{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,2,20]],"date-time":"2026-02-20T06:03:39Z","timestamp":1771567419885,"version":"3.50.1"},"reference-count":26,"publisher":"MDPI AG","issue":"2","license":[{"start":{"date-parts":[[2026,2,18]],"date-time":"2026-02-18T00:00:00Z","timestamp":1771372800000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"North Medicine and Functional Food Characteristic Subject Project in Heilongjiang Province","award":["HLJTSXK-2022-03"],"award-info":[{"award-number":["HLJTSXK-2022-03"]}]},{"DOI":"10.13039\/501100005046","name":"Heilongjiang Provincial Natural Science Foundation of China","doi-asserted-by":"crossref","award":["LH2024H003"],"award-info":[{"award-number":["LH2024H003"]}],"id":[{"id":"10.13039\/501100005046","id-type":"DOI","asserted-by":"crossref"}]},{"name":"Basic Research Support Program for Excellent Young Teachers in Heilongjiang Province","award":["YQJH2023216"],"award-info":[{"award-number":["YQJH2023216"]}]},{"name":"National College Student Innovation and Entrepreneurship Training Program","award":["202510222166"],"award-info":[{"award-number":["202510222166"]}]},{"name":"Heilongjiang Provincial Key Laboratory Fund of New Drug Development and Evaluation of Toxicology","award":["kfkt 2023-05"],"award-info":[{"award-number":["kfkt 2023-05"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Pharmaceutics"],"abstract":"<jats:p>Background: Liver cancer is a complex malignant tumor; gambogic acid (GA) has significant anti-cancer potential, but poor water solubility and low bioavailability limit its clinical application. In this paper, by integrating nanocrystal (NC) technology and an active targeting strategy, a new nanoagent\u2014folic acid-modified phospholipid\u2013gambogic acid nanocrystals (GA-NCs@FA)\u2014was developed to improve the delivery efficiency and therapeutic effect of GA in the treatment of liver cancer. Methods: GA-NCs@FA was prepared by the CO2-assisted precipitation method and the thin-film hydration method. The in vitro anti-tumor activity of GA-NCs@FA was evaluated by cytotoxicity, as well as a scratch and uptake test. A HepG2 tumor-bearing nude mouse model was established to investigate the in vivo distribution and tumor targeting of GA. The in vivo anti-tumor activity was evaluated by the tumor inhibition rate, and the pathological changes of organs in each group were observed by H&amp;E staining. Results: GA-NCs@FA significantly reduced HepG2 cell viability (IC50: 0.50 \u03bcg\u00b7mL\u22121) and migration ability (48 h healing rate: 11.50%) and enhanced intracellular fluorescence intensity. In vivo analysis showed that GA-NCs@FA significantly increased the accumulation of drugs in tumor tissues by active targeting and achieved a tumor growth inhibition rate of 70.9%. Histopathology confirmed that GA-NCs@FA induced the most obvious nuclear pyknosis and necrosis in tumor tissues while maintaining good biosafety. Conclusions: GA-NCs@FA significantly prolongs the systemic circulation time of the drug and enhances intratumoral accumulation; therefore, it is a method that can be considered for active targeting and treatment of liver cancer.<\/jats:p>","DOI":"10.3390\/pharmaceutics18020253","type":"journal-article","created":{"date-parts":[[2026,2,18]],"date-time":"2026-02-18T15:28:18Z","timestamp":1771428498000},"page":"253","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":0,"title":["Preparation and Antitumor Activity Evaluation of Folic Acid-Modified Phospholipid\u2013Gambogic Acid Nanocrystals"],"prefix":"10.3390","volume":"18","author":[{"given":"Xiwen","family":"Zeng","sequence":"first","affiliation":[{"name":"Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Sizhuo","family":"Liu","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Qianhui","family":"He","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yanwen","family":"Ling","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"ORCID":"https:\/\/orcid.org\/0009-0008-4674-743X","authenticated-orcid":false,"given":"Jingqi","family":"Sun","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Yang","family":"Ping","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China"},{"name":"Heilongjiang Provincial Key Laboratory of New Drug Development and Pharmacotoxicological Evaluation, Jiamusi University, Jiamusi 154007, China"}],"role":[{"role":"author","vocabulary":"crossref"}]},{"given":"Jin","family":"Su","sequence":"additional","affiliation":[{"name":"Department of Pharmaceutics, School of Pharmacy, China Jiamusi University, Jiamusi 154007, China"},{"name":"Heilongjiang Provincial Key Laboratory of New Drug Development and Pharmacotoxicological Evaluation, Jiamusi University, Jiamusi 154007, China"}],"role":[{"role":"author","vocabulary":"crossref"}]}],"member":"1968","published-online":{"date-parts":[[2026,2,18]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"4380","DOI":"10.3748\/wjg.v30.i40.4380","article-title":"Promise and Challenges of Traditional Chinese Medicine, Specifically Calculus Bovis, in Liver Cancer Treatment","volume":"30","author":"Xu","year":"2024","journal-title":"World J. 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