Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance
The aim of this study was to prepare polymeric micelles composed of enrofloxacin (ENR) and methoxy poly (ethylene glycol)-poly(lactide) (mPEG-PLLA) using a solvent evaporation method to overcome the solubility-limited oral bioavailability of ENR. The formulation was optimized using a Box–Behnken des...
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Frontiers Media S.A.
2025-07-01
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| Series: | Frontiers in Veterinary Science |
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| Online Access: | https://www.frontiersin.org/articles/10.3389/fvets.2025.1595137/full |
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| author | Yanling Sun Yanan Mao Xin He Xinghua Zhao |
| author_facet | Yanling Sun Yanan Mao Xin He Xinghua Zhao |
| author_sort | Yanling Sun |
| collection | DOAJ |
| description | The aim of this study was to prepare polymeric micelles composed of enrofloxacin (ENR) and methoxy poly (ethylene glycol)-poly(lactide) (mPEG-PLLA) using a solvent evaporation method to overcome the solubility-limited oral bioavailability of ENR. The formulation was optimized using a Box–Behnken design (BBD) to obtain ENR polymeric micelles (ENR-m) with high drug loading (DL, %) and entrapment efficiency (EE, %). The physicochemical properties, in vitro drug release, pharmacokinetics, and antibacterial efficacy were evaluated in comparison to pure ENR. ENR-m was successfully prepared and demonstrated satisfactory drug loading (68.38 ± 0.22%), entrapment efficiency (88.40 ± 0.91%), particle size (PS) (133.67 ± 3.10 nm), and polydispersity index (PDI) (0.13 ± 0.03). The ENR-m also exhibited excellent stability under environmental conditions (40°C and 75% relative humidity (RH)). In vitro release of ENR from micelles was accelerated in a PBS solution. A pharmacokinetic study on beagles revealed that the oral bioavailability of ENR-m was enhanced by approximately 1.60-fold compared to pure ENR (p < 0.01) and by 1.66-fold compared to commercially available tablets of ENR (p < 0.01). The antibacterial activity of ENR-m against Escherichia coli (E. coli) and Salmonella typhi (S. typhi) was stronger than that of pure ENR. |
| format | Article |
| id | doaj-art-0fd34a588ba044ef8ceb231fbbcd3e57 |
| institution | Kabale University |
| issn | 2297-1769 |
| language | English |
| publishDate | 2025-07-01 |
| publisher | Frontiers Media S.A. |
| record_format | Article |
| series | Frontiers in Veterinary Science |
| spelling | doaj-art-0fd34a588ba044ef8ceb231fbbcd3e572025-08-20T03:27:43ZengFrontiers Media S.A.Frontiers in Veterinary Science2297-17692025-07-011210.3389/fvets.2025.15951371595137Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performanceYanling SunYanan MaoXin HeXinghua ZhaoThe aim of this study was to prepare polymeric micelles composed of enrofloxacin (ENR) and methoxy poly (ethylene glycol)-poly(lactide) (mPEG-PLLA) using a solvent evaporation method to overcome the solubility-limited oral bioavailability of ENR. The formulation was optimized using a Box–Behnken design (BBD) to obtain ENR polymeric micelles (ENR-m) with high drug loading (DL, %) and entrapment efficiency (EE, %). The physicochemical properties, in vitro drug release, pharmacokinetics, and antibacterial efficacy were evaluated in comparison to pure ENR. ENR-m was successfully prepared and demonstrated satisfactory drug loading (68.38 ± 0.22%), entrapment efficiency (88.40 ± 0.91%), particle size (PS) (133.67 ± 3.10 nm), and polydispersity index (PDI) (0.13 ± 0.03). The ENR-m also exhibited excellent stability under environmental conditions (40°C and 75% relative humidity (RH)). In vitro release of ENR from micelles was accelerated in a PBS solution. A pharmacokinetic study on beagles revealed that the oral bioavailability of ENR-m was enhanced by approximately 1.60-fold compared to pure ENR (p < 0.01) and by 1.66-fold compared to commercially available tablets of ENR (p < 0.01). The antibacterial activity of ENR-m against Escherichia coli (E. coli) and Salmonella typhi (S. typhi) was stronger than that of pure ENR.https://www.frontiersin.org/articles/10.3389/fvets.2025.1595137/fullenrofloxacinMPEG-PLLAmicellesoral bioavailabilityantibacterial activity |
| spellingShingle | Yanling Sun Yanan Mao Xin He Xinghua Zhao Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance Frontiers in Veterinary Science enrofloxacin MPEG-PLLA micelles oral bioavailability antibacterial activity |
| title | Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance |
| title_full | Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance |
| title_fullStr | Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance |
| title_full_unstemmed | Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance |
| title_short | Development and evaluation of mPEG-PLLA polymeric micelles encapsulating enrofloxacin for enhanced solubility, bioavailability, and antibacterial performance |
| title_sort | development and evaluation of mpeg plla polymeric micelles encapsulating enrofloxacin for enhanced solubility bioavailability and antibacterial performance |
| topic | enrofloxacin MPEG-PLLA micelles oral bioavailability antibacterial activity |
| url | https://www.frontiersin.org/articles/10.3389/fvets.2025.1595137/full |
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