Preparation of PEGylated nedaplatin liposomes with sustained release behavior for enhancing the antitumor efficacy of non-small cell lung cancer

作者全名："Tang, Jinsong; Yang, Zhangyou; Zhang, Yuan; Huang, Ruixue; Yu, Chaoqun; Yu, Chao"

作者地址："[Tang, Jinsong; Huang, Ruixue; Yu, Chaoqun; Yu, Chao] Chongqing Med Univ, Coll Pharm, Res Ctr Pharmaceut Preparat & Nanomed, Chongqing 400016, Peoples R China; [Yang, Zhangyou; Yu, Chao] Chongqing Med Univ, Coll Pharm, Pharmaceut Engn Res Ctr, Chongqing 400016, Peoples R China; [Zhang, Yuan] Chongqing Med Univ, Dept Pharm, Affiliated Hosp 1, Chongqing 400010, Peoples R China"

通信作者："Yu, CQ; Yu, C (通讯作者)，Chongqing Med Univ, Coll Pharm, Res Ctr Pharmaceut Preparat & Nanomed, Chongqing 400016, Peoples R China.; Yu, C (通讯作者)，Chongqing Med Univ, Coll Pharm, Pharmaceut Engn Res Ctr, Chongqing 400016, Peoples R China."

来源：INTERNATIONAL JOURNAL OF PHARMACEUTICS

ESI学科分类：PHARMACOLOGY & TOXICOLOGY

WOS号：WOS:000948164400001

JCR分区：Q1

影响因子：5.8

年份：2023

卷号：635

期号：　

开始页：　

结束页：　

文献类型：Article

关键词：Nedaplatin; PEGylated liposomes; Drug-excipient compatibility; Lung cancer; Sustained-release; Antitumor activity

摘要："Nedaplatin (NDP) plays an important role in the chemotherapies of non-small cell lung cancer (NSCLC). How-ever, dose-limiting toxicities such as myelosuppression and drug resistance restrict its clinical application. Herein, we intended to overcome these defects by developing a PEGylated liposomal formulation encapsulated NDP (NDP-LPs). For the first time, we found the incompatibility between NDP and natural phospholipids such as egg phosphatidylcholine (EPC) using the high-performance liquid chromatography (HPLC) method. The orthogonal experimental design was applied to optimize the conditions for preparing NDP-LPs, with encapsu-lation efficiency (EE) as the evaluation indicator. The physicochemical properties of optimized NDP-LPs were further characterized, including particle size, zeta potential, EE, drug release profiles, and so on. Results showed that a significantly sustained-release profile of NDP-LPs was observed and the releasing time of NDP could reach as long as 8 days. At the cellular level, NDP encapsulated in the PEGylated liposomes enhanced its cellular uptake and possessed potent cytotoxic activity. After intravenous injection, NDP-LPs could accumulate at tumor sites and effectively inhibit tumor growth of mice without obvious adverse effects. In conclusion, our results demonstrated that PEGylated liposomes could serve as a promising carrier to enhance the therapeutic effects of NDP."

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