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Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design

Purpose: Kojic acid (KA) a natural metabolite and its dipalmitate ester, kojic acid dipalmitate(Kadp) are both prescribed to treat skin hyperpigmentation. Stress test reveals the intrinsicstability of active ingredients and leads to selection of the suitable formulations. This researchevaluates the...

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Autores principales: Tazesh, Sahar, Tamizi, Elnaz, Siahi Shadbad, Mohammadreza, Mostaghimi, Nazli, Monajjemzadeh, Farnaz
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Tabriz University of Medical Sciences 2022
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9106968/
https://www.ncbi.nlm.nih.gov/pubmed/35620332
http://dx.doi.org/10.34172/apb.2022.031
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author Tazesh, Sahar
Tamizi, Elnaz
Siahi Shadbad, Mohammadreza
Mostaghimi, Nazli
Monajjemzadeh, Farnaz
author_facet Tazesh, Sahar
Tamizi, Elnaz
Siahi Shadbad, Mohammadreza
Mostaghimi, Nazli
Monajjemzadeh, Farnaz
author_sort Tazesh, Sahar
collection PubMed
description Purpose: Kojic acid (KA) a natural metabolite and its dipalmitate ester, kojic acid dipalmitate(Kadp) are both prescribed to treat skin hyperpigmentation. Stress test reveals the intrinsicstability of active ingredients and leads to selection of the suitable formulations. This researchevaluates the comparative stability of KA and its di-palmitate ester under liquid oxidative stress. Methods: The HPLC-UV/PDA method with a C(18) column was utilized. Liquid oxidative stresswas induced using hydrogen peroxide (H(2)O(2)). Degradation was separately induced for eachdrug, and they were compared to each other. Results: Kadp degraded more rapidly in similar liquid oxidative stress conditions than KA did.The superior degradation model was the first order for both drugs based on the mean percentage error (MPE) values, indicating the dependency of the reaction rate on the initial concentrationof the reactive substance. Ring opening was proposed as the most possible theory for KA andKadp oxidative degradation. Conclusion: It is suggested to use KA instead of Kadp in less stable formulations, such asextemporaneous preparations. The incorporation of antioxidant excipients in Kadp formulationsis recommended for yielding better stability results. Formulating Kadp in the internal phase ofo/w emulsion formulations may protect this susceptive molecule from oxidative degradationduring the shelf life of the pharmaceutical preparation. Further studies are required to study theexact mechanism of the degradation process.
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spelling pubmed-91069682022-05-25 Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design Tazesh, Sahar Tamizi, Elnaz Siahi Shadbad, Mohammadreza Mostaghimi, Nazli Monajjemzadeh, Farnaz Adv Pharm Bull Research Article Purpose: Kojic acid (KA) a natural metabolite and its dipalmitate ester, kojic acid dipalmitate(Kadp) are both prescribed to treat skin hyperpigmentation. Stress test reveals the intrinsicstability of active ingredients and leads to selection of the suitable formulations. This researchevaluates the comparative stability of KA and its di-palmitate ester under liquid oxidative stress. Methods: The HPLC-UV/PDA method with a C(18) column was utilized. Liquid oxidative stresswas induced using hydrogen peroxide (H(2)O(2)). Degradation was separately induced for eachdrug, and they were compared to each other. Results: Kadp degraded more rapidly in similar liquid oxidative stress conditions than KA did.The superior degradation model was the first order for both drugs based on the mean percentage error (MPE) values, indicating the dependency of the reaction rate on the initial concentrationof the reactive substance. Ring opening was proposed as the most possible theory for KA andKadp oxidative degradation. Conclusion: It is suggested to use KA instead of Kadp in less stable formulations, such asextemporaneous preparations. The incorporation of antioxidant excipients in Kadp formulationsis recommended for yielding better stability results. Formulating Kadp in the internal phase ofo/w emulsion formulations may protect this susceptive molecule from oxidative degradationduring the shelf life of the pharmaceutical preparation. Further studies are required to study theexact mechanism of the degradation process. Tabriz University of Medical Sciences 2022-03 2021-05-30 /pmc/articles/PMC9106968/ /pubmed/35620332 http://dx.doi.org/10.34172/apb.2022.031 Text en ©2022 The Authors. https://creativecommons.org/licenses/by/4.0/This is an Open Access article distributed under the terms of the Creative Commons Attribution (CC BY), which permits unrestricted use, distribution, and reproduction in any medium, as long as the original authors and source are cited. No permission is required from the authors or the publishers.
spellingShingle Research Article
Tazesh, Sahar
Tamizi, Elnaz
Siahi Shadbad, Mohammadreza
Mostaghimi, Nazli
Monajjemzadeh, Farnaz
Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design
title Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design
title_full Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design
title_fullStr Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design
title_full_unstemmed Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design
title_short Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design
title_sort comparative stability of two anti-hyperpigmentation agents: kojic acid as a natural metabolite and its di-palmitate ester, under oxidative stress; application to pharmaceutical formulation design
topic Research Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9106968/
https://www.ncbi.nlm.nih.gov/pubmed/35620332
http://dx.doi.org/10.34172/apb.2022.031
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