Design and Evaluation of a Novel Felbinac Transdermal Patch: Combining Ion-Pair and Chemical Enhancer Strategy

Liu, Nannan; Song, Wenting; Song, Tian; Fang, Liang

doi:10.1208/s12249-015-0342-9

Cited by 15 publications

(6 citation statements)

References 41 publications

(51 reference statements)

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“…In IR spectrum of clozapine, the absorption at 3296.71 cm −1 was assigned to the stretching vibration of N-H group which was red shifted to the wavenumber of 3289.24 cm −1 for clozapine formulation. [59] As reported in literature, red shift is attributable for the intermolecular hydrogen bonding, [60] the same has been observed in case of the matrix patch of clozapine.…”

Section: Ftir Studiessupporting

confidence: 68%

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Patel¹

2020

AJP

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Introduction: The present research work was intended to develop and optimize transdermal matrix patch of clozapine using Box-Behnken experimental design (Box-Behnken design [BBD]) for improved bioavailability as compared to oral formulation. The 3-factor, 3-level BBD was employed to investigate the combined influence of formulation variables on flux, tensile strength (TS), and in vitro drug release. The generated polynomial equation was validated and desirability function was utilized for optimization. Materials and Methods: Optimized formulation evaluated for physicochemical characterization, Fourier transform infrared, differential scanning calorimetry, in vitro drug release, permeability enhancement potential by ex vivo, skin irritation, and in vivo pharmacokinetics and stability studies. Results: The results of the optimized formulation (F 15) showed TS of 6.84 ± 0.64 MPa, flux of 104.80 ± 1.39 (µg/h/cm 2), and % drug release after 20 h (Q 20) of 82.19 ± 1.12% which was stable up to 6 months in accelerated condition. Observed and the predicted values of the responses were found to be in good agreement. Optimized transdermal patch of clozapine found free from skin irritation as per Draize score method. The pharmacokinetic result had shown the bioavailability of clozapine improved about 2.18-fold after transdermal drug delivery when compared with oral marketed formulation. Discussion and Conclusion: The results of the study revealed that the developed transdermal patch of clozapine can be a promising alternative which provides effective management of schizophrenia in terms of improved patient compliance.

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Section: Ftir Studiessupporting

confidence: 68%

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Patel¹

2020

AJP

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“…Ma et al and Tan et al also found that the flux of drug was influenced by the pK a of counter-ions (22,23). The apparent solubility of ion-pair in the donor phases was also an important factor affecting the permeation rate (24). The controlled flux of ESP ion-pair complexes was also due to the low solubility in IPP.…”

Section: Discussionmentioning

confidence: 93%

Regulating the Skin Permeation Rate of Escitalopram by Ion-pair Formation with Organic Acids

et al. 2016

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Abstract. In order to regulate the skin permeation rate (flux) of escitalopram (ESP), ion-pair strategy was used in our work. Five organic acids with different physicochemical properties, benzoic acid (BA), ibuprofen (IB), salicylic acid (SA), benzenesulfonic acid (BSA), and p-aminobenzoic acid (PABA), were employed as counter-ions to regulate the permeation rate of ESP across the rabbit abdominal skin in vitro. The interaction between ESP and organic acids was characterized by FTIR and 13 C NMR spectroscopy. Results showed that all organic acids investigated in this study performed a controlling effect on ESP flux. To further analyze the factors concerned with the permeation capability of ESP-acid complex, a multiple linear regression model was used. It is concluded that the steady-state flux (J) of ESP-acid complexes had a positive correlation with log K o/w (the n-octanol/water partition coefficient of ion-pair complex) and pK a (the acidity of organic acid counter-ion), but a negative correlation with MW (the molecular weight of ionpair complex). The logK o/w of ion-pair complex is the primary one in all the factors that influence the skin permeation rate of ESP. The results demonstrated that organic acid with appropriate physicochemical properties can be considered as suitable candidate for the transdermal drug delivery of escitalopram.

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“…Felbinac (biphenylacetic acid), an active metabolite of fenbufen, is a non-steroidal anti-inflammatory and analgesic API. It reduces pain and swelling from inflammation resulting from prostaglandin secretion, especially in joints and muscles [ 3 ]. However, oral administration of felbinac is contraindicated, due to its adverse side-effects affecting the gastrointestinal tract; therefore, the best administration method for felbinac is TDDS.…”

Section: Introductionmentioning

confidence: 99%

Rheological and Mechanical Analyses of Felbinac Cataplasms by Using Box–Behnken Design

Yang¹,

Zhu²,

Diao³

et al. 2018

Pharmaceutics

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Felbinac, an active pharmaceutical ingredient (API) used clinically for the treatment of osteoarthritis, has poor solubility. Felbinac cataplasm product design was investigated using rheological and mechanical analyses. Experiments using a response surface methodology based on Box–Behnken design (BBD) incorporated three independent variables: the proportions of partially neutralized polyacrylate (NP800), dihydroxyaluminum aminoacetate (DAAA), and felbinac. Statistically significant quadratic models obtained using BBD demonstrated optimal NP-800, DAAA, and felbinac cataplasm proportions of 4.78–5.75%, 0.30–0.59%, and 0.70–0.90%, respectively. Felbinac cataplasms exhibited “gel-like” mechanical property with predominantly elastic behavior. Rheological studies correlated increasing NP-800 and DAAA concentrations with increased complex modulus (G*) values that were inversely related to peeling strength. Frequency sweep and creep tests revealed decreasing tan θ values with increasing NP-800 and DAAA concentrations. G’ and G” values were higher for higher NP-800 and DAAA levels, although G” values decreased with increasing DAAA concentration. Response surface methodology was applied to develop mathematical models. Variance analysis showed that the quadratic model effectively predicted felbinac and matrix material interactions, with two verification samples upholding model predictions. Relative errors between predicted and measured G* values were 3.28% and 1.10% and for peeling strength were 1.24% and 5.59%, respectively. In conclusion, rheological and mechanical analyses of felbinac cataplasms using BBD permits optimization of cataplasms as topical drug delivery vehicles.

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Design and Evaluation of a Novel Felbinac Transdermal Patch: Combining Ion-Pair and Chemical Enhancer Strategy

Cited by 15 publications

References 41 publications

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Regulating the Skin Permeation Rate of Escitalopram by Ion-pair Formation with Organic Acids

Rheological and Mechanical Analyses of Felbinac Cataplasms by Using Box–Behnken Design

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