Design, Development, and Characterization of Carmustine-Loaded Nanostructured Lipid Carriers for Enhanced Brain Accumulation and Antitumor Efficacy in Glioblastoma

Abstract

Glioblastoma is one of the aggressive and hard-to-treat forms of brain tumor, and this is largely due to the presence of the blood-brain barrier and the inability of conventional chemotherapeutic agents to cross this barrier and act on the tumor cells.

The main aim of the current study is to design and evaluate Carmustine-loaded nanostructured lipid carriers (Carm-NLCs) for the treatment of glioblastoma with improved efficacy. The formulation of the NLCs was performed using a high-shear homogenization technique and ultrasonication, using Compritol as the solid lipid and oleic acid as the liquid lipid. Optimization of the formulation of NLCs was performed using a central composite design, and the effect of lipid composition on the size, zeta potential, and entrapment efficiency of the NLCs was evaluated.

The optimized formulation of NLCs had a size of approximately 193 ± 15 nm, polydispersity index of 0.25, zeta potential of 26.3 ± 0.36mV, and drug entrapment efficiency of 74.64 ± 2.4%. The spherical shape and well-dispersed nature of the nanoparticles were also confirmed using transmission electron microscopy. In-vitro studies on the release of the drug showed sustained release up to 48 h, whereas the pure drug, Carmustine, was released rapidly. Evaluation of the drug’s cytotoxicity using the MTT assay on U87MG glioblastoma cells showed a concentration-dependent effect on the cancer cells.

In-vivo studies showed a reduction in tumor volume, increased accumulation of the drug in the brain, and enhanced antioxidant enzyme levels, with favorable pharmacokinetics, indicating that the nanoparticles are a promising system for the management of glioblastoma.

Continue reading here

Dewangan, H.K., Garg, N., Bhushan, B. et al. Design, Development, and Characterization of Carmustine-Loaded Nanostructured Lipid Carriers for Enhanced Brain Accumulation and Antitumor Efficacy in Glioblastoma. J Pharm Innov 22, 95 (2027). https://doi.org/10.1007/s12247-026-10952-w

Read also our introduction article on Lipid Nanoparticles here:

• Milling of poorly water-soluble drugs in oil via dual centrifugation – A closer look at stabilization and application on orodispersible films
• Physical stability of RNA–lipid nanoparticles under agitation, freeze–thaw and accelerated stability testing
• Comparing the impact of various sucrose concentrations on the performance of various lipid-based nanoformulations for the delivery of trans-resveratrol as a model drug