Fluorometholone

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Cat Number

API426131

CAS Number

426-13-1

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Product Detail Description Advanced Innovations Customer Q&A

CAS Number

426-13-1

EINECS

207-041-5

Storage

2-8℃

Synonyms

(6S,8S,9R,10S,11S,13S,14S,17R)-17-acetyl-9-fluoro-11,17-dihydroxy-6,10,13-trimethyl-6,7,8,11,12,14,15,16-octahydrocyclopenta[a]phenanthren-3-one;2Chemicalbook1-Desoxy-9a-fluoro-6-methylprednisolone;6a-Methyl-9a-fluoro-21-desoxyprednisolone;9a-Fluoro-11b,17a-dihydroxy-6a-methylpregna-1,4-diene-3,20-dione

Molecular Formula

C22H29FO4

Molecular Weight

376.5

Smiles

C[C@H]1C[C@H]2[C@@H]3CC[C@@]([C@]3(C[C@@H]([C@@]2([C@@]4(C1=CC(=O)C=C4)C)F)O)C)(C(=O)C)O

Appearance

White to off-white solid

Melting Point

292-303℃

Boiling Point

527℃

Relative Density

1.06

pKa

12.5

General Description

Fluorometholone is a synthetic fluorinated glucocorticoid developed specifically for ophthalmic applications. It features a 9-fluoro and 6-methyl substitution on the pregnane steroid skeleton, which together provide potent anti-inflammatory activity with a pharmacokinetic profile that reduces intraocular pressure elevation compared to prednisolone.

Mechanism of Action

Fluorometholone binds to intracellular glucocorticoid receptors in ocular tissues, and the receptor complex modulates transcription to suppress production of prostaglandins, leukotrienes, and cytokines in the anterior segment. Its relatively lower corneal penetration reduces the trabecular meshwork exposure that drives steroid-induced ocular hypertension.

Application

Indicated for the treatment of ocular inflammation including postoperative inflammation, anterior uveitis, and allergic conjunctivitis. Fluorometholone is a synthetic fluorinated glucocorticoid designed specifically for ophthalmic use, providing potent anti-inflammatory activity with reduced risk of intraocular pressure elevation.

Fluorometholone-loaded PLGA nanoparticles were incorporated into thermosensitive in-situ forming gels for ocular delivery. The nanoparticles maintained their spherical morphology and average size within the gel matrix as confirmed by transmission electron microscopy. The formulation exists as a sol at temperatures below 25°C, allowing administration as eye drops, and transforms into a gel at corneal temperature. The in-situ gelling system prevented burst release of fluorometholone, providing a slow and sustained release profile. Ocular tolerance studies confirmed no eye irritation. The developed formulations significantly improved precorneal residence time and enhanced ocular bioavailability, allowing the drug to reach deep tissues including the aqueous humour and crystalline lens.

Fig. 2 Characterization of Fluorometholone-loaded PLGA nanoparticles. (Gonzalez-Pizarro R.; et al. 2019)

References

Gonzalez-Pizarro R, et al. In-situ forming gels containing fluorometholone-loaded polymeric nanoparticles for ocular inflammatory conditions. Colloids and Surfaces B: Biointerfaces, 2019, 175: 365-374.

What distinguishes Fluorometholone from prednisolone in ophthalmic therapy?

Fluorometholone has lower corneal and intraocular penetration than prednisolone, resulting in reduced aqueous humor accumulation and lower risk of steroid-induced ocular hypertension.

What storage conditions are required?

Should be stored at 2-8℃ in a tightly sealed container, protected from light and moisture.

What purity grade is available?

Supplied as a high-purity grade suitable for ophthalmic R&D and pharmaceutical manufacturing.

Can packaging be customized?

Packaging formats and order quantities are customizable upon request for R&D and production needs.