Evaluation of anticancer activity of celastrol liposomes in prostate cancer cells

Abstract

Context Celastrol, a natural compound derived from the herb Tripterygium wilfordii, is known to have anticancer activity, but is not soluble in water. Objective Formation of celastrol liposomes, to avoid the use of toxic solubilizing agents. Materials and methods Two different formulations of pegylated celastrol liposomes were fabricated. Liposomal characteristics and serum stability were determined using dynamic light scattering. Drug entrapment efficacy and drug release were measured spectrophotometrically. Cellular internalization and anticancer activity was measured in prostate cancer cells. Results Liposomal celastrol displayed efficient serum stability, cellular internalization and anticancer activity, comparable to that of the free drug reconstituted in dimethyl sulfoxide. Discussion and conclusion Liposomal celastrol can decrease the viability of prostate cancer cells, while eliminating the need for toxic solubilizing agents.

Inhibition of telomerase activity and cell growth by free and nanoliposomal forms of punicalagin in human leukemia cell line K562

“…Similar anticancer activity had been reported in previous investigations with other liposomal natural plant products such as celastrol [25], epigallocatechin-3-gallate [24], gossypol [26], wagonin [27], berberin [28], curcumin [29] and tea polyphenol [30] in various cancer cell lines. Therefore, punicalagin and other effective plantderived agents in the free and encapsulated forms may be considered as promising strategy to develop new anticancer drugs.…”

“…Several hypotheses, including increased penetration of plant-derived compounds into cells and stability of encapsulated materials may explain the mechanism of enhanced anticancer efficacies of this nanoliposomal formulation [25][26][27][28][29][30]. Our data showed a significant and positive correlation between telomerase inhibition and induction of apoptosis.…”

Nanoencapsulation of natural triterpenoid celastrol for prostate cancer treatment

“…15,16 To date, only two studies have explored the effectiveness of nanoencapsulated CL in the treatment of prostate cancer. 14,17 In the first study, CL-loaded PEGylated liposomes displayed anticancer activity in VCaP cells, comparable to that of the free drug reconstituted in DMSO.…”

“…11,12 Furthermore, harmful solvents such as dimethyl sulfoxide (DMSO) need to be used to solubilize the hydrophobic CL, and this limits its clinical use. 13,14 In spite of this, to overcome these physicochemical and pharmacokinetic deficiencies, and to reduce the amount of the effective dose, the nanoencapsulation of CL can represent a useful strategy. 15,16 To date, only two studies have explored the effectiveness of nanoencapsulated CL in the treatment of prostate cancer.…”

Stealth, biocompatible monoolein-based lyotropic liquid crystalline nanoparticles for enhanced aloe-emodin delivery to breast cancer cells: in vitro and in vivo studies

“…After incubation, samples were centrifuged for 5 minutes at 3,000 rpm and supernatants were taken to quantify the hemoglobin (Hb) content spectrophotometrically at λ max =540 nm, against negative control (1 mL RBCs diluted with 1 mL normal saline). 1% Triton-X-treated RBCs were used as positive control (Ab positive control ) inducing 27 Samples were withdrawn at different time points and diluted in distilled water (1:50 v/v) and assessed for PDI and PS, using a Zetasizer (Nano ZS).…”