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Evaluation the effect of cyclodextrin complexation on aqueous solubility of fluorometholone to achieve ophthalmic solution

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Abstract

In this study, the effect of different CDs including α-CD, β-CD, γ-CD, hydroxypropyl β-CD (HP β-CD), sulphobutylether β-CD (SBE β-CD) and HP γ-CD on aqueous solubility of fluorometholone (Flu) was investigated. Also the phase solubility studies were performed in the presence of eye drop excipients such as benzalkonium chloride, hydroxypropyl methylcellulose (HPMC) and buffers. The aqueous solubility of Flu was increased by 8, 15, 5, 100, 65 and 135 folds in the presence of 20% w/v α-CD, β-CD, γ-CD, HP β-CD, HP γ-CD and SBE β-CD, respectively. Aqueous solubility of Flu was 0.43 ± 0.08 and 1.16 ± 0.04 mg/mL in systems containing 5% w/v HP γ-CD and SBE β-CD, respectively. The aqueous solubility of Flu in the presence of HP γ-CD was not influenced by buffer type while the phosphate buffer caused a reduction in the aqueous solubility in the presence of SBE-β-CD. Also, investigations on the solubility of Flu in water in the presence of 5% HP γ-CD and SBE-β-CD and the additives such as benzalkonium chloride and HPMC indicated that these components had no remarkable effect on the aqueous solubility of Flu. In conclusion, CD complexation is able to improve the aqueous solubility of Flu and it would be possible to prepare ophthalmic solution of Flu by this method.

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Acknowledgment

This work was supported financially by a research grant from the Vice Chancellor for Research of Mashhad University of Medical Sciences, Mashhad, Iran.

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Authors and Affiliations

  1. Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Research Centre, Mashhad University of Medical Sciences, P.O. Box 91775-1365, Mashhad, Iran

    Bizhan Malaekeh-Nikouei

  2. Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Research Centre for Medicinal Plants, Mashhad University of Medical Sciences, Mashhad, Iran

    Sayyed A. Sajadi Tabassi

  3. School of Pharmacy, Mashhad University of Medical Sciences, Mashhad, Iran

    Hossein Ashari & Ali Gholamzadeh

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  1. Bizhan Malaekeh-Nikouei
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  2. Sayyed A. Sajadi Tabassi
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Correspondence to Bizhan Malaekeh-Nikouei.

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Malaekeh-Nikouei, B., Sajadi Tabassi, S.A., Ashari, H. et al. Evaluation the effect of cyclodextrin complexation on aqueous solubility of fluorometholone to achieve ophthalmic solution. J Incl Phenom Macrocycl Chem 65, 335–340 (2009). https://doi.org/10.1007/s10847-009-9590-1

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  • DOI: https://doi.org/10.1007/s10847-009-9590-1

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