Erlotinib loaded chitosan nanoparticles: Formulation, physicochemical characterization and cytotoxic potential

• Published in: International journal of biological macromolecules 2019-10, Vol.139, p.1304-1316
• Main Authors: Pandey, Parijat, Dua, Kamal, Dureja, Harish
• Format: Article
• Language: English
• Subjects: A549 Cells; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Box-behnken design; Chemical Phenomena; Chitosan - chemistry; Drug Carriers - chemistry; Drug Compounding; Drug Liberation; Erlotinib; Erlotinib Hydrochloride - chemistry; Erlotinib Hydrochloride - pharmacology; Humans; Kinetics; Nanoparticles - chemistry; Particle Size; Spray drying
• ISSN: 0141-8130; 1879-0003
• DOI: 10.1016/j.ijbiomac.2019.08.084

Cancer is the major cause of mortality and morbidity throughout the world where >10 million patients with new cases diagnosed every year. The objective of this study was to prepare and evaluate erlotinib loaded chitosan nanoparticles for their anticancer potential. Also, to study the effect of various formulation variables on prepared nanoparticles using box-behnken design. Erlotinib loaded chitosan nanoparticles were prepared by ionic gelation method using the spray drying technique. It was found that batch SNP-9 has a maximum loading capacity (74.45 ± 0.34%) and entrapment efficiency (43 ± 0.57%) with a particle size 170.2 nm. Analysis of variance (ANOVA) was applied on the particle size, entrapment efficiency and % cumulative drug release to study the fitting and the significance of the model. The batch SNP-9 showed 89.46% and 40.12% drug release after 24 h in 0.1 N HCl and Phosphate Buffer (pH 6.8), respectively. The IC50 value of SNP-9 evaluated on A549 Lung cancer cells was found to be 4.41 μM. The optimized formulation was found stable after the six-month study as no considerable transformation was detected. The optimized formulation released erlotinib slowly in comparison to the marketed tablet formulation. Erlotinib loaded chitosan nanoparticles were prepared successfully using spray drying technique with suitable particle size, entrapment efficiency, drug release. The synthesized and optimized nanoparticles were found to possess activity against cancer cells when evaluated in-vitro.