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  3. Cholesterol sulfate-mediated ion-pairing facilitates the self-nanoassembly of hydrophilic cationic mitoxantrone

Cholesterol sulfate-mediated ion-pairing facilitates the self-nanoassembly of hydrophilic cationic mitoxantrone

  • J Colloid Interface Sci. 2024 Sep:669:731-739. doi: 10.1016/j.jcis.2024.05.029.
Jingxuan Zhang 1,  Hongkai Fang 1,  Yuebin Dai 1,  Yaqiao Li 1,  Lingxiao Li 1,  Shiyi Zuo 1,  Tian Liu 1,  Yixin Sun 1,  Xianbao Shi 2,  Zhonggui He 3,  Jin Sun 4,  Bingjun Sun 5
Affiliations

Affiliations

  • 1 Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China.
  • 2 Department of Pharmacy, The First Affiliated Hospital of Jinzhou Medical University, Jinzhou 121001, China.
  • 3 Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China; Joint International Research Laboratory of Intelligent Drug Delivery Systems, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China.
  • 4 Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China; Joint International Research Laboratory of Intelligent Drug Delivery Systems, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address: sunjin@syphu.edu.cn.
  • 5 Wuya College of Innovation, Shenyang Pharmaceutical University, Shenyang 110016, China; Joint International Research Laboratory of Intelligent Drug Delivery Systems, Ministry of Education, Shenyang Pharmaceutical University, Shenyang 110016, China. Electronic address: sunbingjun_spy@sina.com.
PMID: 38735255 DOI: 10.1016/j.jcis.2024.05.029
Abstract

Hypothesis: Hydrophilic cationic drugs such as mitoxantrone hydrochloride (MTO) pose a significant delivery challenge to the development of nanodrug systems. Herein, we report the use of a hydrophobic ion-pairing strategy to enhance the nano-assembly of MTO.

Experiments: We employed biocompatible sodium cholesteryl sulfate (SCS) as a modification module to form stable ion pairs with MTO, which balanced the intermolecular forces and facilitated nano-assembly. PEGylated MTO-SCS nanoassemblies (pMS NAs) were prepared via nanoprecipitation. We systematically evaluated the effect of the ratio of the drug module (MTO) to the modification module (SCS) on the nanoassemblies.

Findings: The increased lipophilicity of MTO-SCS ion pair could significantly improve the encapsulation efficiency (∼97 %) and cellular uptake efficiency of MTO. The pMS NAs showed prolonged blood circulation, maintained the same level of tumor antiproliferative activity, and exhibited reduced toxicity compared with the free MTO solution. It is noteworthy that the stability, cellular uptake, cytotoxicity, and in vivo pharmacokinetic behavior of the pMS NAs increased in proportion to the molar ratio of SCS to MTO. This study presents a self-assembly strategy mediated by ion pairing to overcome the challenges commonly associated with the poor assembly ability of hydrophilic cationic drugs.

Keywords

Chemotherapy; Cholesterol sulfate; Drug delivery; Ion-pairing strategy; Mitoxantrone hydrochloride; Self-assembly.

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