Intra-articular drug delivery from an optimized topical patch containing teriflunomide and lornoxicam for rheumatoid arthritis treatment: Does the topical patch really enhance a local treatment?

Xi, Honglei; Cun, Dongmei; Xiang, Rongwu; Yan-li, Guan; Zhang, Yuxiu; Li, Yuanru; Fang, Liang

doi:10.1016/j.jconrel.2013.03.028

Cited by 53 publications

(19 citation statements)

References 24 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…A similar result was received with ibuprofen (Dominkus et al, 1996). Recently, our group also confirmed that the transdermal patches applied topically exerted a RA therapeutic activity by drug delivery via systemic circulation (Xi et al, 2013).…”

Section: Assessment Of Anti-inflammatory Activitymentioning

confidence: 56%

See 1 more Smart Citation

The effect of ion-pair formation combined with penetration enhancers on the skin permeation of loxoprofen

et al. 2014

Self Cite

View full text Add to dashboard Cite

Context: Loxoprofen (LOXO) is a non-steroidal anti-inflammatory drug. Repeated oral administrations induce gastrointestinal side effects. Patches are a promising alternative. Objective: The aim of this study was to investigate the effects of organic amines on the skin permeation of LOXO and finally design a patch with a comparable permeation profile and pharmacodynamic effects to the commercial LOXONA Õ plaster. Materials and methods: The effects of organic amines were assessed by flux values of LOXO from isopropyl myristate (IPM), using horizontal diffusion cell and rabbit skin. FTIR spectroscopy was used to confirm ion-pair formation. Anti-inflammatory and analgesic activity assessments were performed in the adjuvant arthritis rat model and acetic acid-induced writhing syndrome in mouse, separately. Results and discussion: Results showed that triethylamine (TEA) was the most potential candidate in IPM, with the highest flux of 499.75 ± 32.40 mg/cm 2 /h. In patch, the highest flux of 369.37 ± 34.32 mg/cm 2 /h was still obtained by LOXO-TEA. Combined with penetration enhancers, the cumulative amounts were further increased in presence of 5% IPM, which exhibited a flux of 840.04 ± 66.38 mg/cm 2 /h as two times of the commercial one. Ultimately, anti-inflammatory and analgesic activity assessment presented that a comparable pharmacodynamic activity with the commercial one could be obtained by the patch we designed. Additionally, we also found that LOXO patch applied topically exerted a systemic effect, and the effect was dose-dependent. Conclusion: It was feasible for LOXO patch design by combination of ion-pair technology and chemical enhancers.

show abstract

Section: Assessment Of Anti-inflammatory Activitymentioning

confidence: 56%

“…The procedure of anti-inflammatory activity assessment was based on Xi et al (2013). Wistar rats were divided into four groups each consisting of six animals.…”

Section: Assessment Of Anti-inflammatory Activitymentioning

confidence: 99%

The effect of ion-pair formation combined with penetration enhancers on the skin permeation of loxoprofen

et al. 2014

Self Cite

View full text Add to dashboard Cite

show abstract

“…The analgesic effect of the patches was evaluated by means of acetic acid-induced writhing response in mice (Xi et al, 2013). Forty KM mice were randomly divided into four groups, which were blank group, negative group, positive group and test group, respectively.…”

Section: Analgesic Effect Assessmentmentioning

confidence: 99%

“…Unlike prodrugs, ion pairs act with no changes on drug structure and pharmacologic action, thus are independent of enzymatic conversion into active parent compounds (Cheong & Choi, 2002;Xi et al, 2012). The ion-pair strategy has been used to facilitate skin permeation of a number of ionizable drugs (Ma et al, 2010;Xi et al, 2013;Pawar et al, 2015), and diclofenac diethylamine in a topical gel is already available in market. The formation of ion pairs can be described by the '' represents the hydrogen-bonded ion pairs.…”

Section: Introductionmentioning

confidence: 99%

Development of a drug-in-adhesive patch combining ion pair and chemical enhancer strategy for transdermal delivery of zaltoprofen: pharmacokinetic, pharmacodynamic and in vitro/in vivo correlation evaluation

et al. 2016

Self Cite

View full text Add to dashboard Cite

The aim of the study was to develop a drug-in-adhesive patch system for transdermal delivery of zaltoprofen (ZAL). The formulation was designed in combination with the ion pair and chemical enhancer strategy. Seven organic amines were chosen as counter ions, and the prepared ion pairs were characterized by Fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). The in vivo pharmacokinetic performance of ZAL was studied on rabbits following transdermal and intravenous administration. A deconvolution method was applied to determine the correlation between the in vitro permeation and the in vivo absorption. Acetic acid-induced writhing response was conducted on mice to evaluate the analgesic effect. In vitro permeation results showed that both ion pairs and chemical enhancers were effective in modulating ZAL skin permeation from patches. The enhancement ratio was negatively correlated to the polar surface area (PSA) of counter ions, and was positively correlated to the octanol-water partition coefficient (log K o/w ) of chemical enhancers, respectively. The optimized formulation contained 10% (w/w) ZAL-triethylamine and 10% (w/w) isopropyl myristate, with DURO-TAK Õ 87-4098 as the pressure sensitive adhesive matrix. Furthermore, the in vitro permeation data were well correlated with the in vivo absorption data. The analgesic effect of the optimized patch was comparable to the commercial indometacin plasters. In conclusion, it was feasible for transdermal delivery of ZAL by the synergistic action of ion pair and chemical enhancer, and the in vitro permeation data were indicative of the in vivo performance for the developed patches. KeywordsIon pair, in vitro/in vivo correlation, pharmacokinetic, transdermal, zaltoprofen History

show abstract

“…The process of rabbit skin preparation was carried out according to our previous report (11). Full thickness skin (including the SC, epidermis, and dermis) was excised from the abdominal area and stored at −70°C prior to further experiments (used within 1 month after preparation).…”

Section: In Vitro Skin Permeability Studymentioning

confidence: 99%

Lamellar Liquid Crystal Improves the Skin Retention of 3-O-Ethyl-Ascorbic Acid and Potassium 4-Methoxysalicylate In Vitro and In Vivo for Topical Preparation

Dong

Cun

et al. 2015

AAPS PharmSciTech

Self Cite

View full text Add to dashboard Cite

Abstract. The study aimed at increasing the skin retention of 3-O-ethyl-ascorbic acid (EA) and potassium 4-methoxysalicylate (4-MSK) via topical administration for effective skin-whitening. To achieve this goal, EA and 4-MSK were formulated into lamellar liquid crystalline (LLC) cream, and response surface methodology (RSM) was employed to optimize the formulation. Polarized light microscopy (PLM), differential scanning calorimetry (DSC), and rheological experiments were performed to confirm the presence of the LLC structure in the base of cream. In addition, a comparison analysis of the skin retention of the two drugs between the LLC cream and the common o/w (COW) cream was made through in vitro permeation and in vivo drug distribution experiments. As a result, the optimal formulation was defined as 1.2% of EA, 1.48% of 4-MSK, 14.05% of Schercemol™ DISM Ester (DISM) as the oil, 4.0% of Emulium® Delta as the emulsifier, and 3.0% of stearyl alcohol as the co-emulsifier. In comparison with the COW cream, the LLC cream significantly increased the skin retention of EA and 4-MSK both in vitro and in vivo. In conclusion, the LLC carrier serves as a promising choice for topical preparation by enhancing skin retention and providing desirable rheological characteristics.

show abstract

Intra-articular drug delivery from an optimized topical patch containing teriflunomide and lornoxicam for rheumatoid arthritis treatment: Does the topical patch really enhance a local treatment?

Cited by 53 publications

References 24 publications

The effect of ion-pair formation combined with penetration enhancers on the skin permeation of loxoprofen

The effect of ion-pair formation combined with penetration enhancers on the skin permeation of loxoprofen

Development of a drug-in-adhesive patch combining ion pair and chemical enhancer strategy for transdermal delivery of zaltoprofen: pharmacokinetic, pharmacodynamic and in vitro/in vivo correlation evaluation

Lamellar Liquid Crystal Improves the Skin Retention of 3-O-Ethyl-Ascorbic Acid and Potassium 4-Methoxysalicylate In Vitro and In Vivo for Topical Preparation

Contact Info

Product

Resources

About