Article(id=1309634588163531654, tenantId=1146029695717560320, journalId=1227999776411738115, issueId=1309634582362809158, articleNumber=null, orderNo=null, doi=10.12048/j.issn.1674-229X.2026.04.003, pmid=null, cstr=null, oa=null, hot=null, price=null, onlineType=0, articleFormat=0, articleType=null, articleTypeStr=null, receivedDate=1756310400000, receivedDateStr=2025-08-28, revisedDate=null, revisedDateStr=null, acceptedDate=null, acceptedDateStr=null, onlineDate=1790170817652, onlineDateStr=2026-09-23, pubDate=1777046400000, pubDateStr=2026-04-25, doiRegisterDate=null, doiRegisterDateStr=null, onlineIssueDate=1790170817652, onlineIssueDateStr=2026-09-23, onlineJustAcceptDate=null, onlineJustAcceptDateStr=null, onlineFirstDate=null, onlineFirstDateStr=null, sourceXml=null, magXml=null, createTime=1790170817652, creator=13701087609, updateTime=1790170817652, updator=13701087609, issue=Issue{id=1309634582362809158, tenantId=1146029695717560320, journalId=1227999776411738115, year='2026', volume='36', issue='4', pageStart='241', pageEnd='320', issueExtLink='null', onlineDate='null', pubDate='1777046400000', pubDateStr='2026-04-25', beforeIssueId=null, nextIssueId=null, price=null, status=1, issueComplete=1, articleOrder=1, issueType=-1, specialIssue=null, createTime=1790170816268, creator='13701087609', updateTime=1790219015105, updator='13701087609', preIssue=null, nextIssue=null, articleTotal=null, ext={EN=IssueExt(id=1309836742979576497, tenantId=1146029695717560320, journalId=1227999776411738115, issueId=1309634582362809158, language=EN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=), CN=IssueExt(id=1309836742979576498, tenantId=1146029695717560320, journalId=1227999776411738115, issueId=1309634582362809158, language=CN, specialIssueTitle=, coverIllustrator=null, specialIssueEditor=, specialIssueAbout=)}, issueFiles=null, downloadFileDto=null}, startPage=263, endPage=269, ext={EN=ArticleExt(id=1309634588381635463, articleId=1309634588163531654, tenantId=1146029695717560320, journalId=1227999776411738115, language=EN, title=Study on Formulation Process Optimization and Physicochemical Properties of Amikacin Liposomes Based on Reverse-phase Evaporation Method, columnId=null, journalTitle=Pharmacy Today, columnName=null, runingTitle=null, highlight=null, articleAbstract=
OBJECTIVE

In view of the limitations of amikacin intravenous administration, including poor permeability in lung tissue and significant toxic and side effects, this study adopted the reverse-phase evaporation method to prepare and optimize the formulation and process of amikacin liposomes, and systematically evaluated their physical and chemical properties, in order to provide experimental basis for lung targeted delivery.

METHODS

Amikacin liposomes were prepared by the reverse-phase evaporation method using dipalmitoylphosphatidylcholine (DPPC) and cholesterol as lipid materials. The encapsulation efficiency was determined by ultrafiltration centrifugation-HPLC. Based on the single factor investigation, the formulation and process parameters were optimized by the Box-Behnken response surface method with encapsulation efficiency as the evaluation index, and their encapsulation efficiency, morphology, particle size, polydispersity index (PDI), Zeta potential and in vitro release behavior were studied.

RESULTS

The optimum prescription process parameters were as follows: the phospholipid-to-cholesterol ratio was 4, the phospholipid concentration was 53.79 mg·mL-1, the ratio of lipid to drug was 3.78, the amount of organic solvent (chloroform) was 24.4 mL, the ultrasonic frequency was 40 times, and the rotary evaporation pressure was 600 mbar. The average encapsulation efficiency of the liposomes was (50.40 ± 0.89)%, the average particle size was (218.37 ± 2.47) nm, the PDI was (0.24 ± 0.01), and the Zeta potential was (-0.684 ± 0.21) mV. The in vitro release showed an obvious sustained release effect, with a cumulative release rate of 52.99% at 48 h, which was consistent with the Higuchi model.

CONCLUSION

The optimized preparation process of amikacin liposomes has good stability and reproducibility. The product has uniform particle size, stable morphology and sustained-release property. It has the potential advantages of achieving pulmonary targeted delivery, improving local efficacy and reducing toxic and side effects, thus laying a foundation for subsequent pharmacodynamics and safety studies.

, authors=Zhonghui CHEN1, Bin CHEN2, *, authorsList=Zhonghui CHEN, Bin CHEN, authorCompany=null, correspAuthors=Bin CHEN, 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=1309634588683625352, articleId=1309634588163531654, tenantId=1146029695717560320, journalId=1227999776411738115, language=CN, title=基于逆相蒸发法的阿米卡星脂质体处方工艺优化及理化性质研究, columnId=1228268589086606089, journalTitle=今日药学, columnName=论著, runingTitle=null, highlight=null, articleAbstract=
目的

针对阿米卡星静脉给药在肺组织渗透性差、毒副作用大等局限,本研究采用逆相蒸发法制备并优化阿米卡星脂质体处方工艺,系统评价其理化特性,以期为肺部靶向递送提供实验依据。

方法

以二棕榈酰磷脂酰胆碱(DPPC)和胆固醇为脂质材料,通过逆相蒸发法制备阿米卡星脂质体,结合超滤离心-HPLC测定包封率。以包封率为评价指标,在单因素考察的基础上,采用Box-Behnken响应面法优选处方工艺参数,并对其包封率、形态、粒径和多分散系数(PDI)、Zeta电位及体外释放行为进行研究。

结果

最佳处方工艺参数为:磷胆比4,磷脂浓度53.79 mg·mL-1,脂药比3.78,有机溶剂(三氯甲烷)用量24.4 mL,超声次数40次,旋蒸压力600 mbar。所得脂质体平均包封率为(50.40±0.89)%,平均粒径为(218.37 ± 2.47)nm,PDI为(0.24 ± 0.01),Zeta电位为(-0.684 ± 0.21)mV,体外释放具有明显的缓释效果,48 h累积释放百分率为52.99%,符合Higuchi模型。

结论

优化后的阿米卡星脂质体制备工艺稳定性与重现性良好,产物粒径均一、形态稳定且具有缓释性,有实现肺部靶向递送、提升局部药效及降低毒副作用的潜在优势,为后续药效学与安全性方面研究奠定基础。

, authors=陈中会1, 陈斌2, *, authorsList=陈中会, 陈斌, authorCompany=null, correspAuthors=陈斌, authorNote=

陈中会,在读硕士研究生,研究方向:长效缓控释制剂研究和改良型新药研发

, correspAuthorsNote=

*

陈斌,博士,高级工程师,硕士生导师,研究方向:长效缓控释制剂研究和改良型新药研发,E-mail:
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基于逆相蒸发法的阿米卡星脂质体处方工艺优化及理化性质研究
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陈中会 1 , 陈斌 2, *
今日药学 | 论著 2026,36(4): 263-269
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今日药学 |论著 2026 , 36 (4) : 263 -269
基于逆相蒸发法的阿米卡星脂质体处方工艺优化及理化性质研究
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陈中会,在读硕士研究生,研究方向:长效缓控释制剂研究和改良型新药研发

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陈中会1, 陈斌2, *
作者信息
  • 1.昆明医科大学药学院暨云南省天然药物药理重点实验室,云南 昆明 650000
  • 2.珠海市丽珠微球科技有限公司,广东 珠海 519000
通讯作者:

*

陈斌,博士,高级工程师,硕士生导师,研究方向:长效缓控释制剂研究和改良型新药研发,E-mail:
作者简介:

陈中会,在读硕士研究生,研究方向:长效缓控释制剂研究和改良型新药研发

Study on Formulation Process Optimization and Physicochemical Properties of Amikacin Liposomes Based on Reverse-phase Evaporation Method
Zhonghui CHEN1, Bin CHEN2, *
Affiliations
  • 1.School of Pharmaceutical Sciences and Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming, Yunnan 650000, China
  • 2.Zhuhai Livzon Weiqiu Technology Co., Ltd., Zhuhai, Guangdong 519000, China
出版时间: 2026-04-25 doi: 10.12048/j.issn.1674-229X.2026.04.003
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目的

针对阿米卡星静脉给药在肺组织渗透性差、毒副作用大等局限,本研究采用逆相蒸发法制备并优化阿米卡星脂质体处方工艺,系统评价其理化特性,以期为肺部靶向递送提供实验依据。

方法

以二棕榈酰磷脂酰胆碱(DPPC)和胆固醇为脂质材料,通过逆相蒸发法制备阿米卡星脂质体,结合超滤离心-HPLC测定包封率。以包封率为评价指标,在单因素考察的基础上,采用Box-Behnken响应面法优选处方工艺参数,并对其包封率、形态、粒径和多分散系数(PDI)、Zeta电位及体外释放行为进行研究。

结果

最佳处方工艺参数为:磷胆比4,磷脂浓度53.79 mg·mL-1,脂药比3.78,有机溶剂(三氯甲烷)用量24.4 mL,超声次数40次,旋蒸压力600 mbar。所得脂质体平均包封率为(50.40±0.89)%,平均粒径为(218.37 ± 2.47)nm,PDI为(0.24 ± 0.01),Zeta电位为(-0.684 ± 0.21)mV,体外释放具有明显的缓释效果,48 h累积释放百分率为52.99%,符合Higuchi模型。

结论

优化后的阿米卡星脂质体制备工艺稳定性与重现性良好,产物粒径均一、形态稳定且具有缓释性,有实现肺部靶向递送、提升局部药效及降低毒副作用的潜在优势,为后续药效学与安全性方面研究奠定基础。

阿米卡星  /  脂质体  /  逆相蒸发法  /  Box-Behnken响应面法
OBJECTIVE

In view of the limitations of amikacin intravenous administration, including poor permeability in lung tissue and significant toxic and side effects, this study adopted the reverse-phase evaporation method to prepare and optimize the formulation and process of amikacin liposomes, and systematically evaluated their physical and chemical properties, in order to provide experimental basis for lung targeted delivery.

METHODS

Amikacin liposomes were prepared by the reverse-phase evaporation method using dipalmitoylphosphatidylcholine (DPPC) and cholesterol as lipid materials. The encapsulation efficiency was determined by ultrafiltration centrifugation-HPLC. Based on the single factor investigation, the formulation and process parameters were optimized by the Box-Behnken response surface method with encapsulation efficiency as the evaluation index, and their encapsulation efficiency, morphology, particle size, polydispersity index (PDI), Zeta potential and in vitro release behavior were studied.

RESULTS

The optimum prescription process parameters were as follows: the phospholipid-to-cholesterol ratio was 4, the phospholipid concentration was 53.79 mg·mL-1, the ratio of lipid to drug was 3.78, the amount of organic solvent (chloroform) was 24.4 mL, the ultrasonic frequency was 40 times, and the rotary evaporation pressure was 600 mbar. The average encapsulation efficiency of the liposomes was (50.40 ± 0.89)%, the average particle size was (218.37 ± 2.47) nm, the PDI was (0.24 ± 0.01), and the Zeta potential was (-0.684 ± 0.21) mV. The in vitro release showed an obvious sustained release effect, with a cumulative release rate of 52.99% at 48 h, which was consistent with the Higuchi model.

CONCLUSION

The optimized preparation process of amikacin liposomes has good stability and reproducibility. The product has uniform particle size, stable morphology and sustained-release property. It has the potential advantages of achieving pulmonary targeted delivery, improving local efficacy and reducing toxic and side effects, thus laying a foundation for subsequent pharmacodynamics and safety studies.

amikacin  /  liposomes  /  reverse-phase evaporation method  /  Box-Behnken response surface method
陈中会, 陈斌. 基于逆相蒸发法的阿米卡星脂质体处方工艺优化及理化性质研究. 今日药学, 2026 , 36 (4) : 263 -269 . DOI: 10.12048/j.issn.1674-229X.2026.04.003
Zhonghui CHEN, Bin CHEN. Study on Formulation Process Optimization and Physicochemical Properties of Amikacin Liposomes Based on Reverse-phase Evaporation Method[J]. Pharmacy Today, 2026 , 36 (4) : 263 -269 . DOI: 10.12048/j.issn.1674-229X.2026.04.003
  • “重大新药创制”国家科技重大专项基金资助项目(2017ZX09201004)
  • 广东省“珠江人才计划”引进第六批创新创业团队资助项目(2016ZT06Y229)
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doi: 10.12048/j.issn.1674-229X.2026.04.003
  • 接收时间:2025-08-28
  • 首发时间:2026-09-23
  • 出版时间:2026-04-25
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  • 收稿日期:2025-08-28
基金
“重大新药创制”国家科技重大专项基金资助项目(2017ZX09201004)
广东省“珠江人才计划”引进第六批创新创业团队资助项目(2016ZT06Y229)
作者信息
    1.昆明医科大学药学院暨云南省天然药物药理重点实验室,云南 昆明 650000
    2.珠海市丽珠微球科技有限公司,广东 珠海 519000

通讯作者:

*

陈斌,博士,高级工程师,硕士生导师,研究方向:长效缓控释制剂研究和改良型新药研发,E-mail:
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2种不同金属材料的力学参数
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鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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