with β-cyclodextrin (BCD). This new CPT formulation showed a rod-like structure of nanoscaled size and with semiamorphous or amorphous CPT. These BCD-CPT nanoparticles showed improved dissolution rate, stability, dispersion, and cellular uptake. When tested on cancer cells, BCD-CPT nanoparticles showed a much higher anticancer activity (IC50=14-28 μmol/l) in comparison with free CPT (IC50>500 μmol/l) and CPT nanocrystals (IC50>200 μmol/l). In addition, BCD-CPT nanoparticles can be physically mixed with CPT nanocrystals, leading to CPT formulations with tailored drug-release profiles to achieve customized therapeutics and flexible treatments in clinics.

The polyphenol/saponin-rich Rhus tripartita extract has an apoptotic effect on THP-1 cells through the PI3K/AKT/mTOR signaling pathway

“…2 b). Moreover, regarding the proportion of apoptotic cells for total plant extract treatment, there was no statistically significant difference ( p -value ≥0.05) with mean value (87.08 ± 0.46%) obtained from cells treated with the camptothecin (2 μM) (CTRL(+), an alkaloid with known antineoplastic and antitumor activity [ 43 ] (Fig. 2 b).…”

The polyphenol/saponin-rich Rhus tripartita extract has an apoptotic effect on THP-1 cells through the PI3K/AKT/mTOR signaling pathway

“…2b). Moreover, regarding the proportion of apoptotic cells for total plant extract treatment, there was no statistically signi cant difference (p-value ≥ 0.05) with mean value (87.08 ± 0.46%) obtained from cells treated with the camptothecin (2 µM) (CTRL(+), an alkaloid with known antineoplastic and antitumor activity [43] (Fig. 2b).…”

Biomedical applications of cerium vanadate nanoparticles: a review

“…21 Camptothecin (CPT) was combined with b-cyclodextrin (BCD) to enhance its solubility, stability, dispersion, and cellular absorption, according to a study by Zhan et al Anticancer activity was significantly enhanced in the BCD-CPT NPs compared to that of free CPT and CPT nanocrystals. 95 In a separate study, Kumar et al found that the increased surface-volume ratio of catalase-active CeVO 4 NPs boosted the activity of nanozymes. Excellent peroxidasemimicking activity can be obtained from CeVO 4 NS due to its high stability and activity in a severe reaction environment.…”