Percutaneous absorption of non-steroidal anti-inflammatory drugs from in situ gelling xyloglucan formulations in rats

Takahashi, Akie; Suzuki, Satoru; Kawasaki, Naoko; Kubo, Wataru; Miyazaki, Shôzo; Löebenberg, Raimar; Bachynsky, John; Attwood, David

doi:10.1016/s0378-5173(02)00394-0

Cited by 59 publications

(22 citation statements)

References 24 publications

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“…Isopropyl myristate presents high solvent action for poorly hydrosoluble drug and immiscibility with b. Models with a membrane Such models have been fully published and involve injectable or topical formulations in which the gel is not expected to be quickly dissolved in physiological fluids (15,71,72,75,76,84,87) but have also been proposed for liquid suppositories (semi-permeable tube containing the liquid suppository secured with a thread and placed in the dissolution medium) (51,69,85). In this model, a membrane, which is permeable to the drug isolates both media (i.e., formulation and receptor medium, respectively) and thus Evaluation of enhancers presents the advantage of avoiding direct dissolution of Poloxamer 407 in the receptor medium.…”

Section: Membranementioning

confidence: 99%

“…Semi-permeable inert cellulose (or cellulose acetate) membrane allows drug release in the receptor medium without any diffusion of poloxamer by means of an appropriate molecular weight cut-off (õ6,000 Y 8,000) (51). The cumulative amount of drug released per unit area generally approaches the Higuchi square root equation, especially when the quantity released does not exceed 50 Y 60% (72,83). Nevertheless, this model efficiency highly depends on whether or not additives are present, because these one have been held responsible for significant alteration.…”

Section: Membranementioning

confidence: 99%

“…Predictive interest of in vitro release has been retrieved with ibuprofen and ketoprofen (72). These authors compared a 25% Poloxamer 407 gel containing nonsteroidal anti-inflammatory drugs with a xyloglycan thermoreversible gel.…”

Section: Membranementioning

confidence: 99%

“…Most of the time, these preparations included a thickening agent like carbopol or cellulose derivatives (70,72,93,101,102). Despite solubilisation enhancement of Poloxamer 407 by means of micelle formation, a nonaqueous solvent like ethanol may be added to formulate a topical preparation with insoluble drugs like ketoprofen (insolubility at a concentration greater than 3%) (61).…”

Section: Topical Formulationmentioning

confidence: 99%

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A Review of Poloxamer 407 Pharmaceutical and Pharmacological Characteristics

et al. 2006

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Poloxamer 407 copolymer (ethylene oxide and propylene oxide blocks) shows thermoreversible properties, which is of the utmost interest in optimising drug formulation (fluid state at room temperature facilitating administration and gel state above sol-gel transition temperature at body temperature promoting prolonged release of pharmacological agents). Pharmaceutical evaluation consists in determining the rheological behaviour (flow curve or oscillatory studies), sol-gel transition temperature, in vitro drug release using either synthetic or physiological membrane and (bio)adhesion characteristics. Poloxamer 407 formulations led to enhanced solubilisation of poorly water-soluble drugs and prolonged release profile for many galenic applications (e.g., oral, rectal, topical, ophthalmic, nasal and injectable preparations) but did not clearly show any relevant advantages when used alone. Combination with other excipients like Poloxamer 188 or mucoadhesive polymers promotes Poloxamer 407 action by optimising sol-gel transition temperature or increasing bioadhesive properties. Inclusion of liposomes or micro(nano)particles in Poloxamer 407 formulations offers interesting prospects, as well. Besides these promising data, Poloxamer 407 has been held responsible for lipidic profile alteration and possible renal toxicity, which compromises its development for parenteral applications. In addition, new findings have demonstrated immuno-modulation and cytotoxicity-promoting properties of Poloxamer 407 revealing significant pharmacological interest and, hence, human trials are in progress to specify these potential applications.

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Section: Membranementioning

confidence: 99%

Section: Membranementioning

confidence: 99%

Section: Membranementioning

confidence: 99%

Section: Topical Formulationmentioning

confidence: 99%

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A Review of Poloxamer 407 Pharmaceutical and Pharmacological Characteristics

et al. 2006

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“…Other investigators, using photon correlation spectroscopy, have also reported a pronounced decrease in diffusion coefficient of a compound as the concentration of poloxamer 407 as gelling agent exceeded 10%. It was interpreted that these changes in diffusion coefficient were due to marked increase of mean micellar size and the polydispersity of the micelles (18,37).…”

Section: In Vitro Diffusion Through Cellulose Membranementioning

confidence: 99%

Evaluation of Glycofurol-Based Gel as a New Vehicle for Topical Application of Naproxen

Barakat

2010

AAPS PharmSciTech

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Abstract. In view of the good skin tolerability, glycofurol was used as a vehicle-based gel, and its effect in the topical penetration of Naproxen (NAP) was investigated. The aims of this study were to develop a suitable gel with bioadhesive property, spreadability, and viscosity for topical anti-inflammatory effect. Three gelling and adhesive agents were examined: Carbopol 974P, Gantrez AN 119, and polyvinylpyrollidone K30. Skin permeation rates and lag times of NAP were evaluated using the Franz-type diffusion cell in order to optimize the gel formulation. The permeation rate of NAP-based gel across the excised rat skin was investigated. A significant increase in permeability parameters such as steady-state flux (J ss ), permeability coefficient (K p ), and penetration index (PI) was observed in optimized formulation containing 2% Transcutol as an permeation enhancer. From skin irritation test, it was concluded that the optimized novel glycofurol-based gel formulation was safe to be used for topical drug delivery. The developed glycofurol-based gel appeared promising for dermal and transdermal delivery of naproxen and could be applicable with water-insoluble drugs, which would circumvent most of the problems associated with drug therapy.

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