Investigation of bioavailability and anti-pancreatic cancer efficacy of a self-nanoemulsifying erlotinib delivery system

Aims

A new self-nanoemulsifying drug delivery system (SNEDDS) was developed for erlotinib (Ert) oral delivery.

Highlights

• A pseudo-ternary phase diagram for olive oil, Tween 80 and PEG 600 was constructed.

• A SNEDDS composed of 10% olive oil, 20% Tween 80 and 70% (V) PEG 600 was selected for Ert loading.

• ERT-SNEDDS formed oil droplets of 83.9 ± 0.6 nm.

• Loading capacity and entrapment efficiency were 22.7 ± 0.7 and 40.7 ± 0.5%, respectively.

• Ert-SNEDDS led to enhancement in the drug bioavailability, and changed the release route of Ert.

• Ert-SNEDDS showed enhanced cytotoxicity toward ASPC-1 and PANC-1 cells.

Results and conclusions

SNEDDS formed 31.2-nm droplets upon dilution in water, and Ert loading led to increment in the oil droplets to 83.9 ± 0.6 nm. Ert-SNEDDS represented a loading capacity and an entrapment efficiency of 22.7 ± 0.7 and 40.7 ± 0.5%, respectively. Ert release from Ert-SNEDDS was monitored in both a mixture of phosphate buffer saline and 0.5% Tween 80, and artificial gastric fluid. Ert-SNEDDS was orally administrated in rats, and the Ert plasma level was monitored over time to measure pharmacokinetic parameters. Ert-SNEDDS led to enhancement in the drug bioavailability and changed the release route of Ert. Ert-SNEDDS showed enhanced cytotoxicity toward ASPC-1 and PANC-1 cells, and half-maximal inhibitory concentration values were obtained and compared with free Ert. Ert-SNEDDS may be considered as an alternative route for oral Ert delivery.

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Materials and methods

A pseudo-ternary phase diagram for olive oil, Tween 80 and polyethylene glycol (PEG) 600 mixtures, was firstly constructed. Based on the data about Ert solubility and cytotoxicity of these components, a SNEDDS composed of 10% olive oil, 20% Tween 80 and 70% (V/V) polyethylene glycol 600 was selected for Ert loading (Ert-SNEDDS).

Karimi, M., Dehdari Vais, R., Karimian, K., Parsaei, A., & Heli, H. (2025). Investigation of bioavailability and anti-pancreatic cancer efficacy of a self-nanoemulsifying erlotinib delivery system. Therapeutic Delivery, 1–10. https://doi.org/10.1080/20415990.2025.2466412

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