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Discovery of Novel Diesters Incorporating Kojic Acid With NSAIDs and Palmitic Acid as Dual Inhibitor of Melanogenesis and Inflammation.
Moharir, Shreyash; Khobragade, Prachi; Rane, Rajesh; Suryawanshi, Mugdha; Pal, Kavita; Gawade, Bapu; Kumar, Dileep; Satpute, Bharat.
Afiliación
  • Moharir S; Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune 411038, India.
  • Khobragade P; Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune 411038, India.
  • Rane R; Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune 411038, India. Electronic address: rajeshrane.uict@gmail.com.
  • Suryawanshi M; Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune 411038, India. Electronic address: mugdha.rs@gmail.com.
  • Pal K; Advanced Centre for Treatment, Research and Education in Cancer (ACTREC), Tata Memorial Centre, Kharghar, Navi Mumbai 410210, India.
  • Gawade B; Cleanchem Lifesciences Pvt. Ltd., Kopar-Khairane, Navi Mumbai 400710, India.
  • Kumar D; Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune 411038, India. Electronic address: dileep0@gmail.com.
  • Satpute B; Department of Pharmaceutical Chemistry, Poona College of Pharmacy, Bharati Vidyapeeth (Deemed to be University), Pune 411038, India.
J Pharm Sci ; 113(7): 1769-1778, 2024 Jul.
Article en En | MEDLINE | ID: mdl-38663499
ABSTRACT
Our study focuses on creating hybrid compounds and assessing their suitability for use in skincare products. The synergistic combination of Kojic acid, NSAIDs, and Palmitic acid proved to be an effective approach in inhibiting melanin production, making it a promising solution for individuals with hyperpigmentation concerns with Kojic acid (KA) Ibuprofen monoester (IBUM) and Ibuprofen-Kojic acid-Palmitic acid diester (IBUD) exhibiting a potential tyrosinase (38 % and 49 % inhibition at 200 µM) and anti-melanogenesis activity (77 % and 79 % inhibition at 100 µM). Furthermore, these compounds exhibited potent anti-inflammatory effects, Kojic acid-Diclofenac monoester (DICM) and Diclofenac-Kojic acid-Palmitic acid diester (DICD) offering potential benefits for inflammation by lowering the paw volume. A stability study under chemical conditions and enzymatic conditions was also performed, wherein DICM and DICD showed a better half-life of 515, 593 h under chemical stability and 6.3, 7.5 h under enzymatic stability studies respectively. The diester hybrids IBUD, DICD, Naproxen-Kojic acid-Palmitic acid diester (NAPD) showed a better permeation and penetration profiles compared to their parent drugs. In-vitro cell line studies were conducted to assess the safety and efficacy of these hybrid esters, with promising results. The dual inhibitor demonstrated minimal cytotoxicity and remarkable anti-melanogenic and anti-inflammatory activities, showing its potential as a versatile agent in addressing both melanogenesis and inflammation.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pironas / Antiinflamatorios no Esteroideos / Ácido Palmítico / Melaninas Límite: Animals / Humans / Male Idioma: En Revista: J Pharm Sci Año: 2024 Tipo del documento: Article País de afiliación: India Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Pironas / Antiinflamatorios no Esteroideos / Ácido Palmítico / Melaninas Límite: Animals / Humans / Male Idioma: En Revista: J Pharm Sci Año: 2024 Tipo del documento: Article País de afiliación: India Pais de publicación: Estados Unidos