Effects of non-ionic surfactants as permeation enhancers towards piroxicam from the poloxamer gel through rat skins

Shin, Sang‐Chul; Cho, Cheong-Weon; Oh, In-Joon

doi:10.1016/s0378-5173(01)00699-8

Cited by 87 publications

(51 citation statements)

References 8 publications

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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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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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“…Percutaneous administration of piroxicam gel containing polyoxyethylene-2-oleyl ether to rats showed relatively constant, sustained blood concentration with minimal fluctuation [11]. The enhancing effect of non-ionic surfactants on the permeation of piroxicam from the poloxamer gels was evaluated in another study by Shin et al [15]. The effectiveness of penetration enhancers, measured by ratio of piroxicam flux in the presence or absence of enhancers (enhancement factor) indicate that polyoxyethylene-2-oleyl ether showed the highest enhancing effects (Figure 3) with an enhancement factor of 2.84 among the studied surfactants.…”

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

confidence: 99%

“…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%

“…Various hydrogel formulations loaded with poorly water-soluble piroxicam for transdermal delivery has been investigated by some researchers [11,12,15]. The pharmacokinetics and anti-inflammatory activity of piroxicam from Poloxamer 407 gel were determined to investigate percutaneous absorption of piroxicam from poloxamer gels in rats; Poloxamer 407 gel containing 1 % piroxicam showed significant inhibition of carragenin-induced rat foot swelling (%) with a linear relationship of piroxicam dose within ~0.4 -3.2 mg/kg when compared to the control group (Figure 1).…”

Section: Delivery Of Small Moleculesmentioning

confidence: 99%

“…The effectiveness of penetration enhancers, measured by ratio of piroxicam flux in the presence or absence of enhancers (enhancement factor) indicate that polyoxyethylene-2-oleyl ether showed the highest enhancing effects (Figure 3) with an enhancement factor of 2.84 among the studied surfactants. Thermal analysis revealed that various surfactants have different fluidizing effects on stratum corneum, and skin pretreated with the Poloxamer 407 gels containing various surfactants showed a loosely layered stratum corneum and wide intercellular space that elucidated the mechanisms of the action of enhancers [15].…”

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

confidence: 99%

See 2 more Smart Citations

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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Photophysical properties of anti‐inflammatory piroxicam and its Cu(II) complex

Choi

Ahn

Wee

et al. 2021

Bulletin Korean Chem Soc

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Piroxicam (PRX), a nonsteroidal anti-inflammatory drug, exhibits a large Stokesshift emission owing to the excited-state intramolecular proton transfer (ESIPT) from enol-PRX to keto-PRX. In contrast, the Cu-coordinated PRX complex (CuPRX) does not show any emission at 300 K. In the time-resolved transient absorption (TA) spectra, PRX showed two positive TA bands at 430 and 700 nm, corresponding to the S 1 -S n transitions of keto-PRX * and a negative bleaching band at 540 nm due to ESIPT emission. These TA bands decayed with a lifetime of approximately 50 ps. CuPRX showed similar TA features, but no bleaching band was observed for CuPRX and decayed rapidly within 3 ps, indicating a rapid intersystem crossing process owing to the heavy atom effect. Based on the experimental results and theoretical calculations, the fate for excited keto-PRX is discussed in terms of the ESIPT and reverse ESIPT processes.

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Effects of non-ionic surfactants as permeation enhancers towards piroxicam from the poloxamer gel through rat skins

Cited by 87 publications

References 8 publications

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

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

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

Photophysical properties of anti‐inflammatory piroxicam and its Cu(II) complex

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