Article(id=1304415538541777781, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304415531491152712, articleNumber=null, orderNo=null, doi=10.7501/j.issn.0253-2670.2026.09.010, pmid=null, cstr=null, oa=null, hot=0, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=1765900800000, receivedDateStr=2025-12-17, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1788926499257, onlineDateStr=2026-09-09, pubDate=null, pubDateStr=null, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1788926499257, onlineIssueDateStr=2026-09-09, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1788926499257, creator=13701087609, updateTime=1788926499257, updator=13701087609, issue=Issue{id=1304415531491152712, tenantId=1146029695717560320, journalId=1302319053441957962, year='2026', volume='57', issue='9', pageStart='3261', pageEnd='3684', issueExtLink='null', onlineDate='null', pubDate='1778515200000', pubDateStr='2026-05-12', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1788926497576, creator='13701087609', updateTime=1788926796984, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1304416787358049066, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304415531491152712, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1304416787358049067, tenantId=1146029695717560320, journalId=1302319053441957962, issueId=1304415531491152712, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=3365, endPage=3374, ext={EN=ArticleExt(id=1304415540445991799, articleId=1304415538541777781, tenantId=1146029695717560320, journalId=1302319053441957962, language=EN, title=Optimisation of preparation process of asiaticoside mPEG-PLGA microspheres and its invitro evaluation, columnId=null, journalTitle=Chinese Traditional and Herbal Drugs, columnName=null, runingTitle=null, highlight=null, articleAbstract=Objective This study aimed to investigate the optimal preparation process for asiaticoside microspheres using polyethylene glycol-polylactic acid-glycolic acid copolymer (mPEG-PLGA) as the carrier. Methods Key process parameters affecting microsphere preparation were first screened from factors including curing temperature, emulsifier PVA concentration, stirring speed, water-to-oil ratio, and mPEG-PLGA concentration. Subsequently, a Box-Behnken design-response surface methodology (BBD-RSM) experiment was employed to further optimize the preparation conditions for the drug-loaded microspheres. Their morphology, particle size distribution, drug loading, encapsulation efficiency, invitro release behavior, and biocompatibility were comprehensively evaluated. Results Curing temperature, stirring speed, emulsifier PVA and mPEG-PLGA concentrations, and water-to-oil ratio all influenced the encapsulation efficiency and morphology of the microspheres. Among them, curing temperature and mPEG-PLGA concentration had a greater impact: both excessively high and low curing temperatures reduced encapsulation efficiency; increasing mPEG-PLGA concentration improved encapsulation efficiency, but excessively high concentrations led to adhesion and increased particle size. The optimized conditions were 40 ℃, 1 800 r/min, with appropriate emulsifier PVA and mPEG-PLGA concentrations. Using mPEG-PLGA concentration, water-to-oil ratio, and emulsifier PVA concentration as investigation factors in a 3-factor, 3-level BBD experimental design, the optimal preparation process for asiaticoside mPEG-PLGA microspheres was determined as: mPEG-PLGA concentration 123.8 g/L, PVA mass concentration 9.8 g/L, and water-to-oil ratio 12.7∶1. The resulting microspheres had uniform particle size (58.97 ± 4.44) μm, a drug loading of (8.43 ± 0.16)%, and an encapsulation efficiency of (62.66 ± 0.84)%. They released approximately 80% of asiaticoside at a stable rate within 96 h, and maintained over 90% cell viability after 72 h of co-culture with L929 cells. Conclusion Asiaticoside-loaded mPEG-PLGA microspheres were successfully prepared. The obtained microspheres exhibit uniform particle size, relatively high encapsulation efficiency and drug loading, enable sustained drug release, and possess good biocompatibility. This system utilizes the hydrophilicity of mPEG-PLGA to improve drug stability and release behavior, providing a new strategy for the efficient delivery of asiaticoside., authors=CAI Jiajing, ZHANG Xueqiong, HU Chen, CHEN Hailin, DING Jie, authorsList=CAI Jiajing, ZHANG Xueqiong, HU Chen, CHEN Hailin, DING Jie, authorCompany=null, correspAuthors=null, authorNote=null, correspAuthorsNote=null, copyrightStatement=null, copyrightOwner=null, extLink=null, articleAbsUrl=null, sourceXml=null, magXml=null, pdfUrl=null, pdf=null, pdfFileSize=null, pdfExtLink=null, richHtmlUrl=null, mobilePdfUrl=null, reviewReport=null, pdfFirstPage=null, abstractGraph=null, abstractGraphContent=null, abstractVideo=null, citation=null, cebUrl=null, magXmlContent=null, mapNumber=null, fund=null), CN=ArticleExt(id=1304415538793436022, articleId=1304415538541777781, tenantId=1146029695717560320, journalId=1302319053441957962, language=CN, title=积雪草苷mPEG-PLGA微球的制备工艺优化及其体外评价, columnId=1304140189132149234, journalTitle=中草药, columnName=药剂与工艺, runingTitle=null, highlight=null, articleAbstract=目的 以聚乙二醇-聚乳酸羟基乙酸共聚物（polyethylene glycol-polylactic acid-glycolic acid copolymer，mPEG-PLGA）为载体，探究积雪草苷mPEG-PLGA微球的最佳制备工艺。方法 首先从微球固化温度、乳化剂PVA质量浓度、搅拌速度、水油比以及mPEG-PLGA质量浓度中，筛选出影响积雪草苷微球制备的关键工艺参数，随后采用Box-Behnken设计-响应面法（Box-Behnken design-response surface methodology，BBD-RSM）实验进一步优化载药微球的制备条件，并对该微球形态、粒径分布、载药量、包封率、体外释放行为以及生物相容性进行综合评价。结果 固化温度、搅拌速度、乳化剂PVA与mPEG-PLGA质量浓度及水油比均影响微球包封率与形态。其中，固化温度与mPEG-PLGA质量浓度影响较大，固化温度过高或过低均降低微球包封率；mPEG-PLGA质量浓度增加可提高包封率，但过高却导致微球粘连与粒径增大。优化的条件为40 ℃、1 800 r/min、适量乳化剂PVA与mPEG-PLGA。选取mPEG-PLGA质量浓度、水油比和乳化剂PVA质量浓度作为考察因素，进行3因素3水平BBD实验设计，得到的积雪草苷mPEG-PLGA微球的最佳制备工艺为mPEG-PLGA质量浓度123.8 g/L、PVA质量浓度9.8 g/L，水油比12.7∶1。制备的积雪草苷微球粒径均匀，为（58.97.90±4.44）μm，载药量为（8.43±0.16）%，包封率达（62.66±0.84）%，在96 h内以稳定速度释放约80%的积雪草苷，与L929细胞共培养72 h后仍有高于90%的存活率。结论 成功制备积雪草苷mPEG-PLGA微球，所得微球粒径均匀、包封率与载药量较高，可实现药物缓释，并具有良好的生物相容性。该体系利用mPEG-PLGA的亲水性改善了药物稳定性与释放行为，为积雪草苷的高效递送提供了新策略。, authors=蔡佳婧1, 张雪琼1, 胡晨1, 陈海霖1, 丁杰2, authorsList=蔡佳婧, 张雪琼, 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detailUrlEn=https://castjournals.cast.org.cn/joweb/zcy/EN/10.7501/j.issn.0253-2670.2026.09.010, pdfUrlCn=https://castjournals.cast.org.cn/joweb/zcy/CN/PDF/10.7501/j.issn.0253-2670.2026.09.010, pdfUrlEn=https://castjournals.cast.org.cn/joweb/zcy/EN/PDF/10.7501/j.issn.0253-2670.2026.09.010, aliStartDate=null, aliEndDate=null, collectionFlag=false, citedCount=null, citedUrl=null, previewStatus=0, delFlag=0, hasFullText=0, orderTime=1788926499257, fullTextJson=null, articleText=null, reference=秦慧真,林思,邓玲玉,等.积雪草苷的药理作用及机制研究进展[J].中国药房, 2021, 32(21):2683-2688. Shen H Y, Zhu F, Li J S, et al. Protective effect of asiaticoside on radiation-induced proliferation inhibition and DNA damage of fibroblasts and mice death[J]. Open Life Sci, 2020, 15:145-151. He Z L, Hu Y Y, Niu Z Q, et al. A review of pharmacokinetic and pharmacological properties of asiaticoside, a major active constituent of Centella asiatica(L.)Urb[J]. J Ethnopharmacol, 2023, 302:115865. Chen X S, Zhang H M, Liang Y Y, et al. Inflammationmodulating antibacterial hydrogel sustained release asiaticoside for infection wound healing[J]. Biomater Adv,2023, 147:213302. Lee Y J, Kim M S. Advances in drug-loaded microspheres for targeted, controlled, and sustained drug delivery:Potential, applications, and future directions[J]. Biomed Pharmacother, 2025, 189:118244. 邱晓明,甄平,李松凯.聚乳酸-羟基乙酸共聚物载药微球制备工艺研究进展[J].中国组织工程研究, 2018,22(10):1599-1604. Chen W W, Li H, Zhang X Y, et al. Microfluidic preparation of monodisperse PLGA-PEG/PLGA microspheres with controllable morphology for drug release[J]. Lab Chip, 2024, 24(19):4623-4631. Zhou Y, Liu Z H, Luo X, et al. Controllable fabrication of porous PLGA microspheres with adjustable degradability and morphology as cell carrier[J]. Mater Today Commun,2026, 50:114520. Pu C G, Wang Q, Zhang H J, et al. In vitro-in vivo relationship of amorphous insoluble API(progesterone)in PLGA microspheres[J]. Pharm Res, 2017, 34(12):2787-2797. Xing D D, Tang L H, Yang H Y, et al. Effect of mPEGPLGA on drug crystallinity and release of long-acting injection microspheres:In vitro and in vivo perspectives[J]. Pharm Res, 2024, 41(6):1271-1284. Anwar A, Sun P F, Rong X X, et al. Process analytical technology as in-process control tool in semi-continuous manufacturing of PLGA/PEG-PLGA microspheres[J].Heliyon, 2023, 9(5):e15753. Tu S C, Mai S T, Shu D, et al. Microfluidic-based preparation of PLGA microspheres facilitating peptide sustained-release[J]. Mater Lett, 2024, 368:136675. Yi K F, Wang X L, Li P L, et al. Amphiphilic mPEG-PLGA copolymer nanoparticles co-delivering colistin and niclosamide to treat colistin-resistant Gram-negative bacteria infections[J]. Commun Biol, 2025, 8:673. Zhang C Z, Niu J, Chong Y S, et al. Porous microspheres as promising vehicles for the topical delivery of poorly soluble asiaticoside accelerate wound healing and inhibit scar formation in vitro&in vivo[J]. Eur J Pharm Biopharm, 2016, 109:1-13. An T, Choi J, Kim A, et al. Sustained release of risperidone from biodegradable microspheres prepared by in-situ suspension-evaporation process[J]. Int J Pharm, 2016,503(1/2):8-15. Reddy P L, Shanmugasundaram S. Optimizing process parameters for controlled drug delivery:A quality by design(QbD)approach in naltrexone microspheres[J].AAPS Pharm Sci Tech, 2024, 25(5):105. Esnaashari S S, Amani A. Optimization of noscapineloaded m PEG-PLGA nanoparticles and release study:A response surface methodology approach[J]. J Pharm Innov, 2018, 13(3):237-246. Zhang P H, Tang R M, Yang S L, et al. Preparation and in vitro release of m PEG-PLA microspheres of Panax notoginseng saponins[J]. Int J Biol Macromol, 2022, 217:922-930. Liu R, Wang Y, Ma Y D, et al. Effects of the molecular weight of PLGA on degradation and drug release in vitro from an m PEG-PLGA nanocarrier[J]. Chem Res Chin Univ, 2016, 32(5):848-853. Narisepalli S, Salunkhe S A, Chitkara D, et al. Asiaticoside polymeric nanoparticles for effective diabetic wound healing through increased collagen biosynthesis:In-vitro and in-vivo evaluation[J]. Int J Pharm, 2023, 631:122508. Yang Z Y, Wei K, Zhang Y, et al. Study on the preparation of pramipexole sustained-release PLGA microspheres:Effect of fatty acids and polymer blending on the properties of microspheres[J]. J Drug Deliv Sci Technol,2025, 114:107462. White C, Schwendeman S P. Formulation and characterization of exenatide-loaded PLGA microspheres prepared by coacervation[J]. Drug Deliv Transl Res, 2025,doi:10.1007/S13346-025-02008-2. Wei P S, Chen Y J, Lin S Y, et al. In situ subcutaneously injectable thermosensitive PEG-PLGA diblock and PLGA-PEG-PLGA triblock copolymer composite as sustained delivery of bispecific anti-CD3 scFv T-cell/antiEGFR Fab Engager(BiTEE)[J]. Biomaterials, 2021, 278:121166. Pande S. Factors affecting response variables with emphasis on drug release and loading for optimization of liposomes[J]. Artif Cells Nanomed Biotechnol, 2024,52(1):334-344. Luo D, Huang L X, Bai B X, et al. Sequential drug-release microsphere system for scarless wound healing[J]. Mater Today Bio, 2025, 35:102310. 姜朝瑞,许燕,熊莹,等.氧化石墨烯复合材料载药微球的制备与性能研究[J].中国组织工程研究, 2022,26(22):3467-3473. Zhang Y, Awang Nawi M A, Shaari R, et al. Enhancing drug efficacy:A review of research progress in drugloaded microspheres[J]. Cureus, 2025, 17(8):e90498. Wang S Y, Feng X B, Liu P, et al. Blending of PLGA-PEGPLGA for improving the erosion and drug release profile of PCL microspheres[J]. Curr Pharm Biotechnol, 2020,21(11):1079-1087. Hajian M, Erfani-Moghadam V, Arabi M S, et al. A comparison between optimized PLGA and CS-Alg-PLGA microspheres for long-lasting release of glatiramer acetate[J]. J Drug Deliv Sci Technol, 2023, 82:104355.)
Objective This study aimed to investigate the optimal preparation process for asiaticoside microspheres using polyethylene glycol-polylactic acid-glycolic acid copolymer (mPEG-PLGA) as the carrier. Methods Key process parameters affecting microsphere preparation were first screened from factors including curing temperature, emulsifier PVA concentration, stirring speed, water-to-oil ratio, and mPEG-PLGA concentration. Subsequently, a Box-Behnken design-response surface methodology (BBD-RSM) experiment was employed to further optimize the preparation conditions for the drug-loaded microspheres. Their morphology, particle size distribution, drug loading, encapsulation efficiency, invitro release behavior, and biocompatibility were comprehensively evaluated. Results Curing temperature, stirring speed, emulsifier PVA and mPEG-PLGA concentrations, and water-to-oil ratio all influenced the encapsulation efficiency and morphology of the microspheres. Among them, curing temperature and mPEG-PLGA concentration had a greater impact: both excessively high and low curing temperatures reduced encapsulation efficiency; increasing mPEG-PLGA concentration improved encapsulation efficiency, but excessively high concentrations led to adhesion and increased particle size. The optimized conditions were 40 ℃, 1 800 r/min, with appropriate emulsifier PVA and mPEG-PLGA concentrations. Using mPEG-PLGA concentration, water-to-oil ratio, and emulsifier PVA concentration as investigation factors in a 3-factor, 3-level BBD experimental design, the optimal preparation process for asiaticoside mPEG-PLGA microspheres was determined as: mPEG-PLGA concentration 123.8 g/L, PVA mass concentration 9.8 g/L, and water-to-oil ratio 12.7∶1. The resulting microspheres had uniform particle size (58.97 ± 4.44) μm, a drug loading of (8.43 ± 0.16)%, and an encapsulation efficiency of (62.66 ± 0.84)%. They released approximately 80% of asiaticoside at a stable rate within 96 h, and maintained over 90% cell viability after 72 h of co-culture with L929 cells. Conclusion Asiaticoside-loaded mPEG-PLGA microspheres were successfully prepared. The obtained microspheres exhibit uniform particle size, relatively high encapsulation efficiency and drug loading, enable sustained drug release, and possess good biocompatibility. This system utilizes the hydrophilicity of mPEG-PLGA to improve drug stability and release behavior, providing a new strategy for the efficient delivery of asiaticoside.
CAI Jiajing, ZHANG Xueqiong, HU Chen, CHEN Hailin, DING Jie.
Optimisation of preparation process of asiaticoside mPEG-PLGA microspheres and its invitro evaluation[J].
Chinese Traditional and Herbal Drugs,
2026
, 57
(9)
: 3365
-3374
.
DOI: 10.7501/j.issn.0253-2670.2026.09.010
秦慧真,林思,邓玲玉,等.积雪草苷的药理作用及机制研究进展[J].中国药房, 2021, 32(21):2683-2688. Shen H Y, Zhu F, Li J S, et al. Protective effect of asiaticoside on radiation-induced proliferation inhibition and DNA damage of fibroblasts and mice death[J]. Open Life Sci, 2020, 15:145-151. He Z L, Hu Y Y, Niu Z Q, et al. A review of pharmacokinetic and pharmacological properties of asiaticoside, a major active constituent of Centella asiatica(L.)Urb[J]. J Ethnopharmacol, 2023, 302:115865. Chen X S, Zhang H M, Liang Y Y, et al. Inflammationmodulating antibacterial hydrogel sustained release asiaticoside for infection wound healing[J]. Biomater Adv,2023, 147:213302. Lee Y J, Kim M S. Advances in drug-loaded microspheres for targeted, controlled, and sustained drug delivery:Potential, applications, and future directions[J]. Biomed Pharmacother, 2025, 189:118244. 邱晓明,甄平,李松凯.聚乳酸-羟基乙酸共聚物载药微球制备工艺研究进展[J].中国组织工程研究, 2018,22(10):1599-1604. Chen W W, Li H, Zhang X Y, et al. Microfluidic preparation of monodisperse PLGA-PEG/PLGA microspheres with controllable morphology for drug release[J]. Lab Chip, 2024, 24(19):4623-4631. Zhou Y, Liu Z H, Luo X, et al. Controllable fabrication of porous PLGA microspheres with adjustable degradability and morphology as cell carrier[J]. Mater Today Commun,2026, 50:114520. Pu C G, Wang Q, Zhang H J, et al. In vitro-in vivo relationship of amorphous insoluble API(progesterone)in PLGA microspheres[J]. Pharm Res, 2017, 34(12):2787-2797. Xing D D, Tang L H, Yang H Y, et al. Effect of mPEGPLGA on drug crystallinity and release of long-acting injection microspheres:In vitro and in vivo perspectives[J]. Pharm Res, 2024, 41(6):1271-1284. Anwar A, Sun P F, Rong X X, et al. Process analytical technology as in-process control tool in semi-continuous manufacturing of PLGA/PEG-PLGA microspheres[J].Heliyon, 2023, 9(5):e15753. Tu S C, Mai S T, Shu D, et al. Microfluidic-based preparation of PLGA microspheres facilitating peptide sustained-release[J]. Mater Lett, 2024, 368:136675. Yi K F, Wang X L, Li P L, et al. Amphiphilic mPEG-PLGA copolymer nanoparticles co-delivering colistin and niclosamide to treat colistin-resistant Gram-negative bacteria infections[J]. Commun Biol, 2025, 8:673. Zhang C Z, Niu J, Chong Y S, et al. Porous microspheres as promising vehicles for the topical delivery of poorly soluble asiaticoside accelerate wound healing and inhibit scar formation in vitro&in vivo[J]. Eur J Pharm Biopharm, 2016, 109:1-13. An T, Choi J, Kim A, et al. Sustained release of risperidone from biodegradable microspheres prepared by in-situ suspension-evaporation process[J]. Int J Pharm, 2016,503(1/2):8-15. Reddy P L, Shanmugasundaram S. Optimizing process parameters for controlled drug delivery:A quality by design(QbD)approach in naltrexone microspheres[J].AAPS Pharm Sci Tech, 2024, 25(5):105. Esnaashari S S, Amani A. Optimization of noscapineloaded m PEG-PLGA nanoparticles and release study:A response surface methodology approach[J]. J Pharm Innov, 2018, 13(3):237-246. Zhang P H, Tang R M, Yang S L, et al. Preparation and in vitro release of m PEG-PLA microspheres of Panax notoginseng saponins[J]. Int J Biol Macromol, 2022, 217:922-930. Liu R, Wang Y, Ma Y D, et al. Effects of the molecular weight of PLGA on degradation and drug release in vitro from an m PEG-PLGA nanocarrier[J]. Chem Res Chin Univ, 2016, 32(5):848-853. Narisepalli S, Salunkhe S A, Chitkara D, et al. Asiaticoside polymeric nanoparticles for effective diabetic wound healing through increased collagen biosynthesis:In-vitro and in-vivo evaluation[J]. Int J Pharm, 2023, 631:122508. Yang Z Y, Wei K, Zhang Y, et al. Study on the preparation of pramipexole sustained-release PLGA microspheres:Effect of fatty acids and polymer blending on the properties of microspheres[J]. J Drug Deliv Sci Technol,2025, 114:107462. White C, Schwendeman S P. Formulation and characterization of exenatide-loaded PLGA microspheres prepared by coacervation[J]. Drug Deliv Transl Res, 2025,doi:10.1007/S13346-025-02008-2. Wei P S, Chen Y J, Lin S Y, et al. In situ subcutaneously injectable thermosensitive PEG-PLGA diblock and PLGA-PEG-PLGA triblock copolymer composite as sustained delivery of bispecific anti-CD3 scFv T-cell/antiEGFR Fab Engager(BiTEE)[J]. Biomaterials, 2021, 278:121166. Pande S. Factors affecting response variables with emphasis on drug release and loading for optimization of liposomes[J]. Artif Cells Nanomed Biotechnol, 2024,52(1):334-344. Luo D, Huang L X, Bai B X, et al. Sequential drug-release microsphere system for scarless wound healing[J]. Mater Today Bio, 2025, 35:102310. 姜朝瑞,许燕,熊莹,等.氧化石墨烯复合材料载药微球的制备与性能研究[J].中国组织工程研究, 2022,26(22):3467-3473. Zhang Y, Awang Nawi M A, Shaari R, et al. Enhancing drug efficacy:A review of research progress in drugloaded microspheres[J]. Cureus, 2025, 17(8):e90498. Wang S Y, Feng X B, Liu P, et al. Blending of PLGA-PEGPLGA for improving the erosion and drug release profile of PCL microspheres[J]. Curr Pharm Biotechnol, 2020,21(11):1079-1087. Hajian M, Erfani-Moghadam V, Arabi M S, et al. A comparison between optimized PLGA and CS-Alg-PLGA microspheres for long-lasting release of glatiramer acetate[J]. J Drug Deliv Sci Technol, 2023, 82:104355.
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