Transdermal therapeutic system of carvedilol: Effect of hydrophilic and hydrophobic matrix on in vitro and in vivo characteristics

Ubaidulla, Udhumansha; Reddy, M V; Ruckmani, K.; Ahmad, Feroz; Khar, Roop K.

doi:10.1208/pt0801002

Cited by 131 publications

(97 citation statements)

References 14 publications

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“…15 Addition of HPMC has substantially enhanced the drug release by further increasing the wetting property of the release retarding layer. 16 A significant difference in percentage cumulative drug release was observed between F1, F2 and F3 as depicted in Figure 2, p≤0.05 was found to be statistically significant difference. The effect of penetration enhancers on the drug release was studied and the enhancement effect was found to be in the order IPM>MT>AZ.…”

Section: In Vitro Release Studies Of Transdermal Reservoir Systems Ofmentioning

confidence: 77%

Formulation Optimization and Study on Effect of Penetration Enhancers on Reservoir Transdermal Therapeutic Systems of Hydralazine Hydrochloride

Mannam¹,

Yallamalli²

2017

JYP

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INTRODUCTIONPulmonary arterial hypertension is a progressive disease which is due to constriction of pulmonary artery by excessive production of endothelien receptors. Hydralazine hydrochloride (HZH) is a drug candidate used to treat pulmonary arterial hypertension and it acts as a vasodilator by relaxing smooth muscles of pulmonary artery and the treatment lasts for long time. 1,2 Extreme variability in oral dosing of HZH, bioavailability of 31% and variable half-life of 3 to 7 h has made the dosage regimen complicated for oral usage.3 Metabolism variations depending on the phenotype and food interactions had much narrowed its oral usage. Low bioavailability, variable and short half-life may not be suitable to meet the therapeutic needs of the patient where the treatment is for longer duration. There is a need for alternative to oral route where hepatic first pass metabolism can be excluded and which can improve the therapeutic activity and quality of life of patient. As the drug has of low molecular weight 196.6 Daltons 4 transdermal delivery is a better alternative to oral route, where a continuous infusion of drug can be provided and patient compliance can be improved. Transdermal systems with a rate control membrane can provide a relatively constant rate of infusion of drug when the drug was maintained in required concentrations in reservoir system where the release rate will depend upon permeation through rate controlling membrane. 5 Hence, in the present work gel drug reservoir of HZH was formulated and the release rate was controlled by using rate controlling membrane and by varying penetration enhancers.Gel reservoir was formulated by using poloxamer a temperature sensitive hydrogel which is very stable, biocompatible and biodegradable polymer. 6,7 Poloxamer solution forms a clear solution at 4-5°C and converts to gel at room temperature.8 Rate controlling membranes were formulated by using E RLPO and E RSPO, the effect of penetration enhancer on release kinetics was evaluated. Pharmacotechnical properties, in vitro, ex vivo studies, stability studies and in vivo pharmacokinetic studies were evaluated. MATERIALS AND METHODS MaterialsHydralazine Hydrochloride was a gift sample received from Hetero drugs Pvt. Ltd, Hyderabad. Poloxamer 407 was provided as gift sample by Hi-Media Laboratories, Mumbai. Eudragit RLPO (E RLPO) and Eudragit RSPO (E RSPO) were gift samples provided by Zhaveri Pharma Chemicals., Mumbai. Release liner (poly iso butylene tape) was purchased from 3M. Hydroxy Propyl Methyl Cellulose (HPMC) and Poly Vinyl Acetate (PVA) were purchased from Hi-Media Laboratories, Mumbai. Azone (AZ), isopropyl myristate (IPM) and menthol (MT) were purchased from S.D Fine chemicals, Mumbai, India. All the solvents and reagents used were of analytical grade. Measurement of sol-gel transition temperatureSol-gel transition temperature was done to determine the poloxamer 407 concentration which retains its gel formation properties at room temperature. Poloxamer 407 solution with different concentrations ABST...

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Section: In Vitro Release Studies Of Transdermal Reservoir Systems Ofmentioning

confidence: 77%

Formulation Optimization and Study on Effect of Penetration Enhancers on Reservoir Transdermal Therapeutic Systems of Hydralazine Hydrochloride

Mannam¹,

Yallamalli²

2017

JYP

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“…To calculate moisture uptake, a uniformly-sized piece (1 cm 2 ) of each transdermal system was kept in a desiccator at room temperature for 24 h, and then weighted and exposed to a relative humidity of 75% (100 mL of saturated solution of sodium chloride) in a desiccator until its weight became constant (n = 3) (Ubaidulla et al, 2007).…”

Section: Moisture Uptake Studiesmentioning

confidence: 99%

Development and evaluation of occlusive systems employing polyvinyl alcohol for transdermal delivery of sumatriptan succinate

et al. 2010

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“…The skin pieces were mounted over the diffusion cells with the dermal side in contact with the receptor phase, equilibrated for 1 h, and then the air bubbles were removed. Subsequently, the film which contains 2 mg AZT was applied to the stratum corneum side in the donor compartment and wetted with 0.1 mL of 100 mM, pH 7.4, HEPES buffer in order to ensure the humidity (17,24). The amount of AZT penetrated from dorsal skin was determined by collecting 1-mL samples up to 8 h and the receptor phase replenished by adding 1 mL of buffer.…”

Section: Ex Vivo Release Studiesmentioning

confidence: 99%

“…The use of polymethacrylate kind of polymers (Eudragit) in matrix formulations for monolithic transdermal systems has been reported by several authors (13)(14)(15)(16)(17). Drug containing films of water-insoluble polymers were generally prepared by casting and drying organic drugpolymer solutions or suspensions, and the reasons for choosing Eudragit polymers were their high capacity for incorporating drugs and skin toleration (18,19).…”

Section: Introductionmentioning

confidence: 99%

“…ERL is freely permeable to water, whereas EC forms films which are insoluble in water. Varying the ratio of Eudragit or EC polymers in the composition of the films can provide a control for drug release characteristics (14,17). Also, both Eudragit and EC polymers are nontoxic, non-absorbable, and they do not lose their film-forming properties when formulated with the drug and the excipients (14).…”

Section: Introductionmentioning

confidence: 99%

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Studies on Transdermal Delivery Enhancement of Zidovudine

2009

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Abstract. The purpose of this study was to investigate physicochemical characteristics and in vitro release of zidovudine from monolithic film of Eudragit RL 100 and ethyl cellulose. Films included 2.5% or 5% (w/w) zidovudine of the dry polymer weight were prepared in various ratios of polymers by solvent evaporation method from methanol/acetone solvent mixture. The release studies were carried out by vertical Franz cells (2.2 cm 2 area, 20 ml receptor fluid). Ex vivo studies were done on Wistar rat skin within the films F6 (Eudragit RL100) and F7 (Eudragit RL100/Ethylcellulose, 1:1) consisting 5% (w/w) zidovudine in comparison with the same amount of free drug. Either iontophoresis (0.1 and 0.5 mA/cm 2 direct currents, Ag/AgCl electrodes) or dimethyl sulfoxide (pretreatment of 1% and 5%, w/w, solutions) were used as enhancers. Films consisting of ethyl cellulose under the ratio of 50% (w/w) gave similar release profiles, and the highest in vitro cumulative released amount was achieved with F6 film which gave the closest results with the free drug. This result could be due to the high swelling capacity and recrystallization inhibition effect of RL 100 polymer which also influenced the film homogenization. All the films were fitted to Higuchi release kinetics. It was also observed that both 0.5-mA/cm 2 current and 5% (w/w) dimethyl sulfoxide applications significantly increased the cumulative permeated amount of zidovudine after 8 h; however, the flux enhancement ratio was higher for 0.5-mA/cm 2 current application, especially within F6 film. Thus, it was concluded that Eudragit RL100 film (F6) could be further evaluated for the transdermal application of zidovudine.

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Transdermal therapeutic system of carvedilol: Effect of hydrophilic and hydrophobic matrix on in vitro and in vivo characteristics

Cited by 131 publications

References 14 publications

Formulation Optimization and Study on Effect of Penetration Enhancers on Reservoir Transdermal Therapeutic Systems of Hydralazine Hydrochloride

Formulation Optimization and Study on Effect of Penetration Enhancers on Reservoir Transdermal Therapeutic Systems of Hydralazine Hydrochloride

Development and evaluation of occlusive systems employing polyvinyl alcohol for transdermal delivery of sumatriptan succinate

Studies on Transdermal Delivery Enhancement of Zidovudine

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