Dendrimer-mediated transdermal delivery: enhanced bioavailability of indomethacin

Chauhan, Abhay Singh; Sridevi, S.; Chalasani, Kishore B.; Jain, Akhlesh Kumar; Jain, Sanjay; Jain, Narendra Kumar; Diwan, Prakash V.

doi:10.1016/s0168-3659(03)00200-1

Cited by 319 publications

(203 citation statements)

References 16 publications

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“…6 Dendritic architecture and uniformly positioned functionality have been recently reported to carry the anti-inflammatory drug indomethacin for its transdermal delivery as well as anticancer drugs (eg, 6-mercaptopurine). 7,8 Recent studies reported investigation on the effect of 4.0 generation (G) PAMAM dendrimer present in an anionic phospholipid composition, consisting of hydrogenated soyaphosphotidylcholine, cholesterol, dicetylphosphate, and poly(ethylene glycol)-derivatized phosphotidylethnolamine, on the hydration and liquid crystalline structure formation. 9 Flurbiprofen (FB), a phenylpropionic acid derivative with analgesic and anti-inflammatory action, is widely used in the treatment of rheumatoid arthritis and other rheumatic disorders.…”

Section: Introductionmentioning

confidence: 99%

Poly(amidoamine) (PAMAM) dendritic nanostructures for controlled sitespecific delivery of acidic anti-inflammatory active ingredient

et al. 2005

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The purpose of the investigation was to evaluate the potential of polyamidoamine (PAMAM) dendrimer as nanoscale drug delivery units for controlled release of water insoluble and acidic anti-inflammatory drug. Flurbiprofen (FB) was selected as a model acidic anti-inflammatory drug. The aqueous solutions of 4.0 generation (G) PAMAM dendrimer in different concentrations were prepared and used further for solubilizing FB. Formation of dendrimer complex was characterized by Fourier transform infrared spectroscopy. The effect of pH on the solubility of FB in dendrimer was evaluated. Dendrimer formulations were further evaluated for in vitro release study and hemolytic toxicity. Pharmacokinetic and biodistribution were studied in male albino rats. Efficacy of dendrimer formulation was tested by carrageenan induced paw edema model. It was observed that the loaded drug displayed initial rapid release (more than 40% till 3rd hour) followed by rather slow release. Pharmacodynamic study revealed 75% inhibition at 4th hour that was maintained above 50% till 8th hour. The mean residence time (MRT) and terminal half-life (THF) of the dendritic formulation increased by 2-fold and 3-fold, respectively, compared with free drug. Hence, with dendritic system the drug is retained for longer duration in the biosystem with 5-fold greater distribution. It may be concluded that the drug-loaded dendrimers not only enhanced the solubility but also controlled the delivery of the bioactive with localized action at the site of inflammation.

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Section: Introductionmentioning

confidence: 99%

Poly(amidoamine) (PAMAM) dendritic nanostructures for controlled sitespecific delivery of acidic anti-inflammatory active ingredient

et al. 2005

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“…However, many new drugs are hydrophobic causing low water-solubility that results in insufficient levels of drug delivered into cells. Water soluble and biocompatible dendritic species are known to improve drug solubility and plasma circulation time via transdermal formulations and to deliver drugs quickly and effectively [72,[76][77][78][79][80][81]. In this regard, dendrimers have been shown to be useful as transdermal drug delivery systems for various types of medications [77,80,81], including anticancer, antiviral, nonsteroidal anti-inflammatory and antihypertensive drugs.…”

Section: Transdermal Drug Deliverymentioning

confidence: 99%

Polyester Dendrimers: Smart Carriers for Drug Delivery

Twibanire

Grindley

2014

Polymers

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Polyester dendrimers have been shown to be outstanding candidates for biomedical applications. Compared to traditional polymeric drug vehicles, these biodegradable dendrimers show excellent advantages especially as drug delivery systems because they are non-toxic. Here, advances on polyester dendrimers as smart carriers for drug delivery applications have been surveyed. Both covalent and non-covalent incorporation of drugs are discussed.

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“…Cheng et al (2007) suggested that PAMAM dendrimer (G5-NH 2 ) could covalently conjugate with different NSAIDs (ketoprofen or diflunisal), significantly improve the drug permeation through the skin and achieve a prolonged pharmcodynamic profile. An in vivo pharmacokinetic assay showed that the blood concentration of indometacin in rats was increased in the presence of PAMAM dendrimers (G4-NH 2 and G4-OH) (Chauhan et al, 2003). In addition, transdermal delivery of other drugs, such as 8-methoxypsoralen (8-MOP), could also be enhanced by the PAMAM dendrimers (G3-NH 2 and G4-NH 2 ) both in vitro and in vivo.…”

Section: Dendrimersmentioning

confidence: 99%

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

2013

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The highly organized structure of the stratum corneum provides an effective barrier to the drug delivery into or across the skin. To overcome this barrier function, penetration enhancers are always used in the transdermal and dermal drug delivery systems. However, the conventional chemical enhancers are often limited by their inability to delivery large and hydrophilic molecules, and few to date have been routinely incorporated into the transdermal formulations due to their incompatibility and local irritation issues. Therefore, there has been a search for the compounds that exhibit broad enhancing activity for more drugs without producing much irritation. More recently, the use of biomaterials has emerged as a novel method to increase the skin permeability. In this paper, we present an overview of the investigations on the feasibility and application of biomaterials as penetration enhancers for transdermal or dermal drug delivery systems.

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Dendrimer-mediated transdermal delivery: enhanced bioavailability of indomethacin

Cited by 319 publications

References 16 publications

Poly(amidoamine) (PAMAM) dendritic nanostructures for controlled sitespecific delivery of acidic anti-inflammatory active ingredient

Poly(amidoamine) (PAMAM) dendritic nanostructures for controlled sitespecific delivery of acidic anti-inflammatory active ingredient

Polyester Dendrimers: Smart Carriers for Drug Delivery

Biomaterials as novel penetration enhancers for transdermal and dermal drug delivery systems

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