On iontophoretic delivery enhancement: ionization and transport properties of lidocaine hydrochloride in aqueous propylene glycol

Karami, Kiomars; Merclin, Nadia; Brounéus, Fredrik; Beronius, Per

doi:10.1016/s0378-5173(00)00400-2

Cited by 7 publications

(4 citation statements)

References 6 publications

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“…Polycarbophil was found to have no appreciable effect on the conductivity of formulations Tc-Cab formulations but chitosan increased the conductivity of microemulsions from 0.182±0.07 to 3.42±0.12. It may contribute to drug permeation across nasal mucosa as it has been reported (19,34) that skin permeation also increases on application of potential. The pH of the mucoadhesive microemulsions was observed to be shifted from 6.78±0.09 to 5.25±0.12, on incorporation of chitosan or polycarbophil, making it more biocompatible intranasally as normal physiological pH of human nasal mucosa is being reported to be between 4.5 and 6.5.…”

Section: Resultsmentioning

confidence: 98%

Intranasal Cabergoline: Pharmacokinetic and Pharmacodynamic Studies

Mishra

Misra

2009

AAPS PharmSciTech

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Abstract. Aims of this investigation were to prepare and characterize cabergoline intranasal microemulsion formulations, determine brain drug delivery through biodistribution using technetium-99m ( 99m Tc) as a tracer, and assess its performance pharmacodynamically in weight control. Cabergoline microemulsions of different compositions were prepared by water titration method and characterized for globule size and zeta potential. Microemulsion with maximum drug solubilization and stability was considered optimal and taken for further studies with or without addition of mucoadhesive agent. Pharmacokinetics of optimized 99m Tclabeled cabergoline formulations and 99m Tc-labeled drug solution were studied by estimating radioactivity in brain and blood of albino rats post intranasal, intravenous, and oral administrations. To confirm localization of drug in brain following intranasal, intravenous, and oral administrations, gamma scintigraphy imaging was also performed. To assess weight control performance of formulations, body weight, white adipose tissue mass, serum lipids, leptin, and prolactin were determined before and after 40 days of intranasal administrations of these formulations to Wistar rats. Microemulsions were found to be stable both physically and chemically when stored at various stress conditions. Brain/blood uptake ratios, drug targeting efficiency, and direct drug transport were found to be highest for drug mucoadhesive microemulsion followed by drug microemulsion and drug solution post-intranasal administration compared to intravenous drug microemulsion. Significant (p<0.05) reduction in assessed pharmacodynamic parameters was observed after intranasal administration of mucoadhesive microemulsion against control group. The results of the studies conclusively demonstrate that intranasal microemulsion formulations developed in this investigation are stable and can deliver cabergoline selectively and in higher amounts to the brain compared to both drug administrations as a solution intranasally or microemulsion intravenously. The results also demonstrate reduction in weight, adipose tissue mass, serum lipids, and serum prolactin after intranasal administration of drug microemulsion. Hence, long-term studies in at least two more animal models followed by extensive clinical evaluation can safely result into a product for clinical use.KEY WORDS: biodistribution; cabergoline; intranasal; obesity; radiolabeling. INTRODUCTIONCabergoline (Cab) is a potent semi-synthetic ergot alkaloids used for the treatment of diseases caused by hyperprolactinemia (11) (elevated serum prolactin levels >20 μg/L) and few neurological disorders (11) (Parkinson's disease) as dopamine agonist. However, review of recent research suggests its possible application as a lipid lowering and anti-obesity agent by controlling serum prolactin levels. In a study on golden hamsters (8), it was observed that reduced prolactin retards liver lipogenesis even if insulin is available in abundance for supplying glucose for lipogenesis. In a human ...

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Section: Resultsmentioning

confidence: 98%

Intranasal Cabergoline: Pharmacokinetic and Pharmacodynamic Studies

Mishra

Misra

2009

AAPS PharmSciTech

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“…So, the preparation of HPNs of PVA with chitosan is a promising way to obtain hydrogels with limited solubility and adequate ionic conductivity. In our work it is emphasized the effect of PVA ionic conductivity when crosslinked in chitosan HPNs, in which the ionic conductivities are not similar to that of the polymer electrolytes for battery application, therefore they are suitable for iontophoretic drug delivery systems as reported for lidocaine delivery ones based on propylene glycol with ionic conductivity values around 10 À7 X À1 cm À1 [21]. Literature data reported several SPEs synthesized to be used as candidate materials in lithium polymer batteries in which SPEs with enhanced ionic conductivity are required and values around 10 À3 X À1 cm À1 were obtained, for example, with poly(ethylene oxide) and polyvinylidene fluoride based polymer electrolytes [10][11][12].…”

Section: Resultsmentioning

confidence: 95%

Synthesis and characterization of hybrid polymeric networks (HPN) based on polyvinyl alcohol/chitosan

Rodrigues

Forte

Azambuja

et al. 2007

Reactive and Functional Polymers

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“…Low molecular weight glycols have been studied for iontophoretic delivery enhancement [24] and these may be thought of as low molecular weight analogues of polymer electrolytes. They are, however, liquids whereas the solidlike, thin film polymer electrolytes are solutions of ionic salts in immobile, long-chain heteropolymers [25].…”

Section: Polymer Electrolytes As Iontophoretic Electrode Reservoirsmentioning

confidence: 99%

Pharmaceutical and medical applications of polymer electrolytes

Latham

Linford

Schlindwein

2003

Ionics

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Abstract. Classic methods of drug delivery have embraced a number of routes into the site of pharmacological action. Modem preference, wherever possible, is for a non-invasive route to minimise the chance of cross infection, especially of the AIDS virus. The skin, which is the largest organ in the human body, is a particularly appealing route as, in the absence of wounds and blemishes, it offers a natural, high-integrity, barrier to the outside world. Skin patches containing active drug that is allowed to diffuse passively across the external skin barrier into the bloodstream now enjoy wide application but a problem is that the rate of egress is often slow.For certain ionic drugs, including local anaesthetics and, more recently, peptides and gene-based, biotechnological engineered pharmaceuticals, it is possible substantially to enhance transdermal transport by iontophoresis. The technique of iontophoresis facilitates the passage of ionic drugs through the skin using an electric current. IonicaUy conducting polymers (polymer electrolytes) are potential candidates as hosts for drugs to be delivered iontophoreticaUy.Key issues affecting iontophoretic delivery are reviewed in this paper and the potential role of polymer electrolyte materials in iontophoretic devices will be described.

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On iontophoretic delivery enhancement: ionization and transport properties of lidocaine hydrochloride in aqueous propylene glycol

Cited by 7 publications

References 6 publications

Intranasal Cabergoline: Pharmacokinetic and Pharmacodynamic Studies

Intranasal Cabergoline: Pharmacokinetic and Pharmacodynamic Studies

Synthesis and characterization of hybrid polymeric networks (HPN) based on polyvinyl alcohol/chitosan

Pharmaceutical and medical applications of polymer electrolytes

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