Development of drug-in-adhesive patch formulations for transdermal delivery of fluoxetine: In vitro and in vivo evaluations

Jung, Eun-Jae; Lee, Eun Young; Choi, Hoo‐Kyun; Ban, Sang-Jun; Choi, Seung–Hyuk; Kim, Jung Sun; Yoon, In‐Soo; Kim, Dae-Duk

doi:10.1016/j.ijpharm.2015.04.012

Cited by 44 publications

(15 citation statements)

References 29 publications

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“…Described herein before, four renowned acrylate adhesives (Duro-Tak 87-4287, Duro-Tak 87-9301, Duro-Tak 87-2287 and Duro-Tak 87-2510) were selected based on the literature where their potential and suitability in developing transdermal systems of several drug molecules are demonstrated. [14][15][16][17][18] Pressure sensitive adhesives containing carboxylic acid groups were not examined as there is a possible interaction between the drug and adhesive. The properties of the selected adhesives are described in Table 1.…”

Section: Resultsmentioning

confidence: 99%

“…small size, easy to formulate, comfortable to wear, prolonged delivery of active substances, no dose dumping, higher patient compliance etc. 15,16 Several research groups have demonstrated the feasibility of delivering active drug moieties through the skin using drug in adhesive transdermal systems. 17,18 The current study investigate the feasibility of developing a drug in adhesive transdermal system of vildagliptin and its comparison with oral therapy in animal model.…”

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confidence: 99%

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Development of Transdermal Delivery System of Vildagliptin and Its Comparison with Oral Therapy.

Nair¹,

Kumria²,

Al‐Dhubiab³

et al. 2016

IJPER

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Purpose:The long term oral therapy of vildagliptin is associated with potential hepatotoxicity and low patient compliance. This study aims at development of a drug in adhesive transdermal patch system of vildagliptin using pressure sensitive acrylic polymers and compare the pharmacokinetics with oral therapy. Methods: The prospective of different chemical enhancers in improving the transport of vildagliptin was assessed ex vivo. In vivo permeation studies in rats were performed using patch system contain sodium lauryl sulfate as enhancer. Results: Drug solubility varied among adhesive bases tested and maximum value (15% w/w) observed with Duro-Tak 87-2510. Incorporation of chemical agents significantly improved the permeation of vildagliptin, but not to the same extent. The highest flux value of vildagliptin was obtained by the addition of sodium lauryl sulfate (22.96 ± 3.58 µg/cm 2 /h; P<0.0001), which is ~4 folds higher as compared to control. Pharmacokinetic profiles of vildagliptin were different for transdermal and oral delivery with significantly high bioavailability by transdermal delivery. The AUC 0-α in transdermal delivery (1018.43 ± 79.56 ng.h/mL) was ~14 folds higher (P<0.0001) as compared to oral administration. Conclusion: The current study concludes that the fabricated drug in adhesive transdermal system could be employed for the effective delivery of vildagliptin.

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Section: Resultsmentioning

confidence: 99%

mentioning

confidence: 99%

Development of Transdermal Delivery System of Vildagliptin and Its Comparison with Oral Therapy.

Nair¹,

Kumria²,

Al‐Dhubiab³

et al. 2016

IJPER

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“…In many studies, the correlation of permeation characteristics between hairless mouse and human skins has been reported for many drugs, which is due to the similarity of skin lipid composition between two skins (Durrheim et al ., 1980; Jung and Maibach, 2015; Jung et al ., 2015). It is well known that the major skin permeation route is transepidermal pathway, and transappendageal pathway (including hair follicles and sweat gland) contributes less than 0.1% of the total permeation amount (Bond and Barry, 1988).…”

Section: Discussionmentioning

confidence: 99%

“…The calculated concentration of SMM in the 2.14 cm 2 surface area of epidermis/dermis was about 223 μM. The skin permeability of human skin is known to be at least two times lower than that of hairless mouse skin (Jung et al ., 2015; Seo et al ., 2016), and SMM showed wound healing and photoprotective effect in human dermal fibroblast at higher than 100 μM concentration (Kim et al ., 2010, 2015). Thus, it was necessary to further increase the skin deposition of SMM in epidermis/dermis.…”

Section: Discussionmentioning

confidence: 99%

Effect of Enhancers on in vitro and in vivo Skin Permeation and Deposition of S-Methyl-_L-Methionine

Kim

et al. 2017

Biomolecules & Therapeutics

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S-methyl-l-methionine (SMM), also known as vitamin U, is commercially available as skin care cosmetic products for its wound healing and photoprotective effects. However, the low skin permeation expected of SMM due to its hydrophilic nature with a log P value of −3.3, has not been thoroughly addressed. The purpose of this study thus was to evaluate the effect of skin permeation enhancers on the skin permeation/deposition of SMM. Among the enhancers tested for the in vitro skin permeation and deposition of SMM, oleic acid showed the most significant enhancing effect. Moreover, the combination of oleic acid and ethanol further enhanced in vitro permeation and deposition of SMM through hairless mouse skin. Furthermore, the combination of oleic acid and ethanol significantly increased the in vivo deposition of SMM in the epidermis/dermis for 12 hr, which was high enough to exert a therapeutic effect. Therefore, based on the in vitro and in vivo studies, the combination of oleic acid and ethanol was shown to be effective in improving the topical skin delivery of SMM, which may be applied in the cosmetic production process for SMM.

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“…This patch system is widely used in the clinical practice, owing to its advantages of small size and thickness, flexible formulation, simple production process and good patient compliance (Hu et al, 2011;Jung et al, 2015). Therefore, a drug-in-adhesive type patch was developed for ZAL transdermal delivery in the present study.…”

Section: Design and Optimization Of Zal Transdermal Patchesmentioning

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

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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

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Development of drug-in-adhesive patch formulations for transdermal delivery of fluoxetine: In vitro and in vivo evaluations

Cited by 44 publications

References 29 publications

Development of Transdermal Delivery System of Vildagliptin and Its Comparison with Oral Therapy.

Development of Transdermal Delivery System of Vildagliptin and Its Comparison with Oral Therapy.

Effect of Enhancers on in vitro and in vivo Skin Permeation and Deposition of S-Methyl-_L-Methionine

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

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Development of drug-in-adhesive patch formulations for transdermal delivery of fluoxetine: In vitro and in vivo evaluations

Cited by 44 publications

References 29 publications

Development of Transdermal Delivery System of Vildagliptin and Its Comparison with Oral Therapy.

Development of Transdermal Delivery System of Vildagliptin and Its Comparison with Oral Therapy.

Effect of Enhancers on in vitro and in vivo Skin Permeation and Deposition of S-Methyl-L-Methionine

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

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Effect of Enhancers on in vitro and in vivo Skin Permeation and Deposition of S-Methyl-_L-Methionine