Pharmaceutical development and technology · 2026
In vitro antifungal and antibiofilm evaluation of reduction-responsive ketoconazole-loaded nanoparticles based on cystamine-modified poly (isobutene-alt-maleic anhydride) polymer.
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Wang Fuyou, Liu Qingmin, Wu Wenhui, Su Yuxiao, Song Zhimei, Feng Runliang
Аннотация
PURPOSE: In order to develop reduction-responsive nano-drug delivery system for encapsulating antifungal drugs.
METHODS: Herein, with poly (isobutene-alt-maleic anhydride) as skeleton, we synthesized a polymer containing cross-linked disulfide bonds to prepare reduction-responsive ketoconazole-loaded nanoparticles (MPEG-P-KET). The in vitro reduction-responsive behavior and antifungal activity of MPEG-P-KET were investigated.
RESULTS: The MPEG-P-KET improved the dispersion and solubility of lipophilic KET. KET's imidazole group formed a salt with the free carboxyl groups in the polymer carrier, resulting in delayed drug release from MPEG-P-KET. However, MPEG-P-KET still exhibited reduction-sensitive drug release behavior, and showed comparable antifungal activity with KET in vitro. Interestingly, MPEG-P-KET demonstrated higher ability to inhibit biofilm formation and disrupt mature biofilms than KET.
CONCLUSION: The polymeric nanoparticles with disulfide bonds could be used for the encapsulation and controlled delivery of antifungal drugs in the field of fungal infection treatment.
METHODS: Herein, with poly (isobutene-alt-maleic anhydride) as skeleton, we synthesized a polymer containing cross-linked disulfide bonds to prepare reduction-responsive ketoconazole-loaded nanoparticles (MPEG-P-KET). The in vitro reduction-responsive behavior and antifungal activity of MPEG-P-KET were investigated.
RESULTS: The MPEG-P-KET improved the dispersion and solubility of lipophilic KET. KET's imidazole group formed a salt with the free carboxyl groups in the polymer carrier, resulting in delayed drug release from MPEG-P-KET. However, MPEG-P-KET still exhibited reduction-sensitive drug release behavior, and showed comparable antifungal activity with KET in vitro. Interestingly, MPEG-P-KET demonstrated higher ability to inhibit biofilm formation and disrupt mature biofilms than KET.
CONCLUSION: The polymeric nanoparticles with disulfide bonds could be used for the encapsulation and controlled delivery of antifungal drugs in the field of fungal infection treatment.