{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,7,17]],"date-time":"2026-07-17T01:26:52Z","timestamp":1784251612821,"version":"3.55.0"},"reference-count":52,"publisher":"MDPI AG","issue":"12","license":[{"start":{"date-parts":[[2025,6,10]],"date-time":"2025-06-10T00:00:00Z","timestamp":1749513600000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/4.0\/"}],"funder":[{"name":"Zhejiang Hisoar Pharmaceutical Co., Ltd.","award":["KYY-HX-20180525"],"award-info":[{"award-number":["KYY-HX-20180525"]}]},{"name":"Zhejiang Hisoar Pharmaceutical Co., Ltd.","award":["2024XZ001"],"award-info":[{"award-number":["2024XZ001"]}]},{"name":"Zhejiang Shuren University Basic Scientific Research Special Funds","award":["KYY-HX-20180525"],"award-info":[{"award-number":["KYY-HX-20180525"]}]},{"name":"Zhejiang Shuren University Basic Scientific Research Special Funds","award":["2024XZ001"],"award-info":[{"award-number":["2024XZ001"]}]}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Molecules"],"abstract":"<jats:p>Despite their broad pharmacological potential, the clinical application of stilbenes derived from Cajanus cajan (L.) Millsp. leaves (CCMLs) is limited by their poor aqueous solubility, resulting in low oral bioavailability. In this study, an inclusion complex of stilbenes extracted from CCMLs and 2-hydroxypropyl-\u03b2-cyclodextrin (HP-\u03b2-CD) was successfully developed to improve their solubility and oral bioavailability. The preparation conditions were optimized using the response surface methodology, with an optimum mass ratio of CCML extract (CCMLE) to HP-\u03b2-CD of 1.0:8.2 (g\/g) and an optimal temperature of 33 \u00b0C for 2 h. The maximum inclusion efficiency of stilbenes was 82%, and the physicochemical properties of the inclusion complex were characterized. Both in vitro dissolution studies and in vivo pharmacokinetic evaluation demonstrated that HP-\u03b2-CD encapsulation significantly improved the solubility and dissolution rate of stilbenes compared to those of unformulated CCMLE. Notably, the relative bioavailability of cajaninstilbene acid (CSA), longistyle C (LLC) and 4-O-methylpinosylvic acid (MPA) increased to 198%, 177% and 131%, respectively. This work provides a simple and effective strategy to enhance the solubility and bioavailability of naturally derived stilbenes, offering promising potential for the development of other insoluble natural components for both functional food and pharmaceuticals.<\/jats:p>","DOI":"10.3390\/molecules30122526","type":"journal-article","created":{"date-parts":[[2025,6,10]],"date-time":"2025-06-10T03:54:18Z","timestamp":1749527658000},"page":"2526","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":6,"title":["Improved Bioavailability of Stilbenes from Cajanus cajan (L.) Millsp. Leaves Achieved by Hydroxypropyl-\u03b2-Cyclodextrin Inclusion: Preparation, Characterization and Pharmacokinetic Assessment"],"prefix":"10.3390","volume":"30","author":[{"given":"Yingya","family":"Qiu","sequence":"first","affiliation":[{"name":"Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Jiangxuan","family":"Lai","sequence":"additional","affiliation":[{"name":"Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Yuhan","family":"Zhang","sequence":"additional","affiliation":[{"name":"Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-9516-4256","authenticated-orcid":false,"given":"Sheng","family":"Fang","sequence":"additional","affiliation":[{"name":"School of Food Science and Biotechnology, Zhejiang Gongshang University, Hangzhou 310018, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0003-1885-7646","authenticated-orcid":false,"given":"Zili","family":"Guo","sequence":"additional","affiliation":[{"name":"Key Laboratory of Pollution Exposure and Health Intervention of Zhejiang Province, Zhejiang Collaborative Innovation Center for Full-Process Monitoring and Green Governance of Emerging Contaminants, Interdisciplinary Research Academy, Zhejiang Shuren University, Hangzhou 310015, China"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0002-8953-3449","authenticated-orcid":false,"given":"Xianrui","family":"Liang","sequence":"additional","affiliation":[{"name":"Key Laboratory for Green Pharmaceutical Technologies and Related Equipment of Ministry of Education, College of Pharmaceutical Sciences, Zhejiang University of Technology, Hangzhou 310014, China"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2025,6,10]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","unstructured":"Medrano-Padial, C., Prieto, A.I., Puerto, M., and Pichardo, S. 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