In Vitro and In Vivo Evaluation of DMSO and Azone as Penetration Enhancers for Cutaneous Application of Celecoxib

Senna, Thassia D`Arc; Santos, Hílton Antônio Mata dos; Kibwila, Daniel Mabundu; Leitão, Álvaro C.; Pyrrho, Alexandre dos Santos; Pádula, Marcelo de; Rosas, Elaine Cruz; Pádua, Tatiana Almeida; Lara, Marilisa Guimarães; Pierre, Maria Bernadete Riemma

doi:10.2174/1567201814666170125120331

Cited by 6 publications

(4 citation statements)

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“…The anti‐inflammatory effect of the formulations was assessed in the AA‐induced ear oedema mice model, that is in agreement with those recommended in the literature for anti‐inflammatory drugs with topical or transdermal effects …”

Section: Methodssupporting

confidence: 76%

“…The anti-inflammatory effect of the formulations was assessed in the AA-induced ear oedema mice model, that is in agreement with those recommended in the literature for anti-inflammatory drugs with topical or transdermal effects. [30,33,34] The anti-inflammatory activity of the formulation containing C.O that provided the best in vitro Cxb retention was assessed using the AA-induced ear oedema mice model. Briefly, male Swiss mice-44 were divided into six groups (n = 6 animals/group) and treated with the following formulations: group Iuntreated animals; group IIreference treatment with 11.6 mg/g diethylammonium diclofenac in cream gel (commercial product); group IIIformulation vehicle (PEG-400/PG); group IV -25% C.O in PEG-400/PG; group V -2% Cxb in PEG-400/PG (control formulation F1); and group VI -2% Cxb associated with 25% C.O in PEG-400/PG (formulation F4).…”

Section: Neovascularizationmentioning

confidence: 99%

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Copaiba oil enhances in vitro/in vivo cutaneous permeability and in vivo anti-inflammatory effect of celecoxib

Quiñones

Hossy

Pádua

et al. 2018

Journal of Pharmacy and Pharmacology

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Section: Methodssupporting

confidence: 76%

Section: Neovascularizationmentioning

confidence: 99%

Copaiba oil enhances in vitro/in vivo cutaneous permeability and in vivo anti-inflammatory effect of celecoxib

Quiñones

Hossy

Pádua

et al. 2018

Journal of Pharmacy and Pharmacology

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“…Likewise, oral bioavailability of ETF-5 was improved 1.7 times, in comparison with plain film. The increase in the oral absorption rate might be linked to the deformability of transfersomes in films [ 68 ]. The small size of transfersomes increases the surface of drug molecules, subsequently maintaining the surface area in oral film.…”

Section: Discussionmentioning

confidence: 99%

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

et al. 2021

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The main objective of this research work was the development and evaluation of transfersomes integrated oral films for the bioavailability enhancement of Ebastine (EBT) to treat allergic rhinitis. The flexible transfersomes, consisting of drug (EBT), lipid (Phosphatidylcholine) and edge activator (EA) Polyoxyethylene sorbitan monooleate or Sorbitan monolaurate, were prepared with the conventional thin film hydration method. The developed transfersomes were further integrated into oral films using the solvent casting method. Transfersomes were evaluated for their size distribution, surface charge, entrapment efficiency (EE%) and relative deformability, whereas the formulated oral films were characterized for weight, thickness, pH, folding endurance, tensile strength, % of elongation, degree of crystallinity, water content, content uniformity, in vitro drug release and ex vivo permeation, as well as in vivo pharmacokinetic and pharmacodynamics profile. The mean hydrodynamic diameter of transfersomes was detected to be 75.87 ± 0.55 nm with an average PDI and zeta potential of 0.089 ± 0.01 and 33.5 ± 0.39 mV, respectively. The highest deformability of transfersomes of 18.52 mg/s was observed in the VS-3 formulation. The average entrapment efficiency of the transfersomes was about 95.15 ± 1.4%. Transfersomal oral films were found smooth with an average weight, thickness and tensile strength of 174.72 ± 2.3 mg, 0.313 ± 0.03 mm and 36.4 ± 1.1 MPa, respectively. The folding endurance, pH and elongation were found 132 ± 1, 6.8 ± 0.2 and 10.03 ± 0.4%, respectively. The ex vivo permeability of EBT from formulation ETF-5 was found to be approximately 2.86 folds higher than the pure drug and 1.81 folds higher than plain film (i.e., without loaded transfersomes). The relative oral bioavailability of ETF-5 was 2.95- and 1.7-fold higher than that of EBT-suspension and plain film, respectively. In addition, ETF-5 suppressed the wheal and flare completely within 24 h. Based on the physicochemical considerations, as well as in vitro and in vivo characterizations, it is concluded that the highly flexible transfersomal oral films (TOFs) effectively improved the bioavailability and antihistamine activity of EBT.

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“…DMSO has been used extensively to enhance the permeation of many classes of drugs and is included in numerous FDA-approved products, including a diclofenac sodium topical solution (Pennsaid ® ) [49]. In addition, the transdermal permeation of celecoxib through pig skin was enhanced using 5% and 10% DMSO formulations [50]. However, when used at high concentrations, DMSO has the potential to cause skin irritation and potential damage, leading to other sulfoxides, such as decyl methyl sulfoxide (DCMS), being developed [47] Laurocapram (Azone ® ) Laurocapram (Azone ® ), a chemical hybrid of an amide and sulfoxide, was the first agent specifically designed for transdermal penetration enhancement [51].…”

Section: Sulfoxidesmentioning

confidence: 99%

Strategies to Improve the Transdermal Delivery of Poorly Water-Soluble Non-Steroidal Anti-Inflammatory Drugs

Balmanno,

Falconer,

Ravuri

et al. 2024

Pharmaceutics

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The transdermal delivery of non-steroidal anti-inflammatory drugs (NSAIDs) has the potential to overcome some of the major disadvantages relating to oral NSAID usage, such as gastrointestinal adverse events and compliance. However, the poor solubility of many of the newer NSAIDs creates challenges in incorporating the drugs into formulations suitable for application to skin and may limit transdermal permeation, particularly if the goal is therapeutic systemic drug concentrations. This review is an overview of the various strategies used to increase the solubility of poorly soluble NSAIDs and enhance their permeation through skin, such as the modification of the vehicle, the modification of or bypassing the barrier function of the skin, and using advanced nano-sized formulations. Furthermore, the simple yet highly versatile microemulsion system has been found to be a cost-effective and highly successful technology to deliver poorly water-soluble NSAIDs.

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In Vitro and In Vivo Evaluation of DMSO and Azone as Penetration Enhancers for Cutaneous Application of Celecoxib

Cited by 6 publications

References 0 publications

Copaiba oil enhances in vitro/in vivo cutaneous permeability and in vivo anti-inflammatory effect of celecoxib

Copaiba oil enhances in vitro/in vivo cutaneous permeability and in vivo anti-inflammatory effect of celecoxib

Improved Bioavailability of Ebastine through Development of Transfersomal Oral Films

Strategies to Improve the Transdermal Delivery of Poorly Water-Soluble Non-Steroidal Anti-Inflammatory Drugs

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