In Vivo Skin Permeation of Sodium Naproxen Formulated in Pluronic F-127 Gels: Effect of Azone® and Transcutol®

Escobar-Chávez, José Juan; Quintanar‐Guerrero, David; Ganem-Rondero, Adriana

doi:10.1080/03639040500214662

Cited by 50 publications

(30 citation statements)

References 28 publications

(30 reference statements)

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“…It was found that the combination of Azone and Transcutol in Pluronic F127 gels enhanced sodium naproxen penetration, with enhancement ratios of up to two-fold compared with the formulation containing only Transcutol. This was confirmed by transepidermal water loss and attattentuated total reflectance FTIR spectroscopy analyses by Escobar-Chavez et al [16].…”

Section: Effect Of Additives On the Delivery Of Small Molecules From supporting

confidence: 53%

“…Studies on PEO-PPO-based polymeric micelles for transdermal drug delivery have been widely carried out with Poloxamer 407 (Pluronic F127) and these studies mostly focused on small drug molecules in order of anti-inflammatory [8][9][10][11][12][13][14][15][16][17][18][19], analgesic [20], local anesthetic [21] and cardiac effectiveness [19,[22][23][24] and rarely focused on big molecules such as arginine vasopressin (AVP) and insulin [25,26].…”

Section: Peo-ppo Based Copolymers In Transdermal Drug Deliverymentioning

confidence: 99%

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Poly(ethylene oxide)–Poly(propylene oxide)-Based Copolymers for Transdermal Drug Delivery: An Overview

Yapar¹,

Ýnal²

2013

Trop. J. Pharm Res

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Section: Effect Of Additives On the Delivery Of Small Molecules From supporting

confidence: 53%

Section: Peo-ppo Based Copolymers In Transdermal Drug Deliverymentioning

confidence: 99%

Poly(ethylene oxide)–Poly(propylene oxide)-Based Copolymers for Transdermal Drug Delivery: An Overview

Yapar¹,

Ýnal²

2013

Trop. J. Pharm Res

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“…Poloxamers has been used as a delivery system of many drugs for ophthalmic (18,19), rectal (20,21), parenteral (22,23), topical (24), and transdermal (25,26) applications. Recently, PF-127 gel has been explored as a skin delivery system to several NSAIDs as naproxen (27), indometacin (28), piroxicam (26), diclofenac (29), among others, due to higher drug retention at the action site which leads to a sustained drug release and improved therapeutic efficiency.…”

Section: Introductionmentioning

confidence: 99%

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

2010

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Abstract. Transdermal delivery of non-steroidal anti-inflammatory drugs may be an interesting strategy for delivering these drugs to the diseased site, but it would be ineffective due to low skin permeability. We investigated whether oleic acid (OA), a lipid penetration enhancer in poloxamer gels named poloxamer-based delivery systems (PBDS), can improve lumiracoxib (LM) delivery to/through the skin. The LM partition coefficient (K) studies were carried out in order to evaluate the drug lipophilicity grade (K octanol/buffer ), showing values >1 which demonstrated its high lipophilicity. Both in vitro percutaneous absorption and skin retention studies of LM were measured in the presence or absence of OA (in different concentrations) in PBDS using porcine ear skin. The flux of in vitro percutaneous absorption and in vitro retention of LM in viable epidermis increased in the presence of 10.0% (w/w) OA in 25.0% (w/w) poloxamer gel. In vivo cutaneous irritation potential was carried out in rabbits showing that this formulation did not provide primary or cumulative cutaneous irritability in animal model. The results showed that 25.0% poloxamer gel containing 10.0% OA is potential transdermal delivery system for LM.KEY WORDS: in vitro skin permeation; lumiracoxib; oleic acid; poloxamer-based delivery systems; skin delivery.

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“…In addition, PF -127 water-based polymeric gels offer several other advantages over traditional bases in terms of ease of application, cosmetic acceptability (colorless and water-washable), good physicochemical stability and desirable drug release characteristics (25). PBDSs have been suggested as potential drug delivery systems for transdermal application of many antinflammatory drugs (26)(27) including naproxen, (28) indomethacin, (19,29) piroxicam (20) and diclofenac (30) due to higher drug retention at the site of action, sustained release and improved therapeutic effectiveness. This means that transdermal PBDSs may provide comparable antiinflammatory and analgesic activities to oral formulations while significantly reducing systemic side effects and gastrointestinal irritation associated with oral administration (26).…”

Section: Introductionmentioning

confidence: 99%

Influence of Oleic Acid on the Rheology and in Vitro Release of Lumiracoxib from Poloxamer Gels

2010

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-Purpose. Transdermal delivery of anti-inflammatory lumiracoxib (LM) could be an interesting strategy to avoid the side effects associated with systemic delivery, but it is ineffective due to the drug poor skin penetration. We have investigated the effects of oleic acid (OA), a lipid penetration enhancer, on the in vitro release of LM from poloxamer-based delivery systems (PBDS). The rheological behavior (shear rate dependent viscosity) and gelation temperature through measurements of optimal sol-gel transition temperatures (T sol-gel ) were also carried out in these systems. Methods. In vitro release studies of LM from PBDS were performed using cellulose acetate as artificial membrane mounted in a diffusion system. The amount of LM released was divided by exposition area (µg/cm 2 ) and these values were plotted as function of the time (h). The flux of the drug across the membrane (J) was calculated from the slope of the linear portion of the plot and expressed as µg/cm 2 /h. The determination of viscosity was carried out at different shear rates (γ) between 0.1-1000 S -1 using a parallel plate rheometer. Oscillatory measurements using a cone-plate geometry rheometer surrounded by a double jacket with temperature varying 4-40°C, was used in order to determine T sol-gel . Results. Increase of both polymer and OA concentrations increases the viscosity of the gels and consequently reduces the in vitro LM release from the PBDS, mainly for gels containing OA at 10.0% (w/w) compared to other concentrations of the penetration enhancer. T sol-gel transition temperature was decreased by increasing viscosity; in some cases the formulation was already a gel at room temperature. Rheological studies showed a pseudoplastic behavior, which facilitates the flow and improves the spreading characteristics of the formulations. Conclusions. Taken together, the results showed that poloxamer gels are good potential delivery systems for LM, leading to a sustained release, and also have appropriate rheological characteristics.

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In Vivo Skin Permeation of Sodium Naproxen Formulated in Pluronic F-127 Gels: Effect of Azone® and Transcutol®

Cited by 50 publications

References 28 publications

Poly(ethylene oxide)–Poly(propylene oxide)-Based Copolymers for Transdermal Drug Delivery: An Overview

Poly(ethylene oxide)–Poly(propylene oxide)-Based Copolymers for Transdermal Drug Delivery: An Overview

A Novel Transdermal Delivery System for the Anti-Inflammatory Lumiracoxib: Influence of Oleic Acid on In Vitro Percutaneous Absorption and In Vivo Potential Cutaneous Irritation

Influence of Oleic Acid on the Rheology and in Vitro Release of Lumiracoxib from Poloxamer Gels

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