Synergetic effects of isopropyl alcohol (IPA) and isopropyl myristate (IPM) on the permeation of betamethasone-17-valerate from semisolid Pharmacopoeia bases

Mitriaikina, S.; Müller‐Goymann, Christel C.

doi:10.1016/s1773-2247(07)50052-3

Cited by 10 publications

(7 citation statements)

References 61 publications

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“…Additionally, several studies in the scientific literature have reported that combinations of solvents with differing physicochemical properties resulted in synergistic enhancement of drug permeation [ 58 , 59 , 60 , 61 , 62 , 63 ]. Brinkmann and Muller-Goymann (2003) investigated the effect of isopropanol (IPA) and a long-chain fatty acid ester, namely isopropyl myristate (IPM), on the permeation of hydrocortisone (HC) across isolated human SC [ 64 ].…”

Section: Resultsmentioning

confidence: 99%

Dermal Delivery of Diclofenac Sodium—In Vitro and In Vivo Studies

Iliopoulos¹,

Goh

Haque³

et al. 2022

Pharmaceutics

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Previously, we reported the use of confocal Raman spectroscopy (CRS) as a novel non-invasive approach to determine drug disposition in the skin in vivo. Results obtained by CRS were found to correlate with data from the well-established in vitro permeation test (IVPT) model using human epidermis. However, these studies used simple vehicles comprising single solvents and binary or ternary solvent mixtures; to date, the utility of CRS for monitoring dermal absorption following application of complex marketed formulations has not been examined. In the present work, skin delivery of diclofenac sodium (DFNa) from two topical dermatological drug products, namely Diclac® Lipogel 10 mg/g and Primofenac® Emulsion gel 1%, was determined by IVPT and in vivo by both CRS and tape stripping (TS) methodologies under similar experimental conditions. The in vivo data were evaluated against the in vitro findings, and a direct comparison between CRS and TS was performed. Results from all methodologies showed that Diclac promoted significantly greater DFNa delivery to the skin (p < 0.05). The cumulative amounts of DFNa which permeated at 24 h in vitro for Diclac (86.5 ± 9.4 µg/cm2) were 3.6-fold greater than the corresponding amounts found for Primofenac (24.4 ± 2.7 µg/cm2). Additionally, total skin uptake of DFNa in vivo, estimated by the area under the depth profiles curves (AUC), or the signal intensity of the drug detected in the upper stratum corneum (SC) (4 µm) ranged from 3.5 to 3.6-fold greater for Diclac than for Primofenac. The shape of the distribution profiles and the depth of DFNa penetration to the SC estimated by CRS and TS were similar for the two methods. However, TS data indicated a 4.7-fold greater efficacy of Diclac relative to Primofenac, with corresponding total amounts of drug penetrated, 94.1 ± 22.6 µg and 20.2 ± 7.0 µg. The findings demonstrate that CRS is a methodology that is capable of distinguishing skin delivery of DFNa from different formulations. The results support the use of this approach for non-invasive evaluation of topical products in vivo. Future studies will examine additional formulations with more complex compositions and will use a wider range of drugs with different physicochemical properties. The non-invasive nature of CRS coupled with the ability to monitor drug permeation in real time offer significant advantages for testing and development of topical dermatological products.

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Section: Resultsmentioning

confidence: 99%

Dermal Delivery of Diclofenac Sodium—In Vitro and In Vivo Studies

Iliopoulos¹,

Goh

Haque³

et al. 2022

Pharmaceutics

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“…The same group later applied DSC analysis for HSC samples treated with wool fat alcohol ointment and basic cream DAC (German Drug Code) containing 0.1%w/v of betamethasone-17-valerate and two penetration enhancers (isopropyl alcohol (5%w/v) and isopropyl myristate (5%w/v)) (Mitriaikina and Muller-Goymann, 2007). For ointmenttreated samples, the incorporation of individual penetration enhancers greatly reduced the T2 an T3 transitions than the ointment alone.…”

Section: Applications Of Dsc In Advancing Topical and Transdermal Dru...mentioning

confidence: 99%

“…The treatment period with excipients or formulations varying from 30 min to 48 h has been reported. The time shall be determined based on the purpose of studies but several reports have showed the same effect can be studied by just incubating SC samples with only 30 min at room temperature (Mitriaikina and Muller-Goymann, 2007;Winkler and Müller-Goymann, 2005). Hydration of the SC with 20 -40% of water content is recommended especially for HSC prior to the treatment to mimic the in vivo hydration level of the SC (Potts, 1986) and allow better detection of the related transitions.…”

Section: Considerations For Thermal Characterisation Of Sc Samplesmentioning

confidence: 99%

Thermal analysis of mammalian stratum corneum using differential scanning calorimetry for advancing skin research and drug delivery

Goh

Hadgraft

Lane³

2022

International Journal of Pharmaceutics

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“…15 However, the exact mechanism of action of these penetration enhancers is not clear. 16,17 For example, it has been reported that when Dimethyl Sulfoxide (DMSO) was used as a penetration enhancer it shows three different mechanisms of action on the cell membrane based on its concentration. At the lower concentrations (2.5-7.5 mol %), it induces the expansion and thinning of the lipid bilayer, thereby increasing the fluidity of the hydrophobic region of the membrane.…”

Section: Introductionmentioning

confidence: 99%

“…18 The reorientation of lipid head groups minimizes the free energy of the system, which results in pore formation in the skin surface. [15][16][17] However, at the higher concentrations (25-100 mol%), DMSO can extract lipid molecules and disintegrate the lipid layer in SC. [19][20][21] The purpose of this study was to design a transdermal delivery system of TC for hormonal therapy of breast cancer.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Tamoxifen Citrate Loaded Transdermal Reservoir Gel Drug Delivery Systems

Sreeharsha¹,

Hiremath²,

Rawre³

et al. 2019

IJPER

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Background: Successful treatment of cancer is yet remained as a challenging concern in public health. Transdermal delivery of hormonal therapy offers several advantages over the oral route associated with potential side effects. Methods: The present investigation preparation and screening of rate controlling membranes using Eudragit release liners of RS 100, hydroxyl propyl methyl cellulose K4M (HPMC K4M) and ethyl cellulose by plate casting method and their physicochemical characterization. The prepared release liners were subjected for preformualtion studies (thickness, weight variation, moisture uptake, folding endurance and moisture loss). Tamoxifen citrate is an ideal molecule for the transdermal reservoir for the preparation of gel dosage form due its dosage regimen. Results: The main investigation, topical gel TC was prepared using HPMC K4M and Carbopol 934 as gelling agents in different proportions with Dimethyl Sulfoxide (DMSO) as a penetration enhancer. TC gels were subjected for the physicochemical parameters such as pH, viscosity, spreadability. Conclusion: The TC gel diffusion was conducted by using rate controlling membranes (release liner). The TC gel skin permeation was investigated by using excised rat skin as a barrier.

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Synergetic effects of isopropyl alcohol (IPA) and isopropyl myristate (IPM) on the permeation of betamethasone-17-valerate from semisolid Pharmacopoeia bases

Cited by 10 publications

References 61 publications

Dermal Delivery of Diclofenac Sodium—In Vitro and In Vivo Studies

Dermal Delivery of Diclofenac Sodium—In Vitro and In Vivo Studies

Thermal analysis of mammalian stratum corneum using differential scanning calorimetry for advancing skin research and drug delivery

Formulation and Evaluation of Tamoxifen Citrate Loaded Transdermal Reservoir Gel Drug Delivery Systems

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