The development and registration of topical pharmaceuticals

Mugglestone, Christopher J.; Mariz, Segundo; Lane, Majella E.

doi:10.1016/j.ijpharm.2012.03.052

Cited by 23 publications

(9 citation statements)

References 14 publications

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“…The assay is also useful for the comparison of the topical availability of corticosteroid formulations containing the same concentration of the same corticosteroid. 22,36 In many studies, the vasoconstriction assay employed visual evaluation of the degree of blanching by trained observers. 37,38 In this study, a chromameter was utilized to quantify and compare the vasoconstrictor effect of DFV.…”

Section: Skin Blanching Assaymentioning

confidence: 99%

Enhanced dermal delivery of diflucortolone valerate using lecithin/chitosan nanoparticles: in-vitro and in-vivo evaluations

Özcan¹,

Azizoğlu²,

Şenyiğit³

et al. 2013

IJN

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Abstract:The objective of this study was to prepare a suitable formulation for dermal delivery of diflucortolone valerate (DFV) that would maintain the localization in skin layers without any penetration and to optimize efficiency of DFV. Drug-loaded lecithin/chitosan nanoparticles with high entrapment efficiency (86.8%), were successfully prepared by ionic interaction technique. Sustained release of DFV was achieved without any initial burst release. Nanoparticles were also incorporated into chitosan gel at different ratios for preparing a more suitable formulation for topical drug delivery with adequate viscosity. In ex-vivo permeation studies, nanoparticles increased the accumulation of DFV especially in the stratum corneum + epidermis of rat skin without any significant permeation. Retention of DFV from nanoparticle in chitosan gel formulation (0.01%) was twofold higher than commercial cream, although it contained ten times less DFV. Nanoparticles in gel formulations produced significantly higher edema inhibition in rats compared with commercial cream in in-vivo studies. Skin blanching assay using a chromameter showed vasoconstriction similar to that of the commercial product. There were no barrier function changes upon application of nanoparticles. In-vitro and in-vivo results demonstrated that lecithin/chitosan nanoparticles in chitosan gel may be a promising carrier for dermal delivery of DFV in various skin disorders.

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Section: Skin Blanching Assaymentioning

confidence: 99%

Enhanced dermal delivery of diflucortolone valerate using lecithin/chitosan nanoparticles: in-vitro and in-vivo evaluations

Özcan¹,

Azizoğlu²,

Şenyiğit³

et al. 2013

IJN

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“…For example, the transdermal patch of rivastigmine has been covered by a delivery mechanism patent ( 20 ). One of the best scenarios for use patents is when the API for a drug-repositioning case is not already on the market and the new product is only approved for the new use ( 14 ).…”

Section: Discussionmentioning

confidence: 99%

“…Regarding market exclusivity benefits and intellectual property implications (in the United States and European Union), repurposing can offer valuable exclusivity for the new product by protecting its new formulation, indication, or methods of use. This is true even if the original product has already lost its active pharmaceutical ingredient (API), formulation, and/or indications’ patent protection ( 14 ). Table II provides a summary of the incentives and exclusivity protection possibilities that can be offered to a repurposed product in the United States and European Union.…”

Section: Methodsmentioning

confidence: 99%

Drug reformulations and repositioning in the pharmaceutical industry and their impact on market access: regulatory implications

Murteira

Millier

Ghezaiel

et al. 2014

Journal of Market Access & Health Policy

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BackgroundRepurposing has become a mainstream strategy in drug development, but it faces multiple challenges, amongst them the increasing and ever changing regulatory framework. This is the second study of a series of three-part publication project with the ultimate goal of understanding the market access rationale and conditions attributed to drug repurposing in the United States and in Europe. The aim of the current study to evaluate the regulatory path associated with each type of repurposing strategy according to the previously proposed nomenclature in the first article of this series.MethodsFrom the cases identified, a selection process retrieved a total of 141 case studies in all countries, harmonized for data availability and common approval in the United States and in Europe. Regulatory information for each original and repurposed drug product was extracted, and several related regulatory attributes were also extracted such as, designation change and filing before or after patent expiry, among others. Descriptive analyses were conducted to determine trends and to investigate potential associations between the different regulatory paths and attributes of interest, for reformulation and repositioning cases separately.ResultsWithin the studied European countries, most of the applications for reformulated products were filed through national applications. In contrast, for repositioned products, the centralized procedure was the most frequent regulatory pathway. Most of the repurposing cases were approved before patent expiry, and those cases have followed more complex regulatory pathways in the United States and in Europe. For new molecular entities filed in the United States, a similar number of cases were developed by serendipity and by a hypothesis-driven approach. However, for the new indication's regulatory pathway in the United States, most of the cases were developed through a hypothesis-driven approach.ConclusionThe regulations in the United States and in Europe for drug repositionings and reformulations allowed confirming that repositioning strategies were usually filed under a more complex regulatory process than reformulations. Also, it seems that parameters such as patent expiry and type of repositioning approach or reformulation affect the regulatory pathways chosen for each case.

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“…Dermal absorption studies provide information on the bioavailability of xenobiotics, pharmaceutical or cosmetic active substances by means of qualitative and quantitative measurements. The aim of such studies is the evaluation of their passage through skin for the sake of safety assessments or the optimization of cosmetic formulations towards better targeting of the active substance to a specific skin site .…”

Section: Introductionmentioning

confidence: 99%

Formulation of survival acceptor medium able to maintain the viability of skin explants over in vitro dermal experiments

Tarnowska

Briançon

Azevedo

et al. 2019

Intern J of Cosmetic Sci

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OBJECTIVE: In vitro assessments of skin absorption of xenobiotics are essential for toxicological evaluations and bioavailability studies of cosmetic and pharmaceutical ingredients. Since skin metabolism can greatly contribute to xenobiotic absorption, experiments need to be performed with skin explants kept viable in suitable survival media. Existing protocols for non-viable skin are modified to consider those conditions. The objective was to design a survival medium used as an acceptor fluid in Franz cells for testing cutaneous penetration of hydrophilic or lipophilic molecules. Their metabolism inside skin may be investigated under the same conditions. The determining factors involved in survival mechanisms in vitro are discussed. The consequences of short-term skin preservation at 4°C were also evaluated. METHODS: The metabolic activity of fresh skin samples mounted in Franz cells was studied by measurement of lactate release over 24 h in order to assess the impacts of pH, buffering, osmolality, ionic strength, initial glucose supply and the addition of ethanol or non-ionic surfactant in the acceptor part of Franz cells. CONCLUSION: Survival media must maintain physiological pH (>5.5) be isotonic with skin cells (300 mOsm kg À1 ) and contain at least 0.5 g L À1 glucose. Several compositions able to preserve skin metabolism are reported. Storage of skin explants overnight at 4°C impairs skin metabolic activity. The present work provides guidelines for designing survival media according to constraints related to the scientific requirements of the experiments.

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The development and registration of topical pharmaceuticals

Cited by 23 publications

References 14 publications

Enhanced dermal delivery of diflucortolone valerate using lecithin/chitosan nanoparticles: in-vitro and in-vivo evaluations

Enhanced dermal delivery of diflucortolone valerate using lecithin/chitosan nanoparticles: in-vitro and in-vivo evaluations

Drug reformulations and repositioning in the pharmaceutical industry and their impact on market access: regulatory implications

Formulation of survival acceptor medium able to maintain the viability of skin explants over in vitro dermal experiments

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