Abstract
In the present study, ribociclib-loaded nanosponges (RCNs) composed of ethylcellulose and polyvinyl alcohol were developed using an emulsion-solvent evaporation method. Preliminary evaluations of the developed RCNs (RCN1 to RCN7) were performed in terms of size, polydispersity index (PDI), zeta potential (ZP), entrapment efficiency (EE), and drug loading (DL), which allowed us to select the optimized formulation. RCN3 was selected as the optimized carrier system with particle size ([Formula: see text]), PDI ([Formula: see text]), zeta potential ([Formula: see text]), EE ([Formula: see text]), and DL ([Formula: see text]). Further, the optimized nanosponges (RCN3) were subjected to FTIR, XRD, DSC, and SEM studies, and results confirmed the proper encapsulation of the drug within the porous polymeric matrix. In vitro drug release studies showed that the drug release was significantly enhanced with a maximum drug release through RCN3 formulation ([Formula: see text]) and followed the Higuchi model. Moreover, the RCN3 system showed greater cytotoxicity than free ribociclib (RC) against MDA-MB-231 and MCF-7 breast cancer cell lines. The percentage of apoptosis induced by RCN3 was found significantly higher than that of free RC ([Formula: see text]). Overall, ribociclib-loaded ethylcellulose nanosponges could be a potential nanocarrier to enhance the effectiveness of ribociclib in breast cancer treatment.
Highlights
Breast cancer (BC) is considered one of the most common and fatal cancer types detected in women globally [1–4]
Based on the results of particle size analysis, RCN3 was selected as the optimized formulation with optimized particle size, polydispersity index (PDI), and zeta potential (ZP) values of 363:5 ± 4:8 nm, 0:292 ± 0:012, and −18:5 ± 0:05 mV, respectively
From the results of zeta potential, it was suggested that the negative surface charge of the formulations was probably due to ethylcellulose, which further assisted in particle-particle repulsion [38, 39]
Summary
Breast cancer (BC) is considered one of the most common and fatal cancer types detected in women globally [1–4]. The clinically established ribociclib (RC), abemaciclib, and palbociclib, classified as secondgeneration CDK4/6-targeting inhibitors, have showed potential anticancer activities in patients diagnosed with (HER-2) BC [15, 16]. Amongst these inhibitors, RC has been proven as a vastly discerning CDK4/6-selective inhibitor [17], and it acts by merging with the ATP-binding pockets of CDK4/6 [18–21]. It has been noticed that RC as a single moiety or in combination has exhibited potential anticancer activity and has been found to be efficient to overcome the issues associated with resistance, established through clinical or preclinical studies. Anticancer activity of RC and RC-loaded ethylcellulose-based nanosponges was determined in MDA-MB-231 and MCF-7 breast cancer cells by examining cell viability and apoptosis
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