Characterization of piroctone olamine for topical delivery to the skin / Chun Fung Tang in INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Vol. 45, N° 3 (06/2023)  

[article]  inINTERNATIONAL JOURNAL OF COSMETIC SCIENCE > Vol. 45, N° 3 (06/2023) . - p. 345-353 Titre : Characterization of piroctone olamine for topical delivery to the skin Type de document : document électronique Auteurs : Chun Fung Tang, Auteur ; Miguel Paz-Alvarez, Auteur ; Paul D. A. Pudney, Auteur ; Majella E. Lane, Auteur Année de publication : 2023 Article en page(s) : p. 345-353 Note générale : Bibliogr. Langues : Anglais (eng) Catégories : Antifongiques Antipelliculaires Caractérisation Chimie analytique Cuir chevelu -- Soins et hygiène Dermo-cosmétologie Formulation (Génie chimique) Ingrédients cosmétiques Piroctone olamine Solubilité Stabilité chimique Index. décimale : 668.5 Parfums et cosmétiques Résumé : - Objective : Dandruff and its more severe related condition, seborrheic dermatitis affects a high proportion of the population at some point in their life. Piroctone olamine, also known as Octopirox® (OPX) is the monoethanolamine salt of piroctone and is an antifungal agent widely used for the management of dandruff. The aim of the present work was to characterize the physicochemical properties of piroctone olamine and to conduct pre-formulation studies for the development of novel topical formulations of this active. - Methods : An HPLC method was developed and validated for the analysis of OPX. The melting point was determined using the DSC Q2000 (TA Instruments, USA). The distribution coefficient (logD(O/PBS)) and partition coefficient (log Po/w) was determined in phosphate-buffered saline (PBS) AND deionized (DI) water using the shake flask method. All experiments were performed at room temperature. The solubility was determined experimentally by adding amount of active to a solvent. The samples were kept at 32° ± 1°C for 48 h in a water bath. The stability of the compound was determined in a range of solvents by preparing solutions of 1 mg mL-1 in the relevant solvents. These solutions were kept and stirred throughout the experiment at 32 ± 1°C, and aliquots were taken at 24, 48 and 96 h. - Results : The HPLC method was developed successfully; however, samples at the lower end of the calibration curve showed lower degrees of precision and accuracy. Based on experiments with DSC, the melting point was observed at an onset temperature of 132.4°C. The LogD was determined to be 1.84. The compound had the highest solubility in methanol (278.4 mg mL-1) and propylene glycol (PG), with a value of 248.8 mg mL-1. The lowest solubility for OPX was in dimethyl isosorbide (9.9 mg mL-1), Labrafacâ„¢ (3.6 mg mL-1) and isostearyl isostearate (0.5 mg mL-1). Over the 4 days, OPX showed stability in ethanol and PG, while a notable decrease in OPX was observed in PBS and DI water at 32 ± 1°C. - Conclusion : The physicochemical properties of OPX were characterized to find suitable excipients able to target the epidermis for topical delivery. Building on these findings, future work will focus on the development of novel topical formulation of OPX. Note de contenu : - MATERIALS AND METHODS : Materials - Melting point calculation - HPLC/LC–MS method for OPX - Distribution and partition coefficient determination (log Do/PBS, log Po/w) - Solubility and stability studies - RESULTS AND DISCUSSION : Melting point - OPX HPLC method validation - Distribution and partition coefficient determination (log DO/PBS, log PO/W) - Solubility and stability studies - Table 1 : Mobile phase gradient for the detection of OPX - Table 2 : HPLC method validation results for quantitative analysis of OPX. Mean ± SD, precision expressed in RSD% - Table 3 : Experimental values for log D(O/PBS) and log P(O/W) of OPX DOI : https://doi.org/10.1111/ics.12839 En ligne : https://drive.google.com/file/d/1a6TU2ieHdyBPASNWW_rSB9b4UnPHR-Am/view?usp=drive [...] Format de la ressource électronique : Pdf Permalink : https://e-campus.itech.fr/pmb/opac_css/index.php?lvl=notice_display&id=39565 [article]

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Investigation of piroctone olamine delivery to the skin from single, binary and ternary solvent systems / Chun Fung Tang in INTERNATIONAL JOURNAL OF COSMETIC SCIENCE, Vol. 46, N° 3 (06/2024)  

[article]  inINTERNATIONAL JOURNAL OF COSMETIC SCIENCE > Vol. 46, N° 3 (06/2024) . - p. 357-367 Titre : Investigation of piroctone olamine delivery to the skin from single, binary and ternary solvent systems Type de document : texte imprimé Auteurs : Chun Fung Tang, Auteur ; Paul D. A. Pudney, Auteur ; Majella E. Lane, Auteur Année de publication : 2024 Article en page(s) : p. 357-367 Note générale : Bibliogr. Langues : Anglais (eng) Catégories : Antipelliculaires Cosmétiques Cosmétiques -- Administration par voie cutanée Cuir chevelu -- Soins et hygiène Dermo-cosmétologie Formulation (Génie chimique) Pellicules (dermatologie) Perméation Piroctone olamine Produits capillaires solvants Index. décimale : 668.5 Parfums et cosmétiques Résumé : - OBJECTIVE : Disruption of the protective stratum corneum barrier increases the skin's vulnerability to microorganisms and facilitates conditions such as dandruff. Dandruff is a disorder of the scalp that causes increased scaling of the SC and is associated with Malassezia fungus. Consequently, many anti-dandruff commercial products use anti-fungal active ingredients such as piroctone olamine also known as Octopirox (OPX). OPX is an active ingredient used in a number of topical preparations for the management of dandruff. The characterization of the physicochemical properties of OPX was previously reported. The aim of the present work was to investigate a range of solvent systems for their effects on OPX interaction with human skin. - METHODS : The solvents used in this study were propylene glycol (PG), diethylene glycol monoethyl ether or Transcutol® (TC), PG monolaurate (PGML), isopropyl myristate (IPM), caprylic/capric triglyceride or Labrafacâ„¢ Lipophile WL 1349 (LAB), PG caprylate or Capryol® 90 (CAP), isostearyl isostearate (ISIS) and Plurol® Oleique CC 497 (PIOI). The single solvent systems evaluated were PG, TC, PGML, IPM, ISIS and CAP. For the binary solvent systems, PG and TC were examined. Ternary solvent systems consisted of: PG, TC and LAB; PG, PGML and LAB; and PG, TC and IPM. The concentration of OPX used was 1% (w/v). Heat-separated human epidermis was used for 24 h permeation experiments performed under finite dose conditions; mass balance studies were also conducted. - RESULTS : For the six single solvents examined no permeation was evident. Skin permeation of OPX was observed for binary and ternary solvent systems. The highest permeation for all PG:TC binary solvent system ratios tested was from the PG:TC (75:25) system. For the ternary solvent systems investigated, highest cumulative permeation of OPX was observed for PG:PGML:LAB (60:30:10). Considering all systems, PG:TC (75:25) delivered the greatest amount of OPX through the skin. Although OPX is deposited in the skin following the application of neat solvents, higher skin retention values were generally observed for binary and ternary systems. - CONCLUSION : To our knowledge, this is the first study to examine the permeation behaviour of OPX for a range of single, binary and ternary solvent systems. Note de contenu : - MATERIALS AND METHODS : Materials - Solubility studies and solubility parameter calculation - In vitro permeation experiments - Mass balance studies - High-performance liquid chromatography analysis - Statistical analysis - RESULTS AND DISCUSSION : Solubility parameter of single, binary and ternary solvent systems - Single solvent systems - Binary solvent systems - Ternary solvent systems DOI : https://doi.org/10.1111/ics.12935 En ligne : https://drive.google.com/file/d/1Wgn22cWyxcqjXAg9dHLP1fLp_udsevx_/view?usp=drive [...] Format de la ressource électronique : Pdf Permalink : https://e-campus.itech.fr/pmb/opac_css/index.php?lvl=notice_display&id=41338 [article]

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