Transdermal Delivery of Isosorbide 5-Mononitrate from a New Membrane Reservoir and Matrix-Type Patches

Arra, G. S.; Arutla, Srinivas; Krishna, D. R.

doi:10.3109/03639049809085648

Cited by 6 publications

(4 citation statements)

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“…13,14) Different types of terpenes have been shown to be effective penetration enhancers for both hydrophilic 15,16) and lipophilic drugs.…”

Section: )mentioning

confidence: 99%

“…11,12) It has been suggested that terpenes increase the penetration of drugs through the skin by disrupting the intercellular packaging of stratum corneum lipids and by increasing drug diffusivity. 13,14) Different types of terpenes have been shown to be effective penetration enhancers for both hydrophilic 15,16) and lipophilic drugs. 17,18) Nerolidol is an amphiphilic and highly lipophilic sesquiterpene (log P 5.36± 0.38).…”

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confidence: 99%

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Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Bektaş

Cevher

Güngör

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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It was aimed to develop the matrix type polysaccharide-based transdermal films of nifedipine (NFD) to provide its long term plasma concentration. The mechanical tests were carried out on gel formulations which were utilised in the fabrication of transdermal films to determine the type of polymer (pectin, sodium alginate) and plasticizer (propylene glycol, glycerine) as well as their concentrations. The mechanical strength, elasticity, bioadhesiveness and the drug release characteristics of optimised films containing NFD were evaluated. Permeation of NFD from the films with/without adding an enhancer (nerolidol) was followed through excised rat skin using Franz diffusion cells. Results showed that the gels composed of either pectin or sodium alginate were appropriate for the fabrication of transdermal films of NFD, and the addition of propylene glycol improved mechanical strength, flexibility, and bioadhesiveness of the films. Permeation data showed that nerolidol was an effective permeation enhancer for the polysaccharide-based transdermal films of NFD.Key words nifedipine; transdermal film; sodium alginate; pectin; texture analysis; nerolidol Transdermal delivery possesses many advantages over conventional drug administration routes, including avoidance of intestinal and/or hepatic first pass metabolism, reduction in side effects and better patient compliance. Polymers are crucial components for the formulation of transdermal delivery systems. There are some critical parameters for the optimisation of transdermal therapeutic systems including physical or chemical stability of the formulation, compatibility with skin, adhesion to skin, the release characteristics of drug from the vehicle and its permeation through the skin. Therefore, the choice of polymers and plasticizers used in transdermal systems have strong impact on drug release, permeability, elasticity, and wearing properties of transdermal formulations. 1,2)Natural polysaccharides such as sodium alginate, chitosan, pectin, guar gum, gellan gum have been widely evaluated as a polymer in the optimisation of transdermal systems due to their non-toxic, biocompatible and potentially biodegradable properties.3,4) Sodium alginate is a mixture of polyuronic acids composed of residues of D-mannuronic acid and L-guluronic acid, which is used in design of controlled drug delivery formulations.5) It has also been used to formulate transdermal films. 6,7)Despite all the advantages of transdermal drug delivery, stratum corneum, the outermost layer of the skin, provides the greatest resistance to entrance of drugs to the systemic blood stream. In order to achieve therapeutic drug concentration following transdermal administration, penetration enhancers which reduce the barrier characteristics of stratum corneum reversibly are added into transdermal formulations. 8,9)Terpenes appear to have good skin penetration characteristics for transdermal systems due to their low cutaneous irritancies, good toxicological profiles.8) Moreover, this interaction with the stratum cor...

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“…13,14) Different types of terpenes have been shown to be effective penetration enhancers for both hydrophilic 15,16) and lipophilic drugs.…”

Section: )mentioning

confidence: 99%

Section: )mentioning

confidence: 99%

Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Bektaş

Cevher

Güngör

et al. 2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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“…Transdermal therapeutic systems (TTSs) are a typical example of DDSs. Therapeutic medicines in TTSs that have already been marketed include tulobuterol for the treatment of bronchial asthma, 1) clonidine for hypertension, 2) nitroglycerin and isosorbide dinitrate for angina pectoris, 3,4) and rivastigmine for Alzheimer's disease. 5) However, the enhancement of skin permeation is sometimes required for drugs.…”

mentioning

confidence: 99%

“…2) nitroglycerin and isosorbide dinitrate for angina pectoris, 3,4) and rivastigmine for Alzheimer's disease. 5) However, the enhancement of skin permeation is sometimes required for drugs.…”

mentioning

confidence: 99%

Analysis of the Pretreatment Effect of Ethanol on the Stratum Corneum- and Hair Follicular-Penetration of Drugs Using the Hair Follicle-Plugging Method

Horita

Todo

Sugibayashi

2014

CHEMICAL & PHARMACEUTICAL BULLETIN

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The hair follicle-plugging method was used to analyze the effects of EtOH on skin permeation pathways. Methods: In vitro permeation experiments were performed on 4 model drugs [isosorbide mononitrate (ISMN), ionized lidocaine (ionized LC), fluorescein (FL), and fluorescein isothiocyanate (FITC)-dextran 4 kDa (FD-4)] using excised pig ear skin. The skin permeations of ionized LC, FL, and FD-4 were decreased by hair follicle-plugging. Hair follicle-plugging prevented the skin permeation of FL and FD-4 in EtOHpretreated skin, but did not prevent that of ISMN. On the other hand, the effect of hair follicle-plugging on the permeation of ionized LC was different among the pretreatment conditions. These results indicate that the EtOH pretreatment greatly affected the aqueous pathway in the stratum corneum and hair follicles.Key words skin permeation; aqueous pathway; hair follicle-plugging; EtOH pretreatment; permeation route; enhancer Drug delivery systems (DDSs) have been investigated extensively to provide drug formulations with sustained release and/or targeting properties. Transdermal therapeutic systems (TTSs) are a typical example of DDSs. Therapeutic medicines in TTSs that have already been marketed include tulobuterol for the treatment of bronchial asthma, 1) clonidine for hypertension,2) nitroglycerin and isosorbide dinitrate for angina pectoris, 3,4) and rivastigmine for Alzheimer's disease. 5) However, the enhancement of skin permeation is sometimes required for drugs. Skin penetration enhancers are one of the methods used to increase the skin permeation of drugs.Skin penetration enhancers include alcohols, 6,7) fatty acids, 8,9) fatty acid esters, 10,11) terpenes, 12,13) pyrrolidones, 14,15) surfactants, 16,17) and Azone. 18,19) Among these enhancers, ethanol (EtOH) is the most commonly used additive in topical formulations. It is applied not only as a skin penetration enhancer, but also a solvent, such as water, for skin disinfection, as well as a solubilizer for poorly-soluble drugs. Estradiol and fentanyl dermal patches are typical examples that contain EtOH to enhance their absorption into the skin. [20][21][22] The mechanisms underlying the penetration-enhancement effect of EtOH on the stratum corneum barrier were previously reported to be lipid extraction, an increase in lipid fluidity, the enhancement of drug solubility in stratum corneum lipids, changes in skin hydration, effects on the putative pore pathway, alterations in keratinized proteins, and effects on solvent drugs. 23,24) Although many studies have already examined skin permeability with the simultaneous application of EtOH and drugs, few have investigated the effects of an EtOH pretreatment on the skin permeation of drugs. EtOH-containing formulations are frequently applied to the skin surface for the purpose of preventing disinfection and other therapeutic treatments. Other topical formulations may also be applied following treatments with EtOH-containing formulations.We previously investigated the effects of an EtOH pretreatment on th...

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Watanabe

Hasegawa

Takahashi

et al. 2002

Pharmaceutical Research

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Transdermal Delivery of Isosorbide 5-Mononitrate from a New Membrane Reservoir and Matrix-Type Patches

Cited by 6 publications

References 10 publications

Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Design and Evaluation of Polysaccharide-Based Transdermal Films for the Controlled Delivery of Nifedipine

Analysis of the Pretreatment Effect of Ethanol on the Stratum Corneum- and Hair Follicular-Penetration of Drugs Using the Hair Follicle-Plugging Method

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