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

Moreira, Tailane Sant’Anna; Sousa, Valéria Pereira de; Pierre, Maria Bernadete Riemma

doi:10.1208/s12249-010-9420-1

Cited by 38 publications

(18 citation statements)

References 60 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…This behavior is important for a transdermal delivery system, in order to avoid peak in the plasma concentrations with generation of systemic side effects and to reduce administration frequency, and in return a better patient compliance. As mentioned previously, the PBDS containing 25.0% of poloxamer gel and 10.0% OA also showed the highest LM flux through porcine skin and the highest LM retention for in vitro permeability studies and no cutaneous irritability (11).…”

Section: Discussionsupporting

confidence: 72%

“…The diffusion system employed in the in vitro release studies was mounted on a dissolution test apparatus as previously described in details in a recent paper of our research group (11). It is constituted by a glass water bath (maintained at 37 °C) mounted on a six points stirring plate.…”

Section: In Vitro Release Studiesmentioning

confidence: 99%

“…Since gelation is reversible, removal is facilitated by immersion in, or irrigation with cold water (12). The gel allows a 'depot-like' sustained release that has been applied in drug delivery systems for ophthalmic, (15)(16) rectal (17)(18) transdermal (11,(19)(20) parenteral (21)(22)(23) and topical (24) applications. 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).…”

Section: Introductionmentioning

confidence: 99%

See 2 more Smart Citations

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

2010

Self Cite

View full text Add to dashboard Cite

-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.

show abstract

Section: Discussionsupporting

confidence: 72%

Section: In Vitro Release Studiesmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

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

2010

Self Cite

View full text Add to dashboard Cite

show abstract

“…Application of NSAIDs through percutaneous route can also lead to increase in drug concentration in the local soft tissue and joints while reducing their distribution and systemic toxicity (3,4). Unfortunately, the bioavailability of topically applied NSAIDs is only 1-2% in humans due to the barriers posed by the skin constituents (3,(5)(6)(7).…”

Section: Introductionmentioning

confidence: 99%

Potential of Piperazinylalkylester Prodrugs of 6-Methoxy-2-Naphthylacetic Acid (6-MNA) for Percutaneous Drug Delivery

et al. 2014

View full text Add to dashboard Cite

Abstract. Piperazinylalkyl ester prodrugs (4a-5d) of 6-methoxy-2-naphthylacetic acid (6-MNA) (1) were synthesized and evaluated in vitro for the purpose of percutaneous drug delivery. These ionizable prodrugs exhibited varying aqueous solubilities and lipophilicities depending on the pH of the medium. The prodrugs (4a-5c) showed higher aqueous solubility and similar lipophilicity at pH 5.0 and lower aqueous solubility and higher lipophilicity at pH 7.4 in comparison to 6-MNA. The chemical and enzymatic hydrolyses of the prodrugs was investigated in aqueous buffer solutions (pH 5.0 and 7.4) and in 80% human serum (pH 7.4) at 37°C. The prodrugs showed moderate chemical stability (t 1/2 =6-60 h) but got readily hydrolyzed enzymatically to 6-MNA with half-life ranging from 10-60 min. In the in vitro permeation study using rat skin, the flux of 6-MNA and the prodrugs was determined in aqueous buffers of pH 5.0 and 7.4. The prodrug (5b) showed 7.9-and 11.2-fold enhancement in skin permeation compared to 6-MNA (1) at pH 5.0 and 7.4, respectively. It was concluded that the parent NSAIDs having favorable pharmacokinetic and pharmacodynamic properties coupled with increased skin permeability of their prodrugs could give better options for the treatment of rheumatic diseases.

show abstract

“…19,20 An acetate cellulose membrane was mounted on a diffusion system and a sample containing 200 mg of LID was introduced into the donor compartment. Sink conditions were met in all cases and 6 parallel determinations were performed at 37 ± 0.5°C.…”

Section: In Vitro Drug Release Analysismentioning

confidence: 99%

Preparation and evaluation of lidocaine hydrochloride in cyclodextrin inclusion complexes for development of stable gel in association with chlorhexidine gluconate for urogenital use

Silva

Carmo²,

Borges³

et al. 2011

IJN

View full text Add to dashboard Cite

Inclusions of lidocaine hydrochloride in cyclodextrins were prepared to obtain stable complexes compatible for association with chlorhexidine in a new gel formulation for use in urogenital applications. Two cyclodextrins, β-cyclodextrin and methyl-β-cyclodextrin, were used for encapsulating lidocaine hydrochloride through solubilization and kneading techniques. The lidocaine–cyclodextrin complexes were characterized by ultraviolet spectroscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and X-ray diffraction. The results revealed that the techniques generated good yields of inclusion products that maintained the functional properties of lidocaine. In addition, the inclusion products obtained improved the compatibility of lidocaine hydrochloride with chlorhexidine in solution and a gel formulation. The gel formulation displayed desirable rheological and physicochemical properties. The results presented here are the first description of the inclusion of lidocaine with cyclodextrins, which improves compatibility with chlorhexidine in formulations for simultaneous delivery.

show abstract

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

Cited by 38 publications

References 60 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

Potential of Piperazinylalkylester Prodrugs of 6-Methoxy-2-Naphthylacetic Acid (6-MNA) for Percutaneous Drug Delivery

Preparation and evaluation of lidocaine hydrochloride in cyclodextrin inclusion complexes for development of stable gel in association with chlorhexidine gluconate for urogenital use

Contact Info

Product

Resources

About