{"title":"利匹韦林纳米吸附体的制剂开发和体外评估","authors":"Purnima Rawat, Sharad Gupta, Syed Sarim Imam","doi":"10.1007/s12247-024-09852-8","DOIUrl":null,"url":null,"abstract":"<div><p>This study focused on the preparation and characterization of rilpivirine-loaded nanobilosomes. Formulations were developed using rilpivirine, phosphatidylcholine S-100 (SPC), and sodium deoxycholate (SDC) via the thin film hydration method. The nanobilosomes were characterized for vesicle size, polydispersity index (PDI), surface charge, and entrapment efficiency (%EE). Thermal behavior and drug-excipient interactions were analyzed using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). Transmission electron microscopy (TEM) revealed that BS-06 nanobilosomes possess a smooth and uniform surface morphology. In vitro cytotoxicity assays were conducted on HeLa and HEK 293 cell lines, and minimum inhibitory concentration (MIC) was assessed against S. aureus and E. coli. Stability was monitored over 3 months at various temperatures. The optimized formulation (BS-06) exhibited a vesicle size of 132.8 ± 4.0 nm, a zeta potential of -30.10 ± 0.8 mV, and a PDI of 0.20, demonstrating optimal surface characteristics and maximum entrapment efficiency. In vitro release studies indicated a maximum drug release of 84.81 ± 4.6% over 24 h. Cytotoxicity studies showed that BS-06 improved cell viability in HeLa and HEK 293 cell lines at 24 and 48 h and enhanced antibacterial activity against S. aureus and E. coli. Overall, our findings highlight the potential of rilpivirine-loaded nanobilosomes as a promising drug delivery system for HIV/AIDS, with enhanced dissolution, stability and biocompatibility.</p></div>","PeriodicalId":656,"journal":{"name":"Journal of Pharmaceutical Innovation","volume":"19 4","pages":""},"PeriodicalIF":2.7000,"publicationDate":"2024-07-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Formulation Development and In-Vitro Assessment of Rilpivirine Nanobilosomes\",\"authors\":\"Purnima Rawat, Sharad Gupta, Syed Sarim Imam\",\"doi\":\"10.1007/s12247-024-09852-8\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>This study focused on the preparation and characterization of rilpivirine-loaded nanobilosomes. Formulations were developed using rilpivirine, phosphatidylcholine S-100 (SPC), and sodium deoxycholate (SDC) via the thin film hydration method. The nanobilosomes were characterized for vesicle size, polydispersity index (PDI), surface charge, and entrapment efficiency (%EE). Thermal behavior and drug-excipient interactions were analyzed using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). Transmission electron microscopy (TEM) revealed that BS-06 nanobilosomes possess a smooth and uniform surface morphology. In vitro cytotoxicity assays were conducted on HeLa and HEK 293 cell lines, and minimum inhibitory concentration (MIC) was assessed against S. aureus and E. coli. Stability was monitored over 3 months at various temperatures. The optimized formulation (BS-06) exhibited a vesicle size of 132.8 ± 4.0 nm, a zeta potential of -30.10 ± 0.8 mV, and a PDI of 0.20, demonstrating optimal surface characteristics and maximum entrapment efficiency. In vitro release studies indicated a maximum drug release of 84.81 ± 4.6% over 24 h. Cytotoxicity studies showed that BS-06 improved cell viability in HeLa and HEK 293 cell lines at 24 and 48 h and enhanced antibacterial activity against S. aureus and E. coli. Overall, our findings highlight the potential of rilpivirine-loaded nanobilosomes as a promising drug delivery system for HIV/AIDS, with enhanced dissolution, stability and biocompatibility.</p></div>\",\"PeriodicalId\":656,\"journal\":{\"name\":\"Journal of Pharmaceutical Innovation\",\"volume\":\"19 4\",\"pages\":\"\"},\"PeriodicalIF\":2.7000,\"publicationDate\":\"2024-07-19\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Pharmaceutical Innovation\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://link.springer.com/article/10.1007/s12247-024-09852-8\",\"RegionNum\":4,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"PHARMACOLOGY & PHARMACY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Pharmaceutical Innovation","FirstCategoryId":"3","ListUrlMain":"https://link.springer.com/article/10.1007/s12247-024-09852-8","RegionNum":4,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
Formulation Development and In-Vitro Assessment of Rilpivirine Nanobilosomes
This study focused on the preparation and characterization of rilpivirine-loaded nanobilosomes. Formulations were developed using rilpivirine, phosphatidylcholine S-100 (SPC), and sodium deoxycholate (SDC) via the thin film hydration method. The nanobilosomes were characterized for vesicle size, polydispersity index (PDI), surface charge, and entrapment efficiency (%EE). Thermal behavior and drug-excipient interactions were analyzed using differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR). Transmission electron microscopy (TEM) revealed that BS-06 nanobilosomes possess a smooth and uniform surface morphology. In vitro cytotoxicity assays were conducted on HeLa and HEK 293 cell lines, and minimum inhibitory concentration (MIC) was assessed against S. aureus and E. coli. Stability was monitored over 3 months at various temperatures. The optimized formulation (BS-06) exhibited a vesicle size of 132.8 ± 4.0 nm, a zeta potential of -30.10 ± 0.8 mV, and a PDI of 0.20, demonstrating optimal surface characteristics and maximum entrapment efficiency. In vitro release studies indicated a maximum drug release of 84.81 ± 4.6% over 24 h. Cytotoxicity studies showed that BS-06 improved cell viability in HeLa and HEK 293 cell lines at 24 and 48 h and enhanced antibacterial activity against S. aureus and E. coli. Overall, our findings highlight the potential of rilpivirine-loaded nanobilosomes as a promising drug delivery system for HIV/AIDS, with enhanced dissolution, stability and biocompatibility.
期刊介绍:
The Journal of Pharmaceutical Innovation (JPI), is an international, multidisciplinary peer-reviewed scientific journal dedicated to publishing high quality papers emphasizing innovative research and applied technologies within the pharmaceutical and biotechnology industries. JPI''s goal is to be the premier communication vehicle for the critical body of knowledge that is needed for scientific evolution and technical innovation, from R&D to market. Topics will fall under the following categories:
Materials science,
Product design,
Process design, optimization, automation and control,
Facilities; Information management,
Regulatory policy and strategy,
Supply chain developments ,
Education and professional development,
Journal of Pharmaceutical Innovation publishes four issues a year.