Effects of propylene glycol diesters of caprylic and capric acids (Miglyol® 840) and ethanol binary systems on in vitro skin permeation of drugs

Mahjour, Majid; Mauser, Bernadette E.; Rashidbaigi, Z.; Fawzi, Mahdi B.

doi:10.1016/0378-5173(93)90403-3

Cited by 17 publications

(8 citation statements)

References 18 publications

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“…Skin irritation was not observed in either of the three subjects tested. Similar results were reported when a fourth subject (male) was tested with a 95% ethanol:Propylene Glycol Dicaprylate/Dicaprate mixture (40:60) according to the same procedure (Mahjour et al 1993).…”

Section: Skin Irritationsupporting

confidence: 80%

“…Other names for this mixture include: Decanoic Acid, 1-Methyl-1,2-Ethanediyl Ester mixed with 1-Methyl-1,2-Ethanediyl Dioctanoate; Decanoic Acid, Mixed Diesters with Octanoic Acid and Propylene Glycol ; Caprylic, Capric Acid, Propylene Glycol Diester; Propylene Glycol Dicaprate-Caprate; and Propylene Glycol, Caprylate Caprate Diester (Wenninger and McEwen 1997;Chemline 1995). Propylene Glycol Dicaprylate/Dicaprate has also been defined as the propylene glycol diester of saturated vegetable acids (C8-ClO chain length) that contains 65 to 80% caprylic acid and 15 to 30% capric acid (Mahjour et al 1993).…”

Section: Propylene Glycol Dicaprylate/dicapratementioning

confidence: 99%

See 1 more Smart Citation

Final Report on the Safety Assessment of Propylene Glycol (PG) Dicaprylate, PG Dicaprylate/Dicaprate, PG Dicocoate, PG Dipelargonate, PG Isostearate, PG Laurate, PG Myristate, PG Oleate, PG Oleate SE, PG Dioleate, PG Dicaprate, PG Diisostearate, and PG Dilaurate

Johnson¹

1999

Int J Toxicol

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The Propylene Glycol Dicaprylate family of ingredients includes several esters and diesters of Propylene Glycol and fatty acids. These ingredients are used in cosmetic formulations as skin conditioning agents, viscosity increasing agents, and surfactants. Two skin irritation studies (minimal to no irritation) and a comedogenicity study (insignificant comedogen) on Propylene Glycol Dicaprylate/Dicaprate and a skin irritation study (slight) and an acute oral toxicity study (nontoxic) on Propylene Glycol Laurate were available. Available data were also found indicating that Propylene Glycol Dicaprylate/Dicaprate and Propylene Glycol Dipelargonate may enhance the skin penetration of other chemicals. Because of the ability of these Polyethylene Glycol esters and diesters to enhance penetration of other agents, it was recommended that care be taken in using these and other Polyethylene Glycol esters and diesters in cosmetic products. Previous Cosmetic Ingredient Review safety assessments of related ingredients, including Polyethylene Glycol, Polyethylene Glycol Stearate, Coconut Oils and Acids, Isostearic Acid, Lauric Acid, Myristic Acid, Oleic Acid, and Caprylic/Capric Triglyceride, were summarized. Included were mutagenicity, chronic toxicity, and skin irritation and sensitization data. Based in part on the limited data available on the ingredients included in the report, but more so on the previous reviews of chemically similar moieties, it was concluded that Propylene Glycol Dicaprylate, Propylene Glycol Dicaprylate/Dicaprate, Propylene Glycol Dicocoate, Propylene Glycol Dipelargonate, Propylene Glycol Isostearate, Propylene Glycol Laurate, Propylene Glycol Myristate, Propylene Glycol Oleate, Propylene Glycol Oleate SE, Propylene Glycol Dioleate, Propylene Glycol Dicaprate, Propylene Glycol Diisostearate, and Propylene Glycol Dilaurate are safe for use as cosmetic ingredients in the present practices of use.

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Section: Skin Irritationsupporting

confidence: 80%

Section: Propylene Glycol Dicaprylate/dicapratementioning

confidence: 99%

Final Report on the Safety Assessment of Propylene Glycol (PG) Dicaprylate, PG Dicaprylate/Dicaprate, PG Dicocoate, PG Dipelargonate, PG Isostearate, PG Laurate, PG Myristate, PG Oleate, PG Oleate SE, PG Dioleate, PG Dicaprate, PG Diisostearate, and PG Dilaurate

Johnson¹

1999

Int J Toxicol

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“…The three mAbs (formulated at 100 mg/mL with 50 mg/mL trehalose) were spray dried using a bench‐top spray dryer and a pilot‐scale spray dryer (Table 1). Comparable outlet temperatures of 87°C–89°C were employed for all samples because outlet temperature was considered the key parameter dictating the spray‐drying capability 30–34. The pilot‐scale unit demonstrated better performance in powder collection yield (>96%) and water content (4%–5%), whereas the samples dried by the bench‐top unit had 60% yield and 7%–9% water content.…”

Section: Resultsmentioning

confidence: 99%

Investigating High-Concentration Monoclonal Antibody Powder Suspension in Nonaqueous Suspension Vehicles for Subcutaneous Injection

Bowen

Armstrong

Maa

2012

Journal of Pharmaceutical Sciences

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“…Due to low water solubility, the test compounds were prepared in an ethanol-Miglyol 840 (1:9) vehicle, a solution that has been used for permeation studies with poorly soluble drugs (70). After 1 h, 1.14 ml of a 100-g/ml donor solution was applied on the model skin using a positive-displacement pipette.…”

Section: Analysis Of Test Compounds In Biological Samples (I) Skin Tmentioning

confidence: 99%

Topical Treatment for Cutaneous Leishmaniasis: Dermato-Pharmacokinetic Lead Optimization of Benzoxaboroles

Bocxlaer

Gaukel

Hauser

et al. 2018

Antimicrob Agents Chemother

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Cutaneous leishmaniasis (CL) is caused by several species of the protozoan parasite , affecting an estimated 10 million people worldwide. Previously reported strategies for the development of topical CL treatments have focused primarily on drug permeation and formulation optimization as the means to increase treatment efficacy. Our approach aims to identify compounds with antileishmanial activity and properties consistent with topical administration. Of the test compounds, five benzoxaboroles showed potent activity (50% effective concentration [EC] < 5 μM) against intracellular amastigotes of at least one species and acceptable activity (20 μM< EC < 30 μM) against two more species. Benzoxaborole compounds were further prioritized on the basis of the evaluation of progression criteria related to skin permeation, such as the partition coefficient and solubility. An MDCKII-hMDR1 cell assay showed overall good permeability and no significant interaction with the P-glycoprotein transporter for all substrates except LSH002 and LSH031. The benzoxaboroles were degraded, to some extent, by skin enzymes but had stability superior to that of-hydroxybenzoate compounds, which are known skin esterase substrates. Evaluation of permeation through reconstructed human epidermis showed LSH002 to be the most permeant, followed by LSH003 and LSH001. Skin disposition studies following finite drug formulation application to mouse skin demonstrated the highest permeation for LSH001, followed by LSH003 and LSH002, with a significantly larger amount of LSH001 than the other compounds being retained in skin. Finally, the efficacy of the leads (LSH001, LSH002, and LSH003) against was tested LSH001 suppressed lesion growth upon topical application, and LSH003 reduced the lesion size following oral administration.

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Effects of propylene glycol diesters of caprylic and capric acids (Miglyol® 840) and ethanol binary systems on in vitro skin permeation of drugs

Cited by 17 publications

References 18 publications

Final Report on the Safety Assessment of Propylene Glycol (PG) Dicaprylate, PG Dicaprylate/Dicaprate, PG Dicocoate, PG Dipelargonate, PG Isostearate, PG Laurate, PG Myristate, PG Oleate, PG Oleate SE, PG Dioleate, PG Dicaprate, PG Diisostearate, and PG Dilaurate

Final Report on the Safety Assessment of Propylene Glycol (PG) Dicaprylate, PG Dicaprylate/Dicaprate, PG Dicocoate, PG Dipelargonate, PG Isostearate, PG Laurate, PG Myristate, PG Oleate, PG Oleate SE, PG Dioleate, PG Dicaprate, PG Diisostearate, and PG Dilaurate

Investigating High-Concentration Monoclonal Antibody Powder Suspension in Nonaqueous Suspension Vehicles for Subcutaneous Injection

Topical Treatment for Cutaneous Leishmaniasis: Dermato-Pharmacokinetic Lead Optimization of Benzoxaboroles

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