Effect of penetration enhancers on the phase transition of multilamellar liposomes of dipalmitoylphosphatidylcholine. A study by differential scanning calorimetry

Rolland, Alain; Brzokewicz, Alain; Shroot, Braham; Jamoulle, Jean-Claude

doi:10.1016/0378-5173(91)90274-r

Cited by 30 publications

(13 citation statements)

References 22 publications

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“…The CUP parameter (which is very sensitive to the presence of ligands) for this system is also not statistically distinguishable from that of the DMPC control. These observations are in direct contrast to those reported by Rolland et al (31,32) for a preparation using DMPC that had been dissolved with Azone in chloroform, the chloroform then removed, and the DMPCAzone film that remained resuspended in buffer. These observations suggest that Azone may not transfer to the DMPC preparation in any appreciable quantity on the time scale of these experiments.…”

Section: (Eq 6)contrasting

confidence: 55%

Mechanistic studies on percutaneous penetration enhancement by N-(4-halobenzoyl)-S,S-dimethyliminosulfuranes

Чандрасекаран

Heerklotz

Henary

et al. 2005

Journal of Lipid Research

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Halogen-substituted iminosulfuranes are transdermal penetration enhancers (TPEs) in permeation studies using hairless mouse or human cadaver skin. The interaction of N -(4-R -benzoyl)-S,S -dimethyliminosulfuranes 1-4, where R ‫؍‬ H, Cl, Br, and I, with l -␣ -dimyristoyl-sn -glycero-3-phosphocholine (DMPC) has been studied using differential scanning calorimetry, isothermal titration calorimetry, nuclear Overhauser effect spectroscopy (NOESY), and NMR spectroscopy, and by calculation of the iminosulfurane polarizabilities in order to elucidate the molecular basis of the TPE activity. The active compounds reduce the melting temperature of the gel-to-liquid-crystal phase transition and induce multiple components in the transition excess heat capacity profile. The partitioning of the bromo derivative 3, the most active compound, into DMPC is unique in that 3 may be trapped in the bilayer, affording an enhanced residence time and a reason for its high TPE activity. The entropy decrease associated with the transfer of 3 to the bilayer is much lower than that for the other compounds, indicating that 3 occupies or induces sites that afford it considerable local motional freedom. Correlations between the iminosulfurane TPE activities, the partition coefficients, and NOESY crosspeak volume were observed. Molecular polarizabilities are not consistent with a TPE mode of action involving interaction of these agents with protein side chains.

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Section: (Eq 6)contrasting

confidence: 55%

Mechanistic studies on percutaneous penetration enhancement by N-(4-halobenzoyl)-S,S-dimethyliminosulfuranes

Чандрасекаран

Heerklotz

Henary

et al. 2005

Journal of Lipid Research

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“…[64][65][66][67] In this study, DSC was employed to further understand the interaction of the selected membrane additives with the niosome-forming surfactant (Span 60) and monitor their effects on the gel/ liquid transition of the prepared vesicles. Cholesterol can abolish gel/liquid phase transition of niosomes at 1:1 molar ratio.…”

Section: Resultsmentioning

confidence: 99%

Design and Evaluation of Controlled-Release Niosomes and Discomes for Naltrexone Hydrochloride Ocular Delivery

Abdelkader

Ismail

Kamal

et al. 2011

Journal of Pharmaceutical Sciences

157

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“…A saturated alkyl chain with 10 to 20 atoms attached to polar groups causes appearance of strong effect of dermal absorption by fatty acid. These compounds change configuration structure of lipid chains, induce disorder, and decrease phase transition temperature of gel-liquid crystal (23-25). Propylene glycol was used as co-solvent for aminophylline in all gel formulations.…”

Section: Discussionmentioning

confidence: 99%

Effects of Various Penetration Enhancers on Penetration of Aminophylline Through Shed Snake Skin

Kouchak

Handali

2014

Jundishapur J Nat Pharm Prod

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Background:Cellulite is the accumulation of subcutaneous fat and connective tissue in tights and buttocks. Xanthines, such as aminophylline, are used as phosphodiesterase inhibitors, and are also adenosine receptor antagonists. Objectives: The aim of the present study was to characterize in vitro aminophylline transdermal absorption through shed snake skin, and to investigate the absorption enhancing effect of various enhancers. Materials and Methods: Aminophylline gels were prepared using theophylline and ethylenediamine as raw materials of aminophylline, hydroxypropyl methyl cellulose (HPMC) F4M as gelling agent, and propylene glycol as a co-solvent. Sodium tauroglycocholate (STGC) (100, 200, and 500 μg/mL), lauric acid (1.7 and 15%), and ethanol (60%) were added as enhancers. In vitro percutaneous absorption experiments were performed on snake skin using Franz diffusion cells. Flux (J), permeability coefficient (P), and enhancement factor (EF) for each formulation were calculated. Results:The results indicated that all of enhancers significantly enhanced drug permeability. This effect was decreased by increasing the concentration of STGC; in contrast, by increasing the concentration of lauric acid from 1.7 to 15%, EF was enhanced Although ethanol (60%) and STGC (100 μg/mL) showed the highest EFs, the effect of ethanol on drug permeability appeared with a lag time. Conclusions: According to the findings, type and concentration of penetration enhancers can effect on transdermal permeation of drug.

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Effect of penetration enhancers on the phase transition of multilamellar liposomes of dipalmitoylphosphatidylcholine. A study by differential scanning calorimetry

Cited by 30 publications

References 22 publications

Mechanistic studies on percutaneous penetration enhancement by N-(4-halobenzoyl)-S,S-dimethyliminosulfuranes

Mechanistic studies on percutaneous penetration enhancement by N-(4-halobenzoyl)-S,S-dimethyliminosulfuranes

Design and Evaluation of Controlled-Release Niosomes and Discomes for Naltrexone Hydrochloride Ocular Delivery

Effects of Various Penetration Enhancers on Penetration of Aminophylline Through Shed Snake Skin

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