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6 protocols using lecithin s pc

1

In vitro Dissolution and Solubility

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Hydrochloric acid (HCl), potassium hydroxide (KOH), acetic acid, sodium taurocholate, lecithin S PC (phosphatidylcholine from Soybean “98%”) from Lipoid, Germany and Pancreatin from porcine sources, monosodium phosphate (NaH2PO4), sodium chloride (NaCl), chloroform, fenofibrate, and indomethacin were purchased from Sigma-Aldrich, Poole, Dorset UK. The active pharmaceutical ingredients aprepitant, carvedilol, felodipine, probucol, tadalafil and zafirlukast were kindly provided through OrBiTo (see Acknowledgements) by Dr. R. Holm Head of Preformulation, Lundbeck, Denmark. Itraconazole, bromocriptine, valsartan and phenytoin were purchased from Sigma, Poole, Dorset, UK. Sodium oleate was obtained from BDH Chemical Ltd. Poole England. All water used was ultrapure Milli-Q water. The analytical solvents methanol and acetonitrile were of HPLC grade (VWR, UK). Other materials used in this study included trifluoroacetic acid (Merck Schuchardt OHG, Germany) and ammonium acetate (Merck, Germany).
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2

Lipid-based Nanocarrier Formulation

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Sodium taurocholate (>97%), monosodium dihydrogen phosphate (100%), ammonium formate (>99.995%), formic acid (98–100%), sodium chloride (NaCl), potassium hydroxide (KOH, >85%), hydrochloric acid solution (HCl, analytical grade), acetic acid (>99.7%), cholesterol (>99%), chloroform (99.5%), fenofibrate, and chitosan (from crab shells, practical grade) were purchased from Sigma-Aldrich, Poole, Dorset, UK. Lecithin S PC (phosphatidylcholine from soybean, 98%) was supplied by Lipoid, Ludwigshafen, Germany. Sodium oleate (technical grade) was obtained from BDH Chemicals Ltd., Poole, England. Monoglyceride (glyceryl mono-oleate, >92% monoester, and 88% oleic acid) was supplied by CRODA. Polyvinylpyrrolidone (PVP, Plasdone TM K-12 and Plasdone TM K-29/32) were from Ashland, Singapore. Hydroxypropyl methylcellulose (HMPC, Hypromellose) (Methocel E3 and E50 premium LV) were obtained from Colorcon Ltd., Kent, UK. Mannitol (pharmaceutical grade) was obtained from Blackburn Distributions, Nelson, UK. All water used was ultrapure Milli-Q. Methanol and acetonitrile was purchased from VWR Prolabo Chemicals, Poole, UK.
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3

Solubility-Enhancing Formulation Development

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Sodium taurocholate, ammonium formate, sodium chloride (NaCl), chloroform, formic acid, monosodium phosphate (NaH2PO4), fenofibrate, indomethacin and phenythoin were purchased from Sigma Aldrich Poole, Dorset UK. Lecithin S PC (phosphatidylcholine from Soybean “98%”) was purchased from Lipoid. Glycerol mono oleate was obtained from CRODA Healthcare. The active pharmaceutical ingredients felodipine, probucol, aprepitant, tadalafil, carvedilol and zafirlukast were provided through OrBiTo by Dr. R. Holm Head of Preformulation, Lundbeck, Denmark. Sodium oleate was obtained from BDH Chemical Ltd. Poole England. The analytical solvents methanol and acetonitrile were of HPLC grade (VWR, UK). All water was ultra pure Milli-Q water.
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4

Physicochemical Characterization of BCS II Compounds

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Sodium taurocholate (>97%), monosodium
dihydrogen
phosphate (100%), ammonium formate (>99.995%), formic acid (98–100%),
sodium chloride (NaCl), potasium hydroxide (KOH, > 85%), hydrochloric
acid solution (HCl, analytical grade), cholesterol (>99%), chloroform
(99.5%), fenofibrate, indomethacin, and phenytoin were purchased from
Sigma-Aldrich, Poole, Dorest, UK. Lecithin S PC (phosphatidylcholine
from soybean 98%) was supplied from Lipoid, Germany. Sodium oleate
(technical grade) was from BDH chemical Ltd. Poole, England. Monoglyceride
(glyceryl mono-oleate, > 92% monoester, and 88% oleic acid) was
kindly
supplied from CRODA. The BCS class II compounds felodipine, aprepitant,
tadalafil, carvedilol, and zafirlukast were provided through OrBiTo
by Dr. R Holm, Head of Preformulation, Lundbeck, Denmark. All water
used was ultrapure Milli-Q water. Methanol and acetonitrile were purchased
from VWR Prolabo Chemicals, UK.
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5

Lipid-Based Formulation Development

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Hydrochloric acid (HCl),
potassium hydroxide (KOH), acetic acid, sodium dihydrogen orthophosphate
(NaH2PO4), sodium chloride (NaCl), chloroform,
griseofulvin, spironolactone, and fenofibrate were sourced from Sigma-Aldrich,
U.K. Aprepitant, carvedilol, felodipine, and zafirlukast were kindly
provided through the OrBiTo initiative through Dr R. Holm, Head of
Preformulation, Lundbeck, Denmark. The four amphiphiles in this particular
study will be denoted as BS, PL, OA, and MG. Sodium taurocholate (BS)
was purchased from Sigma-Aldrich; Lecithin S PC (phosphatidylcholine
from Soybean “98%”, PL) was purchased from Lipoid, Germany;
sodium oleate (OA) was obtained from BDH Chemical Ltd. Poole England;
monoglyceride (MG) was a gift from Croda International. All water
used was ultrapure Milli-Q water. Methanol and acetonitrile were HPLC
grade (VWR, U.K.), and ammonium acetate was obtained from Merck, Germany.
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6

Formulation Development and Characterization

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Hydrochloric
acid (HCl), potassium hydroxide
(KOH), acetic acid, sodium dihydrogen orthophosphate (NaH2PO4), sodium chloride (NaCl), chloroform, indomethacin,
and fenofibrate were sourced from Sigma-Aldrich, UK. Carvedilol was
kindly provided through the OrBiTo initiative by Dr. R. Holm, Head
of Preformulation, Lundbeck, Denmark. NATC was purchased from Sigma-Aldrich.
Lecithin S PC (phosphatidylcholine from soybean “98%”,
SPC) was purchased from Lipoid, Germany. SO was obtained from BDH
Chemical Ltd., Poole England. GMO was a gift from Croda International.
All water used was ultrapure Milli-Q water. Methanol and acetonitrile
were HPLC grade (VWR, UK), and ammonium acetate was obtained from
Merck, Germany.
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