K. M. Himani, Subbaiyan Anbazhagan, Lakshmi Prakasan, Prasad Thomas, Akhilesh Kumar, Krishnaswamy Narayanan, Praveen Singh, Pallab Chaudhuri
{"title":"增强多西环素和利福平固体脂质纳米颗粒对流产布鲁氏菌的安全性和治疗效果","authors":"K. M. Himani, Subbaiyan Anbazhagan, Lakshmi Prakasan, Prasad Thomas, Akhilesh Kumar, Krishnaswamy Narayanan, Praveen Singh, Pallab Chaudhuri","doi":"10.1186/s43094-024-00753-8","DOIUrl":null,"url":null,"abstract":"<div><h3>Background</h3><p>Prolonged therapy, hepatic damage, and the development of drug resistance are the limitations of doxycycline and rifampicin in the treatment of brucellosis. This study was designed to assess the effect of solid lipid nanoparticles (SLNs) encapsulation of these antimicrobials against brucella. SLNs were prepared by a double emulsion method and characterized for entrapment efficiency, particle size distribution, drug release, infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy. The encapsulated formulations were tested for stability, safety, and in vitro antimicrobial assay on brucella and <i>brucella-infected</i> mice models.</p><h3>Results</h3><p>The particle size, polydispersity index and zeta potential of doxycycline encapsulated SLN size were 443.6 ± 3.03 nm, 0.858 ± 0.00, and + 26.5 ± 1.87 mV, respectively. The rifampicin SLN showed particle size, polydispersity index, and zeta potential of 348.7 ± 3.35 nm, 0.234 ± 0.00, and + 22.9 ± 1.59 mV. The entrapment efficiency of doxycycline and rifampicin encapsulated SLN was 98% and 96%, respectively. The drug-loaded SLN retained the biophysical properties, drug loading, and entrapment efficiency after storage at 4 °C as well as 25 °C for 6 months. The Fourier transform infrared spectroscopy depicted effective encapsulation and the Differential scanning colorimetry thermogram revealed a negative interaction of drug and polymer. Drug release parameters were fitted well with the Korsmeyer–Peppas and Hixson–Crowell model (<i>R</i>2 ≥ .09). The MIC findings showed a reduction in MIC values of SLN-encapsulated rifampicin; whereas, doxycycline did not show any changes. The MBC value for free and SLN-encapsulated doxycycline and rifampicin did not show changes. SLN encapsulation did not show any cytotoxicity on murine macrophage cell line RAW 264.76 for both drugs. Doxycycline and rifampicin significantly reduced the CFU of <i>B. abortus</i> compared to the free drug (<i>P</i> > 0.05), resulting in less damage to the liver and kidneys.</p><h3>Conclusions</h3><p>The present study concludes that SLN encapsulation of doxycycline and rifampicin would be safe and effective for the prolonged treatment regimen against Brucella infection.</p><h3>Graphical abstract</h3>\n<div><figure><div><div><picture><source><img></source></picture></div></div></figure></div></div>","PeriodicalId":577,"journal":{"name":"Future Journal of Pharmaceutical Sciences","volume":"10 1","pages":""},"PeriodicalIF":3.4000,"publicationDate":"2024-12-23","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://fjps.springeropen.com/counter/pdf/10.1186/s43094-024-00753-8","citationCount":"0","resultStr":"{\"title\":\"Augmenting the safety and therapeutic efficacy of doxycycline and rifampicin-loaded solid lipid nanoparticles against Brucella abortus using murine model\",\"authors\":\"K. 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The encapsulated formulations were tested for stability, safety, and in vitro antimicrobial assay on brucella and <i>brucella-infected</i> mice models.</p><h3>Results</h3><p>The particle size, polydispersity index and zeta potential of doxycycline encapsulated SLN size were 443.6 ± 3.03 nm, 0.858 ± 0.00, and + 26.5 ± 1.87 mV, respectively. The rifampicin SLN showed particle size, polydispersity index, and zeta potential of 348.7 ± 3.35 nm, 0.234 ± 0.00, and + 22.9 ± 1.59 mV. The entrapment efficiency of doxycycline and rifampicin encapsulated SLN was 98% and 96%, respectively. The drug-loaded SLN retained the biophysical properties, drug loading, and entrapment efficiency after storage at 4 °C as well as 25 °C for 6 months. The Fourier transform infrared spectroscopy depicted effective encapsulation and the Differential scanning colorimetry thermogram revealed a negative interaction of drug and polymer. 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Augmenting the safety and therapeutic efficacy of doxycycline and rifampicin-loaded solid lipid nanoparticles against Brucella abortus using murine model
Background
Prolonged therapy, hepatic damage, and the development of drug resistance are the limitations of doxycycline and rifampicin in the treatment of brucellosis. This study was designed to assess the effect of solid lipid nanoparticles (SLNs) encapsulation of these antimicrobials against brucella. SLNs were prepared by a double emulsion method and characterized for entrapment efficiency, particle size distribution, drug release, infrared spectroscopy, differential scanning calorimetry, and scanning electron microscopy. The encapsulated formulations were tested for stability, safety, and in vitro antimicrobial assay on brucella and brucella-infected mice models.
Results
The particle size, polydispersity index and zeta potential of doxycycline encapsulated SLN size were 443.6 ± 3.03 nm, 0.858 ± 0.00, and + 26.5 ± 1.87 mV, respectively. The rifampicin SLN showed particle size, polydispersity index, and zeta potential of 348.7 ± 3.35 nm, 0.234 ± 0.00, and + 22.9 ± 1.59 mV. The entrapment efficiency of doxycycline and rifampicin encapsulated SLN was 98% and 96%, respectively. The drug-loaded SLN retained the biophysical properties, drug loading, and entrapment efficiency after storage at 4 °C as well as 25 °C for 6 months. The Fourier transform infrared spectroscopy depicted effective encapsulation and the Differential scanning colorimetry thermogram revealed a negative interaction of drug and polymer. Drug release parameters were fitted well with the Korsmeyer–Peppas and Hixson–Crowell model (R2 ≥ .09). The MIC findings showed a reduction in MIC values of SLN-encapsulated rifampicin; whereas, doxycycline did not show any changes. The MBC value for free and SLN-encapsulated doxycycline and rifampicin did not show changes. SLN encapsulation did not show any cytotoxicity on murine macrophage cell line RAW 264.76 for both drugs. Doxycycline and rifampicin significantly reduced the CFU of B. abortus compared to the free drug (P > 0.05), resulting in less damage to the liver and kidneys.
Conclusions
The present study concludes that SLN encapsulation of doxycycline and rifampicin would be safe and effective for the prolonged treatment regimen against Brucella infection.
期刊介绍：
Future Journal of Pharmaceutical Sciences (FJPS) is the official journal of the Future University in Egypt. It is a peer-reviewed, open access journal which publishes original research articles, review articles and case studies on all aspects of pharmaceutical sciences and technologies, pharmacy practice and related clinical aspects, and pharmacy education. The journal publishes articles covering developments in drug absorption and metabolism, pharmacokinetics and dynamics, drug delivery systems, drug targeting and nano-technology. It also covers development of new systems, methods and techniques in pharmacy education and practice. The scope of the journal also extends to cover advancements in toxicology, cell and molecular biology, biomedical research, clinical and pharmaceutical microbiology, pharmaceutical biotechnology, medicinal chemistry, phytochemistry and nutraceuticals.
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