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96 protocols using poloxamer 407

1

Cyclodextrin-Based Topical Formulation

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Example 38

Quantity (mg/g of
Ingredientformulation)
5% CD solution500.0
methylparaben1.0
TRIS HCl buffer (0.1M)317.0

The Poloxamer 407 (BASF Corp.) is suspended in the TRIS HCl buffer (0.1 M) and the components are mixed under agitation overnight at 4° C. to ensure complete dissolution. The cyclodextrin solution from Example 4 and methylparaben is added and further stirring allowed until complete dissolution is observed. The mixture is maintained below room temperature until use.

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2

Mucoadhesive Gel Formulation of SR-121463

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Example 5

Quantity (mg/g of
Ingredientformulation)
SR-12146320.0
methylparaben1.0
HPMC10.0
Carbopol 934P2.0
TRIS HCl buffer (0.1M)787.0

A 10-g batch of mucoadhesive, gel formulation containing 2.0% of SR-121463 is prepared by suspending 2.0 mg of Carbopol 934P and 1.80 g of Poloxamer 407 (BASF Corp.) in 5.00 g of TRIS HCl buffer (0.1 M) and the components are mixed under agitation overnight at 4° C. to ensure complete dissolution. The SR-121463 (200.0 mg), hydroxypropylmethylcellulose (100.0 mg), methylparaben (10 mg) and additional TRIS HCl buffer (0.1 M) (2.87 g) are added and further stirring allowed until complete dissolution is observed. The mixture is maintained below room temperature until use.

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3

Poloxamer 407-Based TRIS HCl Formulation

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Example 38

Quantity
Ingredient(mg/g of formulation)
5% CD solution500.0
methylparaben1.0
TRIS HCl buffer (0.1M)317.0

The Poloxamer 407 (BASF Corp.) is suspended in the TRIS HCl buffer (0.1 M) and the components are mixed under agitation overnight at 4° C. to ensure complete dissolution. The cyclodextrin solution from Example 4 and methylparaben is added and further stirring allowed until complete dissolution is observed. The mixture is maintained below room temperature until use.

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4

Iniparib Gel Formulation Protocol

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Example 6

IngredientQuantity (mg/g of formulation)
Iniparib20.0
methylparaben1.0
HPMC10.0
TRIS HCl buffer (0.1M)789.0

A 10-g batch of gel formulation containing 2.0% of iniparib is prepared by suspending 1.80 g of Poloxamer 407 (BASF Corp.) in 5.00 g of TRIS HCl buffer (0.1 M) and the components are mixed tinder agitation overnight at 4° C. to ensure complete dissolution. Iniparib (200.0 tug), hydroxvpropylinethylcellulose (100.0 mg), methlviparaben (10 mg) and additional TRIS HCl buffer (0.1 M) (2.89 g) is added and further stirring allowed until dissolution is observed. The mixture is maintained below room temperature until use.

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5

Iniparib Mucoadhesive Gel Formulation

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Example 9

IngredientQuantity (mg/g of formulation)
Iniparib20.0
methylparaben1.0
HPMC10.0
Carbopol 934P2.0
TRIS HCl buffer (0.1M)787.0

A 10-g batch of mucoadhesive, gel formulation containing 2.0% of iniparib is prepared by suspending 2.0 mg of Carbopol 934P and 1.80 g of Poloxamer 407 (BASF Corp.) in 5.00 g of TRIS HCl buffer (0.1 M) and the components are mixed under agitation overnight at 4° C. to ensure complete dissolution. The iniparib (200.0 mg), hydroxypropylmethylcellulose (100.0 mg), methylparaben (10 mg) and additional TRIS HCl buffer (0.1 M) (2.87 g) are added and further stirring allowed until complete dissolution is observed. The mixture is maintained below room temperature until use.

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6

Poloxamer 407 Formulation Protocol

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Example 38

Quantity
Ingredient(mg/g of formulation)
5% CD solution500.0
methylparaben1.0
TRIS HCl buffer (0.1M)317.0

The Poloxamer 407 (BASF Corp.) is suspended in the TRIS HCl buffer (0.1 M) and the components are mixed under agitation overnight at 4° C. to ensure complete dissolution. The cyclodextrin solution from Example 4 and methylparaben is added and further stirring allowed until complete dissolution is observed. The mixture is maintained below room temperature until use.

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7

Poloxamer 407-based Cyclodextrin Formulation

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Example 38

Quantity
Ingredient(mg/g of formulation)
5% CD solution500.0
methylparaben1.0
TRIS HCl buffer (0.1M)317.0

The Poloxamer 407 (BASF Corp.) is suspended in the TRIS HCl buffer (0.1 M) and the components are mixed under agitation overnight at 4° C. to ensure complete dissolution. The cyclodextrin solution from Example 4 and methylparaben is added and further stirring allowed until complete dissolution is observed. The mixture is maintained below room temperature until use.

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8

Poloxamer-Based siRNA Delivery System

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Poloxamer 407 (BASF, Ludwigshafen, Germany; 25% w/w) was added to isotonic phosphate-buffered saline (PBS, pH 7.4, 4°C) with gentle mixing until complete dilution [18 (link)]. Then, rhPTH (1–34) (Lilly, Fegersheim, France) or IGF-1 (ab198570, Abcam, Cambridge, USA) was added to the prepared Poloxamer 407 solutions, and the final concentrations of IGF-1 and rhPTH (1–34) were 60 μg/ml and 80 μg/ml, respectively.
The Pth1r or IGF-1r siRNA (Sigma-Aldrich, USA) transfection complex was prepared according to the manufacturer’s instructions. In brief, 20 μg of siRNA (sequences are provided in Table 1) was dissolved in 20 μl of RNase-free water, followed by the addition of 10 μl of EntransterTM-in vivo (Engreen, Beijing, China) and gentle mixing; the mixture was then incubated for 15 min at room temperature. Finally, 20 μl of Poloxamer 407 (BASF, Ludwigshafen, Germany, 50% w/w) was added to the solution with sufficient mixing.
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9

Mucoadhesive Gel Formulation with Novel Compounds

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Example 52

Quantity (mg/g of
Ingredientformulation)
AL-15469A25.5
AL-3890525.5
methylparaben2.55
Hypromellose25.5
Carbopol 934P5.1
TRIS HCl buffer (0.1M)2006.85

Both AL-15469A and AL-38905 are supplied as solids. They are rehydrated in water to a final molarity of 10 mM.

A 10-g batch of mucoadhesive gel formulation containing 1.0% of AL-15469A and 1% of AL-38905 is prepared by first suspending Poloxamer 407 (BASF Corp.) and Carbopol 934P in TRIS HCl buffer (0.1 M). The Poloxamer 407, Carbopol 934P and TRIS are mixed under agitation overnight at 4° C. to ensure complete dissolution of the Poloxamer 407 and Carbopol 934P in the TRIS. The hypromellose, methylparaben and additional TRIS HCl buffer (0.1 M) is added. The composition is stirred until dissolution is observed. The AL-15469A and AL-38905 solutions are added and the composition is mixed until a homogenous gel is produced. The mixture is maintained below room temperature until use.

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10

Curcuminoid-Loaded Mucoadhesive Formulation

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MFC was prepared by mixing polyethylene glycol 400 and propilenglycol (1:1, v/v) in a heated reactor (65–70 °C). Then, 9.0% (w/v) poloxamer 407 (Basf, Ludwigshafen, Germany) was added to the mixture under mechanical stirring until complete dispersion. After that, curcuminoids from C. longa L. extract (>95% curcuminoid content, Gamma Comércio Importação & Exportação LTDA, São Paulo, Brazil) was added to the organic phase and pH was adjusted by using 0.1 M citric acid (pH 6.5). The final concentration of curcuminoids was 25 mg/mL. An aqueous fraction was prepared by dispersing 6% (w/v) of poloxamer 407 in purified water, under constant stirring. After dispersion, Soluplus® (Basf, Ludwigshafen, Germany), sodium metabisulphite and sodium bisulphite were added under stirring. The aqueous fraction was then heated up to 65 °C and poured into organic fraction. The mixture was stirred for 30 min. MFC was then bottled in ambar flask and stored at room temperature until use. A blank mucoadhesive formulation (control) was prepared as described above, but without adding curcuminoids extract.
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