Development of Nitrendipine Transdermal Patches: In vitro and Ex vivo Characterization

Gannu, Ramesh; Vishnu, Y Vamshi; Veerabrahma, Kishan; Rao, Yi

doi:10.2174/156720107779314767

Cited by 71 publications

(54 citation statements)

References 15 publications

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“…The receptor phase was replenished with an equal volume of phosphate buffer at each sample withdrawal. [12,24] In-vivo studies…”

Section: In Vitro Drug Diffusion Studiesmentioning

confidence: 99%

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Untitled

Boggula¹

2018

AJP

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Aim: The aim of the present study was to design, develop, and evaluate a matrix-type transdermal formulation containing buspirone hydrochloride (HCL) for treatment of anxiety with a goal to increase the bioavailability and improve the patient compliance. Materials and Methods: In the present research work, the different concentrations of hydroxypropyl methylcellulose (HPMC) E50, HPMC E15, and Eudragit RS100 were used in combination to optimize the concentration of HPMC E15 and Eudragit RS100 in the formulation of transdermal patches. These different ratios of hydrophilic and hydrophobic polymeric combinations plasticized with dibutyl phthalate by the solvent evaporation technique. The prepared patches were evaluated for their physicochemical characteristics such as thickness, weight and drug content uniformity, moisture content, moisture uptake and folding endurance, and in vitro drug release studies. Optimized formulation was further evaluated by in vivo release study, drug-excipient compatibility, and stability study. Results and Discussion: Effect of permeation enhancers such as oleic acid was studied. The interference of the polymers was ruled out by Fourier transform infrared and ultraviolet-spectroscopic methods. In vitro release studies of buspirone HCL-loaded patches in phosphate buffer (pH, 7.4) were performed using a modified diffusion cell and showed first-order release rate. Skin studies for the transdermal patches were assessed and were found to be free of irritation. In vivo drug release studies had shown release up to 24 h with the release of 73.82% and it was correlated with in vitro studies. The patches were subjected to short-term stability studies and were found stable. Conclusion: It is concluded from the present studies that the transdermal patches of buspirone HCL were capable of exhibiting controlled release with the stability. Studies had shown promising results, and there was a scope for further pharmacodynamic and pharmacokinetic evaluation.

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“…The receptor phase was replenished with an equal volume of phosphate buffer at each sample withdrawal. [12,24] In-vivo studies…”

Section: In Vitro Drug Diffusion Studiesmentioning

confidence: 99%

“…When compared with other therapies on a cost basis, transdermal systems are generally inexpensive and economical. An ideal features of drug to be formulated as transdermal drug delivery should possess several physicochemical properties [12,13] such as short half-life, small molecular size, low dose, and low oral bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Untitled

Boggula¹

2018

AJP

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“…The final weight of each film was taken in achieving the constant weight. The moisture uptake capacity of each film was determined by taking the difference of initial and final weights with respect to the initial weight [26].…”

Section: Moisture Uptake Capacitymentioning

confidence: 99%

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Ali

Kumar

Ahad

et al. 2015

Journal of Polymer Engineering

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A transdermal therapeutic system (TTS) of diclofenac diethylamine (DDE) was developed to obtain a prolonged controlled drug delivery by the solvent evaporation technique. The matrix diffusion controlled systems used various combinations of hydrophilic (polyvinylpyrrolidone K30) and lipophilic (Eudragit RL 100  and Eudragit RS 100  ) polymers containing dimethyl sulfoxide (DMSO) (0, 5 and 10% w/w) as a penetration enhancer. In vitro drug release was improved with an increased fraction of hydrophilic polymer. Formulation F8 containing Eudragit RL 100 and polyvinylpyrrolidone K30 in the ratio 40:60 presented the highest drug release (92.45%) and permeation rate (0.0988±0.010 mg/cm 2 /h) with sustained release action for 48 h. In vivo pharmacodynamic study of DDE-loaded Eudragit RL 100  transdermal system (formulation F8) showed significant higher percent inhibition of rat paw edema compared with the marketed formulation of the drug. Our results suggest that a developed formulation is an efficient system for transdermal diclofenac delivery against inflammation. The optimized formulation was found to be stable and did not show physicochemical interaction. The system is envisaged to be stable for a sufficiently long period (2.52 years) at room temperature.

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“…These studies evaluated modifications in the permeability of the horny layer by using physical methods, treatment with chemical enhancers, examining the array of lipids and the conformation of proteins in the outermost layer of the skin. The displacement of the infrared bands of the A. L. M. Ruela, A. G. Perissinato, M. E. S. Lino, P. S. Mudrik, G. R. Pereira 536 treated skin relative to those of the untreated skin helped to elucidate the modifications in the stratum corneum caused by chemical or physical treatments (Gupta, Jain, Varshney, 2005;Gannu et al, 2007;Mcauley et al, 2013).Skin samples are directly placed in a crystal of zinc selenite (ZnSe) without previous treatments (Moser et al, 2001). The bands in the range of 2930-2920 cm -1 and 2855-2850 cm -1 are related to asymmetric and symmetric CH 2 stretching that represents the lipid array in the stratum corneum.…”

mentioning

confidence: 99%

Evaluation of skin absorption of drugs from topical and transdermal formulations

Ruela

Perissinato

Lino

et al. 2016

Braz. J. Pharm. Sci.

209

135

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The skin barrier function has been attributed to the stratum corneum and represents a major challenge in clinical practice pertaining to cutaneous administration of drugs. Despite this, a large number of bioactive compounds have been successfully administered via cutaneous administration because of advances in the design of topical and transdermal formulations. In vitro and in vivo evaluations of these novel drug delivery systems are necessary to characterize their quality and efficacy. This review covers the most well-known methods for assessing the cutaneous absorption of drugs as an auxiliary tool for pharmaceutical formulation scientists in the design of drug delivery systems. In vitro methods as skin permeation assays using Franz-type diffusion cells, cutaneous retention and tape-stripping methods to study the cutaneous penetration of drugs, and in vivo evaluations as pre-clinical pharmacokinetic studies in animal models are discussed. Alternative approaches to cutaneous microdialysis are also covered. Recent advances in research on skin absorption of drugs and the effect of skin absorption enhancers, as investigated using confocal laser scanning microscopy, Raman confocal microscopy, and attenuated total reflectance Fourier-transform infrared spectroscopy, are reviewed. Uniterms:Skin absorption/effects/study. Skin absorption/topical formulations. Skin absorption/ transdermal formulations. Skin absorptions/enhancers. INTRODUCTIONTopical and transdermal drug delivery systems have shown significant advantages in clinical practice for drug targeting to the action site in the body; this has reduced the systemic side effects. The administration of drugs by through the skin is also performed to achieve controlled or prolonged drug delivery, and this route can be explored as an alternative to the oral route. The oral route shows some limitations for drugs with irregular absorption in the gastrointestinal tract and low bioavailability and for drugs with increased first pass metabolism and short plasma halflife times (Barry, 2001;Wokovich et al., 2006;Prausnitz, Langer, 2009;Alexander et al., 2012).Many drug products applied to the skin surface may penetrate to some extent into the skin layers, where their effects are expected. This is the case for topical formulations for treatment of skin disorders such as acne and cutaneous inflammatory diseases that include dermatitis, erythematous lupus, and psoriasis. On the other hand, transdermal formulations release drugs that permeate through the skin and enter the systemic circulation. Transdermal therapy must ensure that significant concentrations of the drug are absorbed to reach effective plasma concentrations. Permeation of drugs is targeted in some cases to body regions close to the action site, where a regional effect is expected, e.g., in the muscles, blood vessels, and articulations. In this way, the term "cutaneous absorption" is properly used to characterize the sum of the amounts of drug that penetrate and permeate the skin (Barry, 2001;El Maghraby, Barry;Willi...

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Development of Nitrendipine Transdermal Patches: In vitro and Ex vivo Characterization

Abstract: Nitrendipine matrix type transdermal therapeutic systems could be prepared with the required flux having suitable mechanical properties.

Cited by 71 publications

References 15 publications

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Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation

Evaluation of skin absorption of drugs from topical and transdermal formulations

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Development of Nitrendipine Transdermal Patches: In vitro and Ex vivo Characterization

Abstract: Nitrendipine matrix type transdermal therapeutic systems could be prepared with the required flux having suitable mechanical properties.

Cited by 71 publications

References 15 publications

Untitled

Untitled

Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100® transdermal system against inflammation

Evaluation of skin absorption of drugs from topical and transdermal formulations

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Enhanced delivery of diclofenac diethylamine loaded Eudragit RL 100^® transdermal system against inflammation