Topical delivery of hexamidine

Parisi, N; Paz-Alvarez, Miguel; Matts, Paul J.; Lever, Rebecca; Hadgraft, Jonathan; Lane, Majella E.

doi:10.1016/j.ijpharm.2016.04.069

Cited by 15 publications

(19 citation statements)

References 27 publications

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“…A new HPLC method was also developed for analysis of HEX H. With reference to topical delivery, HEX H has more favourable properties than HEX D, with a lower molecular weight and higher Log D value (pH 7.4). Consistent with these values, we have recently demonstrated >70% delivery of HEX H to porcine skin, in vitro, using a simple binary mixture of propylene glycol and propylene glycol monolaurate [12]. In contrast, the maximum amounts of HEX D that could be delivered were of the order of 30%.…”

Section: Hexamidine Dihydrochloridesupporting

confidence: 76%

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Hexamidine salts – applications in skin health and personal care products

Parisi¹,

Matts

Lever³

et al. 2017

Intern J of Cosmetic Sci

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Hexamidine (HEX) has been used as a preservative in topical preparations since the 1950s. A number of studies also indicate that the molecule plays a beneficial role in skin homoeostasis. In this review, we describe the physicochemical properties of hexamidine diisethionate (HEX D) and the corresponding hydrochloride salt (HEX H). The biocidal and protease inhibition properties of HEX are outlined as well as the effects of HEX on lipid processing enzymes, corneocyte maturity, stratum corneum thickness and transepidermal water loss (TEWL). Skin permeation properties of HEX D and HEX H are summarized, and formulation approaches for effective dermal targeting of HEX are discussed.

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Section: Hexamidine Dihydrochloridesupporting

confidence: 76%

“…Recently, we outlined a rational formulation approach for effective targeting of HEX D and HEX H to the skin . Based on the solubility data reported in our earlier study , propylene glycol (PG), glycerol and PEG 200 were confirmed as suitable solvents.…”

Section: Topical Delivery Of Hexamidine Salts To the Skinmentioning

confidence: 99%

Hexamidine salts – applications in skin health and personal care products

Parisi¹,

Matts

Lever³

et al. 2017

Intern J of Cosmetic Sci

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“…Although the cumulative amount of ANT that permeated was the lowest for PGML, the percentage permeation at 48 h was highest (13.1%) for this vehicle compared with the PG (0.6%) and TC (8.0%). The ability of PGML to act as a skin penetration enhancer has been reported previously (Hirata et al, 2013;Mohammed et al, 2014;Parisi et al, 2016). It has been suggested that the presence of unesterified lauric acid in PGML may contribute to increased membrane permeation.…”

Section: Accepted Manuscriptmentioning

confidence: 75%

“…If effective amounts of ANT penetrate the skin, the potential to progress the molecule as a topical chemotherapeutic agent may be explored further. As reported previously, vehicle selection was based on an assessment of solubility parameter values of various solvents and solubility determination (Parisi et al, 2016).…”

Section: Accepted Manuscriptmentioning

confidence: 99%

Topical delivery of anthramycin I. Influence of neat solvents

Haque¹,

Rahman

Thurston

et al. 2017

European Journal of Pharmaceutical Sciences

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Anthramycin (ANT) was the first pyrrolobenzodiazepine (PBD) molecule to be isolated, and is a potent cytotoxic agent. Although the PBD family has been investigated for use in systemic chemotherapy, their application in the management of actinic keratoses (AK) or skin cancer has not been investigated to date. In the present work, anthramycin (ANT) was selected as a model PBD compound, and the skin penetration of the molecule was investigated using conventional Franz diffusion cells. Finite dose permeation studies of ANT were performed using propylene glycol (PG), 1,3-butanediol (BD), dipropylene glycol (DiPG), Transcutol P® (TC), propylene glycol monocaprylate (PGMC), propylene glycol monolaurate (PGML) and isopropyl myristate (IPM). The skin penetration of BD, DiPG, PG and TC was also measured. Penetration of ANT through human skin was evident for TC, PG and PGML with the active appearing to "track" the permeation of the vehicle in the case of TC and PG. Deposition of ANT in skin could be correlated with skin retention of the vehicle in the case of IPM, PGMC and PGML. These preliminary findings confirm the ability of ANT to penetrate human skin and, given the potency of the molecule, suggest that further investigation is justified. Additionally, the findings emphasise the critical importance of understanding the fate of the excipient for the rational design of topical formulations.

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“…As for PG, a linear correlation between signal intensity of DMI and the signal intensity of NIA was found (Mohammed et al, 2014). However, in a later study, DMI had no enhancing effect on the penetration of hexamidine diisethionate nor its dihydrochloride salt across pig skin in vitro (Parisi et al, 2016). In the present work, single solvent systems of DMI resulted in cumulative permeation of NIA of 9.8 ± 2.7 μg/cm 2 , corresponding to 6.1 ± 2.1% of the applied NIA.…”

Section: Permeation Studies Using Neat Solventsmentioning

confidence: 86%

Topical delivery of niacinamide: Influence of neat solvents

Iliopoulos¹,

Sil

Hossain³

et al. 2020

International Journal of Pharmaceutics

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Niacinamide (NIA) has been widely used in cosmetic and personal care formulations for several skin conditions. Permeation of topical NIA has been confirmed in a number of studies under infinite dose conditions. However, there is limited information in the literature regarding permeation of NIA following application of topical formulations in amounts that reflect the real-life use of such products by consumers. The aim of the present work was therefore to investigate skin delivery of NIA from single solvent systems in porcine skin under finite dose conditions. A secondary aim was to probe the processes underlying the previously reported low recovery of NIA following in vitro permeation and mass balance studies. The solubility and stability of NIA in various single solvent systems was examined.The solvents investigated included Transcutol® P (TC), propylene glycol (PG), 1-2 hexanediol (HEX), 1-2 pentanediol (1-2P), 1-5 pentanediol (1-5P), 1-3 butanediol (1-3B), glycerol (GLY) and dimethyl isosorbide (DMI). Skin permeation and deposition of the molecule was investigated in full thickness porcine skin in vitro finite dose Franz-type diffusion experiments followed by mass balance studies. Stability of NIA for 72 h in the solvents was confirmed. The solubility of NIA in the solvents ranged from 82.9 ± 0.8 to 311.9 ± 4.5 mg/mL. TC delivered the highest percentage permeation of NIA at 24 h, 32.6 ± 12.1 % of the applied dose. Low total recovery of NIA after mass balance studies was observed for some vehicles, with values ranging from 55.2 ± 12.8 % to 106.3 ± 2.3 %. This reflected the formation of a number of NIA degradation by-products in the receptor phase during the permeation studies. Identification of other vehicles for synergistic enhancement of NIA skin delivery will be the subject of future work.

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Topical delivery of hexamidine

Cited by 15 publications

References 27 publications

Hexamidine salts – applications in skin health and personal care products

Hexamidine salts – applications in skin health and personal care products

Topical delivery of anthramycin I. Influence of neat solvents

Topical delivery of niacinamide: Influence of neat solvents

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