Solubilization of poorly water soluble drugs in micelles of hydrophobically modified hydroxypropylcellulose copolymers

Francis, Mira; Piredda, Mariella; Winnik, Françoise M.

doi:10.1016/j.jconrel.2003.08.001

Cited by 98 publications

(70 citation statements)

References 31 publications

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“…It is known that one important role of surfactants is their ability to solubilize or emulsify hydrophobic compounds in water by forming micelles above their CMC 20,21 . This implies that amphiphilic peptides may also emulsify hydrophobic compounds, especially above their CAC.…”

Section: Emulsifying Properties Of Peptidesmentioning

confidence: 99%

Interfacial and Emulsifying Properties of Soybean Peptides with Different Degrees of Hydrolysis

et al. 2015

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Section: Emulsifying Properties Of Peptidesmentioning

confidence: 99%

Interfacial and Emulsifying Properties of Soybean Peptides with Different Degrees of Hydrolysis

et al. 2015

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“…23,24 Due to its high hydrophobicity and poor aqueous solubility, CyA cannot be formulated into the common aqueous formulations, leading to a low absorption and bioavailability. 25 To overcome these obstacles, various ophthalmic formulations have been developed to enhance CyA solubility and bioavailability. 26 So far, only one ophthalmic emulsion, RESTASIS ® (Allergan Inc, Irvine, CA, USA) has been approved by the US Food and Drug Administration for human use.…”

Section: Introductionmentioning

confidence: 99%

Enhanced and sustained topical ocular delivery of cyclosporine A in thermosensitive hyaluronic acid-based in situ forming microgels

Wu¹,

Yao²,

Zhou³

et al. 2013

IJN

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“…However, the effective drug delivery through oral route still remains a major challenge for highly lipophilic drugs in the pharmaceutical field owing to their poor bioavailability [1]. Prerequisite for effective oral drug delivery is the dissolution of pharmaceutical drug formulation in the gastro-intestinal lumen.…”

Section: Introductionmentioning

confidence: 99%

Enhancement of Bioavailability of Fenofibrate with Alpha Tocopherol and Phospholipids as Solubilizers

Indira¹

2012

JBB

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The purpose of this study was to investigate the effect of different solubilizers namely alpha tocopherol, soy phosphatidylcholine 70, Phospholipon 80H, and Phospholipon 90H on the bioavailability of sustained release fenofibrate pellets using fluid bed coating by applying Taguchi design to optimize the type and concentration of solubilizer at four levels namely 0.5%, 1%, 1.5%, and 2%. The pellets were prepared by loading the fenofibrate blended with other excipients onto the core sugar pellets with the aid of the binder solution. Taguchi experimental runs with alpha tocopherol 1% and Phospholipon 90H 2% (test) showed significant differences in in vitro dissolution behavior of drug compared to the pure drug. The pharmacokinetics of pure drug and test was evaluated in healthy male Wistar rats and found that t 1/2 was reduced significantly (4.36 and 4.02 hours) while AUC 0-t (32.14 ± 6.38 μg h/ml, 36.94 ± 6.2 μg h/ml), C max (8.7 ± 2.31 μg/ml, 9.8 ± 2.2 μg/ml) were improved markedly compared to the pure drug with t 1/2 (7.339314 ± 3.1 hours), AUC 0-t (11.89 ± 8.13 μg h/ml), and C max (5.137 ± 3.37 μg/ml). The extent of the mean plasma exposure of fenofibrate was 2.7 and 3.1 fold higher in animals treated with test. The ANOVA results revealed that type and concentration of solubilizer are crucial for enhancement of in vitro dissolution profile. Hence use of solubilizers may be the promising way to improve the oral bioavailability of fenofibrate. Enhancement of Bioavailability of MethodsDrug loading: Drug was loaded onto sugar spheres using fluidized bed processor . The sugar spheres were loaded into the fluidized bed processor and warmed for about 10 -15 minutes. Binder solution was prepared by dissolving Povidone K30 and sugar in purified water under constant stirring. Unmicronized fenofibrate which was pre blended and pulverized (0.5 mm screen pulverizer) with other excipients was incorporated intermittently into the solution under constant stirring. The obtained solution was loaded onto the circulating sugar spheres (800 μm). The wet spheres were dried simultaneously during the process of circulation in wurster chamber. The process was continued till the complete solution was consumed. The various processing variables namely inlet air temperature (40-45°C), outlet air temperature (30-33°C), product temperature (36-40°C), chamber humidity (58-60%), air flow (85 m 3 /hr), compressed air pressure (1.5-3.0 kg/cm 2 )The peristaltic pump rpm (10-35) and spray rate (2 ml/min) were optimized in the preliminary trials.Design of experiment to optimize drug loaded fenofibrate pellets: Taguchi L16 design of experiment was used to study the effect of two variables namely, type of solubilizer and concentration of solubilizer at four different levels as given in Table 1 and Table 2. All the experimental runs were analyzed using Minitab statistical software package (version 15). Characterization methodsInfrared Spectroscopy analysis of drug and excipients: FT-IR spectra were obtained using FT-IR spectrometer (Model Nic...

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Solubilization of poorly water soluble drugs in micelles of hydrophobically modified hydroxypropylcellulose copolymers

Cited by 98 publications

References 31 publications

Interfacial and Emulsifying Properties of Soybean Peptides with Different Degrees of Hydrolysis

Interfacial and Emulsifying Properties of Soybean Peptides with Different Degrees of Hydrolysis

Enhanced and sustained topical ocular delivery of cyclosporine A in thermosensitive hyaluronic acid-based in situ forming microgels

Enhancement of Bioavailability of Fenofibrate with Alpha Tocopherol and Phospholipids as Solubilizers

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