The survival rate of foam cells can be increased with fluocinolone (0.1–50 μg/mL, for two days)[1]. Fluocinolone (0.1–50 μg/mL, 2 days) lowers the build-up of cholesterol ester and suppresses the release of inflammatory cytokines [1]. Fluocinolone (0.1-100 μmol/L, 24 h) stimulates DPC growth [2]. Fluocinolone (1–10 μmol/L, 7 days) upregulates the expression of dentin-specific marker dentin sialophosphoprotein and upregulates BSP, OCN, DSPP, and Wnt4 [2].

In a mouse model produced by PTX, fluocinolone (500 μg/kg, intraperitoneal injection, once daily for two weeks) inhibited the development of severe peripheral neuropathy [3].

Cell Proliferation Assay[2]
Cell Types: DCPs
Tested Concentrations: 0.1 μmol/L, 1 μmol/L, 10 μmol/L, 20 μmol/L, 40 μmol/L, 60 μmol/L, 100 μmol/L
Incubation Duration: 24 h
Experimental Results: Dramatically promoted the growth rate of DPCs of a low concentration.

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Western Blot Analysis[2]
Cell Types: DCPs
Tested Concentrations: 1 μmol/L, 10 μmol/L
Incubation Duration: 7 days
Experimental Results: demonstrated higher expressions of DSPP and Wnt4 protein than negative control.

Animal/Disease Models: PTX-induced peripheral neuropathy model [3]
Doses: 500 μg/kg
Route of Administration: intraperitoneal (ip)injection
Experimental Results: Prevented a marked reduction in intraepidermal nerve fibers density in the plantar surface of the hind paws.

Absorption, Distribution and Excretion
When administered as an eye implant, fluocinolone acetonide presents a sustained delivery for even 12 months in which there can be observed a sustained release. The concentration of fluocinolone acetonide are generally higher in the vitreous and retina with a little dispersion to the aqueous humor. There are reports indicating that topical administration of fluocinolone acetonide produces a percutaneous absorption which is determined by the vehicle, integrity of the epidermal barrier and the use of occlusive dressing. Independently of the route of administration, the systemic absorption of fluocinolone acetonide is below 0.1 ng/ml which indicates that the systemic distribution is very minimal and the effect of fluocinolone is mainly local.
Fluocinolone acetonide is mainly excreted by the kidneys. It is important to mention that the systemically absorbed dose is very minimal.
This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.
This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal and the concentration in urine is lower than the minimum quantitation limit.
METABOLISM OF CORTICOSTEROIDS IS GREATLY SLOWED BY INTRODUCTION OF THE 1,2 DOUBLE BOND OR A FLUORINE ATOM INTO MOLECULE, & HALF-LIFE IS CORRESPONDINGLY PROLONGED. /CORTICOSTEROIDS/
(14)C WAS RAPIDLY & MAINLY EXCRETED IN 48-HR FECES (90%), VIA BILE (70% IN 24 HR), & IN URINE (8%). AFTER DERMAL APPLICATION OF CREAM CONTAINING [(14)C]FLUOCINOLONE ACETONIDE TO MICE, GREATER THAN 7% OF (14)C WAS ABSORBED.
...WITHIN 1 HR OF SC DOSE OF [(14)C]FLUOCINOLONE ACETONIDE TO MICE, LARGE AMT...PRESENT IN LIVER & INJECTION SITE, LOWER AMT IN PANCREAS, KIDNEYS, SALIVARY GLANDS, MYOCARDIUM, PITUITARY, & LACRIMAL GLANDS. TISSUE (14)C DECR FAIRLY RAPIDLY DURING 24 HR, EXCEPT IN LIVER & INTESTINES, BECAUSE OF BILIARY SECRETION...
PENETRATION OF...FLUOCINOLONE ACETONIDE...TOPICALLY APPLIED, THROUGH HUMAN ABDOMINAL SKIN WAS OPTIMAL WHEN CONCN OF DRUGS WAS MAXIMAL WHILE MAINTAINING FAVORABLE PARTITION COEFFICIENT BETWEEN SKIN BARRIER & VEHICLE.
For more Absorption, Distribution and Excretion (Complete) data for FLUOCINOLONE ACETONIDE (6 total), please visit the HSDB record page.

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Metabolism / Metabolites
Following absorption, fluocinolone acetonide metabolism is primarily hepatic. It is important to mention that the systemically absorbed dose is very minimal.
...IT IS GENERALLY ASSUMED THAT METAB OF /CORTISOL &/ ITS CONGENERS & SYNTH DERIV IS QUALITATIVELY SIMILAR. ...METABOLIZED PRINCIPALLY BY REDN OF RING A, REDN OF KETONE AT C 20, & CLEAVAGE OF SIDE CHAIN. METABOLITES ARE EXCRETED...AS GLUCURONIDES, SULFATES, & UNCONJUGATED COMPOUNDS. /CORTICOSTEROIDS/

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Biological Half-Life
The reported half-life of fluocinolone acetonide ranges between 1.3-1.7 hours.

Protein Binding
This pharmacokinetic parameter is not relevant as the systemic absorption of fluocinolone acetonide is very minimal.

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Interactions
REVERSAL OF CORTICOSTEROID-INDUCED IMPAIRMENT OF WOUND HEALING HAS BEEN REPORTED AFTER TOPICAL APPLICATION OF VITAMIN /VITAMIN A/. /CORTICOSTEROIDS/

[1]. The potential of fluocinolone acetonide to mitigate inflammation and lipid accumulation in 2D and 3D foam cell cultures . BioMed Research International, 2018, 2018.

[2]. Fluocinolone acetonide promotes the proliferation and mineralization of dental pulp cells . Journal of endodontics, 2013, 39(2): 217-222.

[3]. Identification of fluocinolone acetonide to prevent paclitaxel‐induced peripheral neuropathy . Journal of the Peripheral Nervous System, 2016, 21(3): 128-133.

[4]. Glucocorticoids with different chemical structures but similar glucocorticoid receptor potency regulate subsets of common and unique genes in human trabecular meshwork cells . BMC medical genomics, 2009, 2(1): 1-14.

[5]. http://en.wikipedia.org/wiki/Fluocinolone_acetonide.

[6]. Glucocorticoids with different chemical structures but similar glucocorticoid receptor potency regulate subsets of common and unique genes in human trabecular meshwork cells. BMC Med Genomics, 2009. 2: p. 58.

Therapeutic Uses
Glucocorticoids, Synthetic; Glucocorticoids, Topical
WITH EXCEPTION OF SUBSTITUTION THERAPY, USE OF CORTICOSTEROIDS & THEIR CONGENERS IN DISEASE IS EMPIRICAL. ...FOR ANY DISEASE, IN ANY PT, APPROPRIATE DOSE TO ACHIEVE GIVEN THERAPEUTIC EFFECT MUST BE DETERMINED BY TRIAL & ERROR & MUST BE REEVALUATED FROM TIME TO TIME AS STAGE & ACTIVITY OF DISEASE ALTER... /CORTICOSTEROID/
GLUCOCORTICOID WITH POTENT ANTI-INFLAMMATORY & METABOLIC ACTIONS & NEGLIGIBLE MINERALOCORTICOID ACTIONS.
IT IS EMPLOYED TOPICALLY IN TREATMENT OF VARIOUS DERMATOSES. IN RESISTANT NUMMULAR DERMATITIS, PSORIASIS, OR CHRONIC NEURODERMATITIS USUALLY USED UNDER OCCLUSIVE DRESSINGS.
For more Therapeutic Uses (Complete) data for FLUOCINOLONE ACETONIDE (7 total), please visit the HSDB record page.

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Drug Warnings
...AS CORTICOSTEROID THERAPY IS PROLONGED OVER PERIODS OF MO, & TO EXTENT THAT DOSE EXCEEDS EQUIV OF SUBSTITUTION THERAPY, INCIDENCE OF DISABLING & POTENTIALLY LETHAL EFFECTS INCR; EXCEPT IN ADRENAL INSUFFICIENCY, ADMIN...IS NEITHER ETIOLOGICAL OR CURATIVE THERAPY BUT ONLY PALLIATIVE...ANTI-INFLAMMATORY... /CORTICOSTEROIDS/
EVEN IN INSTANCES IN WHICH NEARLY WHOLE BODY HAS BEEN COVERED BY CREAM CONTAINING CORTICOID, EVIDENCES OR SYSTEMIC SIDE EFFECTS ARE RARE. ... TOPICAL FLUOCINOLONE IS CONTRAINDICATED IN PRESENCE OF TUBERCULOSIS, FUNGAL INFECTIONS, & MOST VIRAL LESIONS OF SKIN (VACCINIA, VARICELLA, HERPES SIMPLEX, ETC).
...CAUTION SHOULD BE EXERCISED IF FLUORINATED PREPN ARE USED ON FACE OR OTHER COSMETICALLY IMPORTANT AREAS, SINCE PARADOXICAL SKIN ERUPTIONS MAY OCCUR WITH LONG-TERM USE.
VET: SOLN IN PROPYLENE GLYCOL USUALLY PRODUCES FAR MORE THAN "TRANSIENT STINGING SENSATION" DESCRIBED BY MFR & SHOULD BE AVOIDED ESP ON RAW OR DENUDED AREAS.
For more Drug Warnings (Complete) data for FLUOCINOLONE ACETONIDE (7 total), please visit the HSDB record page.

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Pharmacodynamics
Fluocinolone acetonide is a synthetic anti-inflammatory corticosteroid and thus, the effect of its interaction with the body produces vasoconstriction and suppression of membrane permeability, mitotic activity, immune response and release of inflammatory mediators. For its ophthalmic indications, fluocinolone acetonide is administered as intravitreal micro-insert. This preparation was observed in clinical trials to reduce the recurrence of uveitis flares by 2 fold when compared with the non treated patients even after six months after initial administration. As well the intraocular pressure seemed to increase slightly with the presence of the fluocinolone implant but it is important to monitor intraocular pressure.

C24H30F2O6

452.49

452.201

67-73-2

6215

White to off-white solid powder

1.4±0.1 g/cm3

578.5±50.0 °C at 760 mmHg

267-269 °C(lit.)

303.7±30.1 °C

0.0±3.6 mmHg at 25°C

1.577

2.24

2

8

2

32

960

9

C[C@]12C[C@@H]([C@]3([C@H]([C@@H]1C[C@@H]4[C@]2(OC(O4)(C)C)C(=O)CO)C[C@@H](C5=CC(=O)C=C[C@@]53C)F)F)O

FEBLZLNTKCEFIT-VSXGLTOVSA-N

InChI=1S/C24H30F2O6/c1-20(2)31-19-9-13-14-8-16(25)15-7-12(28)5-6-21(15,3)23(14,26)17(29)10-22(13,4)24(19,32-20)18(30)11-27/h5-7,13-14,16-17,19,27,29H,8-11H2,1-4H3/t13-,14-,16-,17-,19+,21-,22-,23-,24+/m0/s1

(1S,2S,4R,8S,9S,11S,12R,13S,19S)-12,19-difluoro-11-hydroxy-8-(2-hydroxyacetyl)-6,6,9,13-tetramethyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icosa-14,17-dien-16-one

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (4.60 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (4.60 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)