Lipid and Biosurfactant Based Core–Shell-Type Nanocapsules Having High Drug Loading of Paclitaxel for Improved Breast Cancer Therapy

The current investigation illustrates high drug loading of Paclitaxel (PTX) in lipid- and biosurfactant-based core–shell-type nanocapsules for improving therapeutic potential and reducing toxicity of PTX. The nanocapsules were prepared using the antisolvent precipitation technique having a particle size of 253.8 ± 15.4 nm and drug loading of ∼19%. The microscopic evaluation revealed the spherical shape of the nanocapsules and corroborated with the particle size obtained from Zetasizer.

It also revealed the drug core enveloped by the relatively lighter shadowed region, that is, the layer of lipids and the biosurfactant. The in vitro release study showed biphasic and sustained release pattern of PTX from core–shell-type nanocapsules. In case of nanocapsules, the cellular uptake in the MCF-7 cell line was augmented ∼3.17-fold as compared to free PTX. Further, it was evident from the cytotoxicity assay that nanocapsules displayed greater cytotoxicity in MCF-7 cells and ∼2.98-fold decrease in the IC₅₀ value as compared to free PTX. The apoptotic index observed in case of nanocapsules was ∼2.04-fold higher than that of free PTX.

Furthermore, the pharmacokinetic profile of nanocapsules revealed a ∼7.21-fold increase in t_1/2 and a ∼3.27-fold higher AUC_(0→∞) compared to Intaxel. Finally, treatment with PTX core–shell-type nanocapsules demonstrated significant cutback in the % tumor burden and serum toxicity markers compared to marketed formulation. Thus, the current approach of core–shell-type nanocapsules with high drug loading can improve the current standards of PTX therapy for treatment of cancer.

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Article Information: Sameer S. Katiyar, Rohan Ghadi, Varun Kushwah, Chander Parkash Dora, and Sanyog Jain. ACS Biomaterials Science & Engineering, 2020. DOI: 10.1021/acsbiomaterials.0c01290