Erlotinib-Loaded Dendrimer Nanocomposites as a Targeted Lung Cancer Chemotherapy

by Selleckchem | Jun 28 2023

Lung cancer is the main cause of cancer-related mortality globally. Erlotinib is a tyrosine kinase inhibitor, affecting both cancerous cell proliferation and survival. The emergence of oncological nanotechnology has provided a novel drug delivery system for erlotinib. The aims of this current investigation were to formulate two different polyamidoamine (PAMAM) dendrimer generations-generation 4 (G4) and generation 5 (G5) PAMAM dendrimer-to study the impact of two different PAMAM dendrimer formulations on entrapment by drug loading and encapsulation efficiency tests; to assess various characterizations, including particle size distribution, polydispersity index, and zeta potential; and to evaluate in vitro drug release along with assessing in situ human lung adenocarcinoma cell culture. The results showed that the average particle size of G4 and G5 nanocomposites were 200 nm and 224.8 nm, with polydispersity index values of 0.05 and 0.300, zeta potential values of 11.54 and 4.26 mV of G4 and G5 PAMAM dendrimer, respectively. Comparative in situ study showed that cationic G4 erlotinib-loaded dendrimer was more selective and had higher antiproliferation activity against A549 lung cells compared to neutral G5 erlotinib-loaded dendrimers and erlotinib alone. These conclusions highlight the potential effect of cationic G4 dendrimer as a targeting-sustained-release carrier for erlotinib.

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The provided information describes a study that aimed to investigate the impact of two different polyamidoamine (PAMAM) dendrimer formulations, specifically generation 4 (G4) and generation 5 (G5) PAMAM dendrimers, on the entrapment and encapsulation efficiency of erlotinib, a tyrosine kinase inhibitor used in the treatment of lung cancer. The study also evaluated various characteristics of the dendrimer formulations, including particle size distribution, polydispersity index, and zeta potential, and assessed in vitro drug release and in situ human lung adenocarcinoma cell culture.

The results of the study indicated that the average particle size of the G4 and G5 nanocomposites was 200 nm and 224.8 nm, respectively. The polydispersity index values were 0.05 for G4 and 0.300 for G5, while the zeta potential values were 11.54 mV for G4 and 4.26 mV for G5 PAMAM dendrimers. These measurements provide insights into the size distribution and surface charge of the dendrimer formulations.

Furthermore, the study compared the in vitro antiproliferative activity of the cationic G4 erlotinib-loaded dendrimer, neutral G5 erlotinib-loaded dendrimers, and erlotinib alone. The results demonstrated that the cationic G4 erlotinib-loaded dendrimer exhibited greater selectivity and higher antiproliferative activity against A549 lung cells, a type of human lung adenocarcinoma cell line, compared to the neutral G5 erlotinib-loaded dendrimers and erlotinib used alone. This suggests that the cationic G4 dendrimer formulation could potentially serve as a targeted and sustained-release carrier for erlotinib in the treatment of lung cancer.

In summary, the study showed that the cationic G4 PAMAM dendrimer formulation had favorable characteristics for drug delivery, such as smaller particle size, lower polydispersity index, and higher zeta potential. Moreover, this formulation demonstrated enhanced antiproliferative activity against lung cancer cells when loaded with erlotinib. These findings highlight the potential of utilizing cationic G4 dendrimers as an effective strategy for targeted and sustained-release delivery of erlotinib in lung cancer treatment.