Cationic Lipid Nanoparticles for Co-Encapsulation of Etoposide and Carboplatin: Formulation, Characterization, and In Vitro Evaluation
JOURNAL OF PHARMACEUTICAL INNOVATION, cilt.22, sa.1, 2026 (SCI-Expanded, Scopus)
- Yayın Türü: Makale / Tam Makale
- Cilt numarası: 22 Sayı: 1
- Basım Tarihi: 2026
- Doi Numarası: 10.1007/s12247-026-10913-3
- Dergi Adı: JOURNAL OF PHARMACEUTICAL INNOVATION
- Derginin Tarandığı İndeksler: Science Citation Index Expanded (SCI-EXPANDED), Scopus, EMBASE, INSPEC, Health Research Premium Collection (ProQuest)
- Ankara Üniversitesi Adresli: Evet
Özet
Objectives This study aimed to enhance the anticancer activity of carboplatin (CRB) and etoposide (ETO) by co-loading them into cationic lipid nanoparticles (LNPs) at reduced doses. This approach sought to minimize dose-related toxicity, improve bioavailability, and increase interaction with the lung epithelium through 1,2-dioleoyl-3-trimethylammonium-propane (DOTAP)-mediated surface charge modification. Several formulations were prepared, characterized, and the most promising system was further evaluated in cell-based studies to develop a more effective and better-tolerated dual-drug delivery platform for lung cancer treatment.Methods LNPs were produced using a modified homogenization-sonication method, in which lipid content and the DOTAP/lipid ratio were systematically varied to assess their impact on particle properties and drug encapsulation. The optimized formulation underwent Differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR), Transmission electron microscopy (TEM), and in vitro release analysis, followed by cytotoxicity, cellular uptake, and apoptosis studies on A549 cells.Results The formulations exhibited particle sizes (PS) of 101-392 nm, polydispersity index (PDI) values of 0.17-0.49, and zeta potentials (ZP) ranging from - 6.9 to + 28.9 mV. Encapsulation efficiencies (EE%) were 88.3-96.7% for ETO and 6.3-52.6% for CRB. The optimized LNPs showed sustained release with a reduced initial burst effect. DSC, FTIR, and TEM confirmed successful drug incorporation and particle integrity. In A549 cells, the co-loaded LNPs exhibited the strongest cytotoxic activity, achieving an IC50 value of 6.39 & micro;g/mL, compared with free drugs and other LNPs.Conclusion Co-delivery of ETO and CRB using cationic LNPs presents a promising approach to improve therapeutic efficacy while potentially reducing systemic toxicity in lung cancer treatment.