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<p>Especially, Vulvovaginal candidiasis is induced by <i>Candida albicans</i>, which is the most common species found in the vaginal secretions of colonizers. <i>Candida</i> infections are increasingly prevalent, posing challenges such as rising antibiotic resistance, adverse drug interactions, and frequent recurrences. This demands an urgent need to develop herbal-based alternatives that reveal strong antifungal activity. Chebulinic acid (CA), a bioactive compound, has shown promising activity against resistant <i>candida</i>; despite its significant therapeutic potential, it faces pitiable challenges seen from a formulation standpoint. Therefore, we proposed carbopol, comprising an optimized gel system for CA topical delivery for the first time. This initial investigation focused on extending its contact time with the target tissue, improving its permeation through the vaginal mucosa, and ensuring better retention in deeper layers, thereby maximizing its antifungal efficacy and minimizing potential side effects. Liposomes (LIPs) were prepared by employing the ethanol injection method, and a vesicle size of 129.8 ± 7.0&#xa0;nm, PDI 0.2967, zeta potential − 24.13 ± 2.3 mV, and 91.00 ± 3.50% of EE were observed. Physicochemical characterization <i>via</i> FTIR, XRD, DSC, SEM, and HR-TEM revealed the structural integrity and morphological characteristics of the LIPs system. In vitro, release was seen from CA, CA-LIPs, and CA-LIPs-gel (approximately 98.11 ± 0.43%) systems. The antifungal efficacy against <i>C. albicans</i> (MTCC 277) exhibited zones of inhibition of 16.6667 ± 0.75&#xa0;mm for CA, 19.33 ± 0.457&#xa0;mm for CA-LIPs, and 23.333 ± 1.15&#xa0;mm for the CA-LIPs gel, and fluconazole (17.67 ± 0.424&#xa0;mm), indicating that the carbopol-based gel reflected superior in vitro efficacy system improved the release and antimicrobial properties of CA, and emphasized the need for in vivo validation before clinical benefits.</p> Graphical Abstract <p></p>

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Fabrication and Optimization of Chebulinic Acid-Loaded Liposomes Based on Carbopol-gel Employing Box-Behnken Design for Vulvovaginal Candidiasis

  • 期刊论文

  • 发表日期：

    2025年10月22日

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  • Manoj Dalabehera,
  • Charul Rathore,
  • Jyoti Mehta,
  • Rudra Narayan Subudhi,
  • Shubham Chaudhari,
  • Neelam Poonia,
  • Uma Ranjan Lal,
  • Alka Kumari

摘要

Especially, Vulvovaginal candidiasis is induced by Candida albicans, which is the most common species found in the vaginal secretions of colonizers. Candida infections are increasingly prevalent, posing challenges such as rising antibiotic resistance, adverse drug interactions, and frequent recurrences. This demands an urgent need to develop herbal-based alternatives that reveal strong antifungal activity. Chebulinic acid (CA), a bioactive compound, has shown promising activity against resistant candida; despite its significant therapeutic potential, it faces pitiable challenges seen from a formulation standpoint. Therefore, we proposed carbopol, comprising an optimized gel system for CA topical delivery for the first time. This initial investigation focused on extending its contact time with the target tissue, improving its permeation through the vaginal mucosa, and ensuring better retention in deeper layers, thereby maximizing its antifungal efficacy and minimizing potential side effects. Liposomes (LIPs) were prepared by employing the ethanol injection method, and a vesicle size of 129.8 ± 7.0 nm, PDI 0.2967, zeta potential − 24.13 ± 2.3 mV, and 91.00 ± 3.50% of EE were observed. Physicochemical characterization via FTIR, XRD, DSC, SEM, and HR-TEM revealed the structural integrity and morphological characteristics of the LIPs system. In vitro, release was seen from CA, CA-LIPs, and CA-LIPs-gel (approximately 98.11 ± 0.43%) systems. The antifungal efficacy against C. albicans (MTCC 277) exhibited zones of inhibition of 16.6667 ± 0.75 mm for CA, 19.33 ± 0.457 mm for CA-LIPs, and 23.333 ± 1.15 mm for the CA-LIPs gel, and fluconazole (17.67 ± 0.424 mm), indicating that the carbopol-based gel reflected superior in vitro efficacy system improved the release and antimicrobial properties of CA, and emphasized the need for in vivo validation before clinical benefits.

Graphical Abstract