AIMS: Most sono/photosensitizers of cancer sonodynamic/photodynamic therapy (SDT/PDT), such as hypocrellin SL052, are water-insoluble, therefore restricting their clinical applications. In this article, we present a water-soluble nanocarrier to load the SDT/PDT sensitizer SL052 with improved pharmacokinetics and therapeutic efficacy. MATERIALS & METHODS: Nanoclusters of polyvinylpyrrolidones with SL052 formed water-soluble nanoparticles (SL052-NPs) while retaining the chemical structure of SL052. RESULTS: The experimental results show that SL052-NPs improve the drug's physicochemical properties and significantly enhance the efficacy of SL052 in terms of pharmacokinetics and cancer killing. Water-soluble SL052-NPs can be used to deliver the drug to deep cancer tissues. A potential benefit of SL052-NPs is that polyvinylpyrrolidones can help SL052 evade the reticuloendothelial system, thereby increasing circulation half-life and improving drug biodistribution. CONCLUSION: SL052-NPs greatly improved the physicochemical properties of SL052 without modifying its chemical structure, allowing for deep-site cancer drug delivery, imaging for diagnosis, and ultrasound or photocontrolled localized cancer therapy.
AIMS: Most sono/photosensitizers of cancer sonodynamic/photodynamic therapy (SDT/PDT), such as hypocrellin SL052, are water-insoluble, therefore restricting their clinical applications. In this article, we present a water-soluble nanocarrier to load the SDT/PDT sensitizer SL052 with improved pharmacokinetics and therapeutic efficacy. MATERIALS & METHODS: Nanoclusters of polyvinylpyrrolidones with SL052 formed water-soluble nanoparticles (SL052-NPs) while retaining the chemical structure of SL052. RESULTS: The experimental results show that SL052-NPs improve the drug's physicochemical properties and significantly enhance the efficacy of SL052 in terms of pharmacokinetics and cancer killing. Water-soluble SL052-NPs can be used to deliver the drug to deep cancer tissues. A potential benefit of SL052-NPs is that polyvinylpyrrolidones can help SL052 evade the reticuloendothelial system, thereby increasing circulation half-life and improving drug biodistribution. CONCLUSION: SL052-NPs greatly improved the physicochemical properties of SL052 without modifying its chemical structure, allowing for deep-site cancer drug delivery, imaging for diagnosis, and ultrasound or photocontrolled localized cancer therapy.