Development and in vitro evaluation of pressure sensitive adhesive patch for the transdermal delivery of galantamine: Effect of penetration enhancers and crystallization inhibition

Ameen, Dina; Michniak‐Kohn, Bozena

doi:10.1016/j.ejpb.2019.04.008

Cited by 41 publications

(16 citation statements)

References 42 publications

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“…The individual permeation profile of each drug molecule was obtained by plotting the cumulative amount of the molecule (µg) in the receptor fluid against time (h). The maximum flux value (J) at steady state (µg/cm 2 /h) represents the slope of the linear portion of the cumulative plot, (which is determined by the linear segment with the highest linearity coefficient value (R 2 ), divided by the surface area (1.77 cm 2 ) [42,58]. The enhancement ration (ER) was calculated according to the equation: ER = % permeation of molecules with MSt/% permeation of molecules without MSt All data were expressed as ± standard error of nine replicate.…”

Section: Discussionmentioning

confidence: 99%

“…This, combined with galantamine's molecular properties, high bioavailability and low daily dose requirement, make this drug an attractive candidate for transdermal drug delivery [40]. The effect of formulation factors such as enhancers and pressure sensitive adhesives for transdermal delivery of galantamine have been previously investigated [41][42][43]. However, transdermal delivery of galantamine using MSts is a novel approach.…”

Section: Introductionmentioning

confidence: 99%

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Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs

et al. 2020

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Polymer-based solid microstructures (MSts) have the potential to significantly increase the quantity and range of drugs that can be administered across the skin. MSt arrays are used to demonstrate their capacity to bypass the skin barrier and enhance permeability by creating microchannels through the stratum corneum, in a minimally invasive manner. This study is designed to demonstrate the ability of MSts to exceed the current boundaries for transdermal delivery of compounds with different molecular weights, partition coefficients, acid dissociation constants, melting points, and water solubilities. In vitro permeation of a range of selected molecules, including acetyl salicylic acid (aspirin), galantamine, selegiline hydrochloride (Sel-HCl), insulin, caffeine, hydrocortisone (HC), hydrocortisone 21-hemisuccinate sodium salt (HC-HS) and bovine serum albumin (BSA) has been studied across excised porcine skin with and without poke and patch application of MSts. Permeation of the molecules was monitored using Franz diffusion cells over 24 h. MSts significantly increased the permeation of all selected molecules up to 40 times, compared to topical applications of the molecules without MSts. The greatest increase in permeation was observed for caffeine with 70 ± 8% permeation and the lowest enhancement was observed for HC with a 2.4 ± 1.3% increase in permeation. The highest obtained flux was BSA (8133 ± 1365 μg/cm2/h) and the lowest flux observed for HC (11 ± 4 μg/cm2/h). BSA and HC also showed the highest (16,275 ± 3078 μg) and the lowest (73 ± 47 μg) permeation amount after 24 h respectively. MSt-treated skin exhibits greatly increased permeation. The molecule parameters (size, acid dissociation constant, partition coefficient and solubility)—traditional hurdles associated with passive diffusion through intact skin—are overcome using MSt skin treatment.

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Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs

et al. 2020

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“…All drug release profiles from DT53, the least retentive copolymer, follow the Peppas-Sahlin equation, a combination of burst-erosion (oversaturated drug proportion) and diffusion (dissolved drug). In addition to these solubilization properties of the polymer, the interaction of -COOH functional groups with amine-containing compounds through hydrogen bonding (23) has influenced the rate and extent of in vitro release of ROP, but not the kinetic mechanism.…”

Section: Descriptive Equations Of the Release Mechanismmentioning

confidence: 99%

Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables

Paterna-Paterna¹,

Miñarro-Carmona²,

Dolors³

et al. 2022

AAPS PharmSciTech

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The aim of this study is to evaluate the cooperative interactions between formulation variables of ropinirole transdermal patches and characterize the effects of drug loading and crystallinity, degree of ionization and drug-polymer solubilization, functionalization of acrylate polymeric basis, and the addition of permeation enhancers over the release profiles. Several series of transdermal films based on carboxylic or hydroxylic acrylates (DuroTak®) and containing 1 to 10% ropinirole hydrochloride were laminated by mold-casting and evaporation. Formulations were characterized for crystallinity, drug particle size, drug assay, and residual solvents. Release profiles were obtained at different drug ionization state using paddle over disk apparatus. Mechanisms were elucidated with nonlinear data fitting of relevant release equations. Fickian and erosion processes were evaluated with the Peppas–Sahlin equation, and burst release risks were estimated as an independent term added to Higuchi kinetics. X-ray diffraction and microscopy evidenced differences in drug-polymer solubilization and density of drug crystals. Concerning drug release, area under the curve of dissolved quantities and release percentage were discriminant variables in mutual influence. Peppas–Shalin equation was the majority descriptor of release suggesting a combination of Fickian and erosion processes, revealing a decrease in the Fickian component as drug loading increased. Major burst release risks were evidenced mostly with Higuchi kinetics with vinylacetate acrylates. The carboxylic polymer without vinylacetate provided the best release extent, being more highly efficient as lower the drug loading was. Permeation enhancers with carboxylic or aliphatic radicals have, additionally, modified the release properties of ropinirole. Chemical interactions between the drug and acrylic polymers have been demonstrated. Only the effect with carboxylic polymer is pH dependent. The vinyl acetate comonomer reduces the drug release rate most effectively in formulations with low drug loads. The acrylic polymers without vinylacetate achieved the highest drug solubilization and thus the highest degree of release, providing a release of approximately 15% of the drug load.

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“…At pH10, the tertiary amine of RP is not ionized and, conversely, it is fully ionized at pH6. In addition to the solubilisation properties of the polymer, and based on the interaction of -COOH functional groups with amine-containing compounds through hydrogen bonding [15], the influence of pH becomes useful to modulate the rate and extent of its in vitro release.…”

Section: Descriptive Equations Of Ropinirole Release From the Formulationsmentioning

confidence: 99%

Release of Ropinirole from Acrylate-Vinylacetate Transdermal Formulations: Modulation Based on Polymer-Drug Interactions

Paterna-Paterna

Miñarro-Carmona

Grau

et al. 2020

The 1st International Electronic Conference on Pharmaceutics

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Optimization of transdermal formulations requires solving simultaneous challenges as the selection of release polymers. The interactions between the formulation components must be taken as a way to modulate its performance. Selection of acrylic polymers with different functionalizations for the transdermal formulation of a tertiary amine drug (ropinirole HCl) have been investigated. Aim of this work is to characterize the influence over drug release of certain experimental interactions. Solubility-crystalization and pharmacopoeial release tests have been used to evaluate the influence of drug loading and the pH of the release media. Area under the curve of dissolved amounts and percentage of release have been used as discriminant variables in mutual influence with the physical state of the drug. Elucidation of release mechanisms has been performed with data fitting of relevant modelystic equations. Fickian release and erosion contribution have been related with drug loading and the risk of burst effects. In conclusion, a rationale to select the best suitable polymer for ropinirole HCl has been demonstrated in terms of efficiency and extent of release.

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Development and in vitro evaluation of pressure sensitive adhesive patch for the transdermal delivery of galantamine: Effect of penetration enhancers and crystallization inhibition

Cited by 41 publications

References 42 publications

Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs

Characterisation of Drug Delivery Efficacy Using Microstructure-Assisted Application of a Range of APIs

Release of Ropinirole in Acrylate Transdermal Patches: Mutual Interactions Between Formulation Variables

Release of Ropinirole from Acrylate-Vinylacetate Transdermal Formulations: Modulation Based on Polymer-Drug Interactions

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