Wansi Li , Panwen Huang , Xianghuan Sun , Yongtai Zhang , Ying Liu , Nianping Feng , Zhi Wang
{"title":"新型固体自乳化给药系统,提高乳香和没药超临界流体提取物的物理性能和生物利用度","authors":"Wansi Li , Panwen Huang , Xianghuan Sun , Yongtai Zhang , Ying Liu , Nianping Feng , Zhi Wang","doi":"10.1016/j.jddst.2025.107030","DOIUrl":null,"url":null,"abstract":"<div><div>Frankincense and myrrh are commonly used in traditional Chinese medicines, and clinical studies have shown that their combined application has a good therapeutic effect on inflammation and tumors. In this study, the supercritical fluid extract of frankincense and myrrh (SFE-FM) was prepared into frankincense and myrrh solid self-emulsifying drug delivery system (FM S-SEDDS) mini-tablets. SFE-FM was used as the main oil phase, and the self-microemulsion was screened using a pseudo-ternary phase diagram and a central composite design. Neusilin was used as the carrier and coating material, with HPMC K100M serving as the matrix material to prepare the sustained-release mini-tablets. Characterization techniques, including scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier-transform infrared (FTIR) analysis, assessed the FM-SEDDS powders, with evaluations of tensile strength (TS), content uniformity, <em>in vitro</em> release, and <em>in vivo</em> pharmacokinetic conducted on the tablets. The FM-SEDDS had an average particle size of 22.36 nm, a polydispersity index (PDI) of 0.23, and a zeta potential of −1.66 mV, with stable properties for 30 d room temperature. It demonstrated suitable tableting properties, including flow, compressibility, and compatibility, while retaining its self-microemulsifying capabilities. <em>In vitro</em> testing confirmed complete release of acetyl-11-keto-<em>β</em>-boswellic acid (AKBA), <em>β</em>-boswellic acid (<em>β</em>-BA), and <em>β</em>-elemonic acid (<em>β</em>-EA) compared to blank tablets. Pharmacokinetic results in Beagle dogs indicated a significant sustained-release effect for the three active ingredients with a strong <em>in vitro</em>–<em>in vivo</em> correlation (IVIVC). SEDDS technology can improve the oral bioavailability of liposoluble drugs like SFE-FM, offering promising industrial application potential.</div></div>","PeriodicalId":15600,"journal":{"name":"Journal of Drug Delivery Science and Technology","volume":"109 ","pages":"Article 107030"},"PeriodicalIF":4.5000,"publicationDate":"2025-05-11","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Novel solid self-emulsifying drug delivery system to improve the physical performance and bioavailability of supercritical fluid extracts of frankincense and myrrh\",\"authors\":\"Wansi Li , Panwen Huang , Xianghuan Sun , Yongtai Zhang , Ying Liu , Nianping Feng , Zhi Wang\",\"doi\":\"10.1016/j.jddst.2025.107030\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div>Frankincense and myrrh are commonly used in traditional Chinese medicines, and clinical studies have shown that their combined application has a good therapeutic effect on inflammation and tumors. In this study, the supercritical fluid extract of frankincense and myrrh (SFE-FM) was prepared into frankincense and myrrh solid self-emulsifying drug delivery system (FM S-SEDDS) mini-tablets. SFE-FM was used as the main oil phase, and the self-microemulsion was screened using a pseudo-ternary phase diagram and a central composite design. Neusilin was used as the carrier and coating material, with HPMC K100M serving as the matrix material to prepare the sustained-release mini-tablets. Characterization techniques, including scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier-transform infrared (FTIR) analysis, assessed the FM-SEDDS powders, with evaluations of tensile strength (TS), content uniformity, <em>in vitro</em> release, and <em>in vivo</em> pharmacokinetic conducted on the tablets. The FM-SEDDS had an average particle size of 22.36 nm, a polydispersity index (PDI) of 0.23, and a zeta potential of −1.66 mV, with stable properties for 30 d room temperature. It demonstrated suitable tableting properties, including flow, compressibility, and compatibility, while retaining its self-microemulsifying capabilities. <em>In vitro</em> testing confirmed complete release of acetyl-11-keto-<em>β</em>-boswellic acid (AKBA), <em>β</em>-boswellic acid (<em>β</em>-BA), and <em>β</em>-elemonic acid (<em>β</em>-EA) compared to blank tablets. Pharmacokinetic results in Beagle dogs indicated a significant sustained-release effect for the three active ingredients with a strong <em>in vitro</em>–<em>in vivo</em> correlation (IVIVC). SEDDS technology can improve the oral bioavailability of liposoluble drugs like SFE-FM, offering promising industrial application potential.</div></div>\",\"PeriodicalId\":15600,\"journal\":{\"name\":\"Journal of Drug Delivery Science and Technology\",\"volume\":\"109 \",\"pages\":\"Article 107030\"},\"PeriodicalIF\":4.5000,\"publicationDate\":\"2025-05-11\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Drug Delivery Science and Technology\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1773224725004332\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Drug Delivery Science and Technology","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1773224725004332","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Novel solid self-emulsifying drug delivery system to improve the physical performance and bioavailability of supercritical fluid extracts of frankincense and myrrh
Frankincense and myrrh are commonly used in traditional Chinese medicines, and clinical studies have shown that their combined application has a good therapeutic effect on inflammation and tumors. In this study, the supercritical fluid extract of frankincense and myrrh (SFE-FM) was prepared into frankincense and myrrh solid self-emulsifying drug delivery system (FM S-SEDDS) mini-tablets. SFE-FM was used as the main oil phase, and the self-microemulsion was screened using a pseudo-ternary phase diagram and a central composite design. Neusilin was used as the carrier and coating material, with HPMC K100M serving as the matrix material to prepare the sustained-release mini-tablets. Characterization techniques, including scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier-transform infrared (FTIR) analysis, assessed the FM-SEDDS powders, with evaluations of tensile strength (TS), content uniformity, in vitro release, and in vivo pharmacokinetic conducted on the tablets. The FM-SEDDS had an average particle size of 22.36 nm, a polydispersity index (PDI) of 0.23, and a zeta potential of −1.66 mV, with stable properties for 30 d room temperature. It demonstrated suitable tableting properties, including flow, compressibility, and compatibility, while retaining its self-microemulsifying capabilities. In vitro testing confirmed complete release of acetyl-11-keto-β-boswellic acid (AKBA), β-boswellic acid (β-BA), and β-elemonic acid (β-EA) compared to blank tablets. Pharmacokinetic results in Beagle dogs indicated a significant sustained-release effect for the three active ingredients with a strong in vitro–in vivo correlation (IVIVC). SEDDS technology can improve the oral bioavailability of liposoluble drugs like SFE-FM, offering promising industrial application potential.
期刊介绍:
The Journal of Drug Delivery Science and Technology is an international journal devoted to drug delivery and pharmaceutical technology. The journal covers all innovative aspects of all pharmaceutical dosage forms and the most advanced research on controlled release, bioavailability and drug absorption, nanomedicines, gene delivery, tissue engineering, etc. Hot topics, related to manufacturing processes and quality control, are also welcomed.