Preparation of high drug-loading celastrol nanosuspensions and their anti-breast cancer activities in vitro and in vivo

Abstract

Stability of CSL-NSps during storage. The CSL-NSps were kept at 4 °C and 25 °C, and the particle size and status of CSL-NSps were monitored at predetermined times. Stability of CSL-NSps in various physiological media and plasma. CSL-NSps were mixed with 1.8% NaCl, PBS (2×) and 10% glucose (1:1, v/v) or mixed with artificial gastric fluid, artificial intestinal fluid and rat plasma (1:4, v/v) and incubated at 37 °C 27,28. The particle size was measured at specific time intervals. Each experiment was performed three times. Lyophilization of CSL-NSps. One mL of CSL-NSps was mixed with 15 mg of lyoprotectant (glucose, sucrose, whey protein and albumin bovine V), placed in an EP tube, covered with lens paper frozen for 6 h at −20 °C and lyophilized for 24 h in a vacuum freeze dryer (ALPHR 2-4 LD plus, CHRIST, Germany) under −43 °C, 0.12 mbar. The freeze-dried powder was dispersed in 1 mL deionized water, and the particle size and PDI value were measured by a particle size analyzer (Zetasizer nano ZS, Malvern Instruments, UK).

Nanotechnology-Based Celastrol Formulations and Their Therapeutic Applications

“…Celastrol was stabilized in an amorphous form in the nanosuspension, hence enhancing its dissolution significantly to 69.2% in 48 h. Compared to intravenous injection of the anticancer drug paclitaxel, the oral and intravenous treatment with celastrol nanosuspension showed similar and higher tumor inhibition rates, respectively. Hence, the unique property of nanoformulations to enhance dissolution of poorly soluble drugs such as celastrol can be explored to enhance solubility and in turn the in vivo efficacy (Huang et al, 2020).…”

Microbial transglutaminase nanoflowers as an alternative nanomedicine for breast cancer theranostics

“…49 Moreover, NFs share the advantages of being a novel drug delivery system (NDDS), such as increased dissolution rate, elevated oral bioavailability, improved in vivo pharmacokinetics, passive targetability to solid tumors and inammatory sites due to the enhanced permeability and retention (EPR) effect. 48,50 Hopefully, this new approach in our present study of testing natural biological sources for breast cancer research will carefully explore the anti-cancer properties of enzyme-microbial transglutaminase. This study explored and assessed the enzymatic MTGase NFs properties as an anti-cancer drug to address the issues of chemotherapies applied.…”

Silk Particles as Carriers of Therapeutic Molecules for Cancer Treatment

“…Other plant-derived substances widely studied concerning cancer therapy include two terpenoids extracted from Tripterygium wilfordii-triptolide and celastrol, which both exhibit anti-cancer and anti-inflammation activities [108]. Similarly to curcumin, the clinical applications of these compounds are limited due to their low solubility in aqueous solutions [109].…”