Effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox

Tuğba Gülsün; Yagmur Akdag; Nihan Izat; Levent Öner; Selma Şahin

Effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox

Abstract

Deferasirox is an oral iron chelator used for the treatment of chronic iron overload in blood transfusions. Deferasirox is a BCS Class II drug with low solubility and high permeability. In the formulation development stage for BCS Class II compounds, one of the main approaches is solubility enhancement to achieve better dissolution profiles, increased bioavailability and in some cases, dose reduction. The aim of the study was to investigate the effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox. Ball milling method was used to reduce the particle size of deferasirox. Pluronic F127 or sodium lauril sulfate (SLS) were selected as surfactants at different concentrations. The maximum increase in the solubility was obtained with 10% SLS at pH 1.2 (from 0.9 µg/mL to 333.7 µg/mL), and with 5% Pluronic F127 at pH 6.8 (from 46.8 µg/mL to 334.2 µg/mL). Dissolution studies revealed that time to dissolve 85% of deferasirox was decreased as a function of ball milling time and particle size. Permeability studies showed that, in 100 µM concentration, deferasirox permeability was significantly enhanced by all concentrations of SLS (p<0.05). With an increase in Pluronic F127 concentration, permeability of deferasirox was not altered (p>0.05). All these results clearly demonstrated that surfactant addition to the formulations was effective for solubility enhancement of deferasirox, and surfactant type in optimized concentrations was very crucial. Particle size reduction can be used as a promising approach to improve dissolution, and hence bioavailability of deferasirox.

Keywords

References

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Details

Primary Language

English

Subjects

Pharmaceutical Chemistry, Pharmaceutical Delivery Technologies

Journal Section

Research Article

Authors

Tuğba Gülsün This is me
Türkiye

Yagmur Akdag
Türkiye

Nihan Izat This is me
Türkiye

Levent Öner
Türkiye

Selma Şahin ^*
Türkiye

Publication Date

June 27, 2025

Submission Date

March 19, 2019

Acceptance Date

April 13, 2019

Published in Issue

Year 2019 Volume: 23 Number: 5

IZ

https://izlik.org/JA73EU97JU

Cite

RIS / Bibtex

APA

Gülsün, T., Akdag, Y., Izat, N., Öner, L., & Şahin, S. (2025). Effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox. Journal of Research in Pharmacy, 23(5), 851-859. https://izlik.org/JA73EU97JU

AMA

1.Gülsün T, Akdag Y, Izat N, Öner L, Şahin S. Effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox. J. Res. Pharm. 2025;23(5):851-859. https://izlik.org/JA73EU97JU

Chicago

Gülsün, Tuğba, Yagmur Akdag, Nihan Izat, Levent Öner, and Selma Şahin. 2025. “Effect of Particle Size and Surfactant on the Solubility, Permeability and Dissolution Characteristics of Deferasirox”. Journal of Research in Pharmacy 23 (5): 851-59. https://izlik.org/JA73EU97JU.

EndNote

Gülsün T, Akdag Y, Izat N, Öner L, Şahin S (July 1, 2025) Effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox. Journal of Research in Pharmacy 23 5 851–859.

IEEE

[1]T. Gülsün, Y. Akdag, N. Izat, L. Öner, and S. Şahin, “Effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox”, J. Res. Pharm., vol. 23, no. 5, pp. 851–859, July 2025, [Online]. Available: https://izlik.org/JA73EU97JU

ISNAD

Gülsün, Tuğba - Akdag, Yagmur - Izat, Nihan - Öner, Levent - Şahin, Selma. “Effect of Particle Size and Surfactant on the Solubility, Permeability and Dissolution Characteristics of Deferasirox”. Journal of Research in Pharmacy 23/5 (July 1, 2025): 851-859. https://izlik.org/JA73EU97JU.

JAMA

1.Gülsün T, Akdag Y, Izat N, Öner L, Şahin S. Effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox. J. Res. Pharm. 2025;23:851–859.

MLA

Gülsün, Tuğba, et al. “Effect of Particle Size and Surfactant on the Solubility, Permeability and Dissolution Characteristics of Deferasirox”. Journal of Research in Pharmacy, vol. 23, no. 5, July 2025, pp. 851-9, https://izlik.org/JA73EU97JU.

Vancouver

1.Tuğba Gülsün, Yagmur Akdag, Nihan Izat, Levent Öner, Selma Şahin. Effect of particle size and surfactant on the solubility, permeability and dissolution characteristics of deferasirox. J. Res. Pharm. [Internet]. 2025 Jul. 1;23(5):851-9. Available from: https://izlik.org/JA73EU97JU