Development and Optimisation of Docetaxel-Loaded Polymeric Nanoparticles for Oral Chemotherapy in Breast Cancer by Divya Wali Shivakumar H. Nanjappa Avichal Kumar & Rushikesh Shinde

Author:Divya Wali, Shivakumar H. Nanjappa, Avichal Kumar & Rushikesh Shinde
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Tags: Docetaxel (DTX)-loaded polymeric nanoparticles composed of Eudragit RL and RS 100 were developed by solvent evaporation using D–tocopheryl polyethene glycol 1000 succinate as an emulsifier and optimised by Central Composite Design. The effects of homogenisation and sonication times on entrapment efficiency (%EE) and drug release (%DR) were statistically analysed across nine batches. Particle size (PS) ranged from 302 1.0 to 502 2.0 nm, and zeta potential (ZP) from 25.8 2.5 to 42.9 1.7 mV. %EE and %DR (pH 1.2 for 2 h, then pH 7.4 for 22 h, 40 mL medium at 37 0.5 C) ranged from 69.32 3.77 to 92.71 0.16% and 19.24 3.03 to 49.17 1.98%, respectively. Optimised DTX nanoparticles (DNPs) showed EE of 78.18 0.56%, DR of 46.21 1.41% at 24 h, PS of 357.9 2.4 nm, and ZP of 42.9 3.7 mV. Scanning electron microscopy revealed ~300 nm cuboidal particles with smooth surfaces. X-Ray Diffraction and Differential Scanning Colorimetry confirmed reduced drug crystallinity in DNPs. In vitro haemolysis assays showed ~11.5-fold lower haemolytic potential (p < 0.0001) versus DTX, confirming improved safety. Fluorescence microscopy indicated enhanced cellular uptake of DNPs in MDA-MB-231 cells, while cytotoxicity assays of DNPs showed a lower IC50 (39.52 M) compared to DTX (60.81 M), demonstrating superior anticancer efficacy. Overall, DNPs represent a promising oral chemotherapy platform for breast cancer management., docetaxel-loaded nanoparticles; eudragit RL 100 and RS 100; oral chemotherapy; scanning electron microscopy; in vitro haemolysis; cell line study (MDA-MB-231); MTT Assay


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