Enhancing delivery and cytotoxicity of resveratrol through a dual nanoencapsulation approach

Abstract

Despite the known anticancer potential of resveratrol, its clinical applications are often hindered by physicochemical limitations such as poor solubility and stability. The encapsulation of resveratrol in formulations such as polymeric nanoparticles and liposomes has shown limited success. This study aimed to develop and optimize a novel drug carrier by co-encapsulating pristine resveratrol alongside cyclodextrin-resveratrol inclusion complexes in the lipophilic and hydrophilic compartments of liposomes, respectively by using a novel dual carrier approach. The particle size, polydispersity index and zeta potential of the final formulation were 131±1.30nm, 0.089±0.005 and -2.64±0.51mV, respectively. Compared to free resveratrol and conventional liposomal formulations with drug release profile of 40-60%, our novel nanoformulations showed complete (100%) drug release in 24h. The formulation was stable for 14days at 4°C. We also studied the in vitro cytotoxicity of resveratrol encapsulated liposomes in HT-29 colon cancer cell lines. The cytotoxicity profile of our liposomes was observed to be dose dependent and enhanced in comparison to free resveratrol (in DMSO). Our study demonstrates that co-encapsulation of pristine resveratrol along with its cyclodextrin complex in liposomal formulations is a plausible option for the enhanced delivery of the hydrophobic chemotherapeutic agent.

Blend Hydrogel Microspheres of Carboxymethyl Chitosan and Gelatin for the Controlled Release of 5-Fluorouracil

“…In the recent past, many polymeric, as well as non-polymeric, CR systems have been developed, to study their anticancer drug delivery characteristics [24,25,26]. In search of an effective biopolymeric CR device for 5-FU, to minimize its high plasma concentration-related toxic side effects, Chaturvadi et al [27] have developed blend microspheres of poly(3-hydroxy butyrate) and cellulose acetate phthalate, and investigated their CR characteristics.…”

Role of apoptosis-related miRNAs in resveratrol-induced breast cancer cell death

“…It is emerging as a promising anticancer agent because of its chemopreventive and pro-apoptotic properties. 8, 9, 10, 11 Resveratrol has been shown to have a crucial role in apoptosis induction in human breast cancer cells. 12, 13 Moreover, studies show that several members of the mitogen-activated protein kinase signaling pathway are involved in this activation 14 and the intrinsic mitochondrial pathway, via activation of caspase-9 along with other key mediators calcium and calpain, is the major pathway involved in resveratrol-induced apoptosis.…”

Recent Strategies in Resveratrol Delivery Systems

“…Studies of RSV release from RSV‐CD inclusion complex‐liposomes were carried out at pH 7.4 and 37 °C for 24 h. The cumulative release of RSV was almost complete for dual encapsulated liposomes (94 %) compared to its free form (44 %), due to the increased RSV aqueous solubility because of CD inclusion complex …”