5-Fluorouracil and Anti-EGFR antibody scaffold chitosan-stabilized Pickering emulsion: Formulations, physical characterization, in-vitro studies in NCL-H226 cells, and in-vivo investigations in Wistar rats for the augmented therapeutic effects against squamous cell carcinoma

This research seeks to optimize a chitosan-stabilized Pickering emulsion (PE) containing 5-fluorouracil (5-FU) as a potential Squamous Cell Carcinoma therapy. The 5-Fluorouracil was also thoroughly analysed using UV spectrophotometry and RP-HPLC, demonstrating exceptional linearity, sensitivity, pre...

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Veröffentlicht in:International journal of biological macromolecules 2023-12, Vol.253, p.126716-126716, Article 126716
Hauptverfasser: Bhattacharya, Sankha, Shinde, Prafull, Page, Amit, Sharma, Satyam
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Sprache:eng
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Zusammenfassung:This research seeks to optimize a chitosan-stabilized Pickering emulsion (PE) containing 5-fluorouracil (5-FU) as a potential Squamous Cell Carcinoma therapy. The 5-Fluorouracil was also thoroughly analysed using UV spectrophotometry and RP-HPLC, demonstrating exceptional linearity, sensitivity, precision, and robustness. The techniques of characterization revealed Pickering emulsion (PE) morphology, solid-like gel properties, successful encapsulation, and promising anticancer effects. FTIR was used to validate the efficacy of encapsulation, and DSC was used to confirm the post-encapsulation drug stability. The 0.6 % chitosan-stabilized PE showed exceptional stability and drug loading efficiency. Anti-EGFR-5-FU-CS-PE gel was developed for sustained drug release in the treatment of Squamous Cell Carcinoma. Anti-EGFR-5-FU-CS-PE demonstrated potent anticancer effects in vitro, with a lower IC50 than 5-FU and 5-FU-CS-PE. Anti-EGFR-5-FU-PE Pickering emulsions based on chitosan were investigated for their rheological properties, cellular interactions, and therapeutic potential. Both emulsions and gel exhibited sustained in vitro drug release after successful encapsulation. Anti-EGFR-5-FU-CS-PE induced apoptosis, decreased mitochondrial membrane potential, and inhibited the migration of cancer cells. Wistar mice were tested for safety and tumour growth inhibition. All formulations exhibited exceptional six-month stability. Anti-EGFR-5-FU-CS-PE emerges as a viable therapeutic option, necessitating additional research. [Display omitted] •0.6 % chitosan and 3–6 pH have positive impact on Pickering emulsion stability.•Anti-EGFR-5-FU-CS-PE Pickering emulsions exhibit lower deformability.•Anti-EGFR-5-FU-CS-PE exhibits potent anticancer effects.•Flow cytometry confirms apoptosis induction in NCL-H226 cells.•Anti-EGFR-5-FU-CS-PE gel reduces tumour burden in Wistar rats.
ISSN:0141-8130
1879-0003
DOI:10.1016/j.ijbiomac.2023.126716