Characterization of chitosan-coated PLGA nanoemulsion loaded with cepharanthine and inhibitory effect on
Ruonan Bo1, Jiahao Wu2, Ya Tao2
1College of Veterinary Medicine, Jiangsu Co-innovation Center for Prevention and Control of Important Animal Infectious Diseases and Zoonoses, Yangzhou University, Yangzhou 225009, China; Joint International Research Laboratory of Agriculture and Agri-Product Safety, The Ministry of Education of China, Yangzhou University, Yangzhou 225009, China.
Abstract:
Staphylococcus aureus (S. aureus), particularly methicillin-resistant strains (MRSA), poses a significant threat to global public health due to its resistance to conventional antibiotics. The urgent need for alternative treatments has highlighted cepharanthine (CEP), a bisbenzylisoquinoline alkaloid, known for its antiviral, antibacterial, and anti-inflammatory properties. However, the clinical application of CEP is constrained by several factors. These include the requirement for a high therapeutic dosage, low aqueous solubility, restricted oral absorption, and a short half - life. In this study, we developed a chitosan-coated Poly Lactic-co-Glycolic Acid (PLGA) nanoemulsion encapsulating CEP (CCPN) using the double-emulsion solvent evaporation method. The formulation was optimized to achieve ideal physicochemical properties, including a particle size of 588.13 ± 31.87 nm and a zeta potential of 48.60 ± 1.00 mV, ensuring stability and uniformity. Biological evaluations demonstrated that CCPN effectively inhibited hemolysis, suppressed biofilm formation, disrupted mature biofilms, and displayed potent antibacterial activity against S. aureus. In vivo studies using a murine pneumonia model revealed that CCPN significantly alleviated lung damage, reduced bacterial load, mitigated inflammatory responses, and improved survival rates of mice infected with S. aureus or MRSA. These findings highlight CCPN as a promising therapeutic strategy for treating bacterial pneumonia. This novel nanoemulsion effectively tackles the key limitations in antimicrobial therapy by boosting the solubility, stability, and antibacterial efficacy of CEP. It holds great promise in the fight against antibiotic - resistant infections and shows substantial potential for promoting the treatment of pulmonary diseases.
Insights
A novel nanoemulsion effectively delivers cepharanthine (CEP) to combat antibiotic-resistant Staphylococcus aureus infections. This formulation improves CEP
Area of Science:
- Nanotechnology in Medicine
- Antimicrobial Drug Development
- Infectious Diseases
Background:
- Staphylococcus aureus (S. aureus), including methicillin-resistant strains (MRSA), is a major public health threat due to antibiotic resistance.
- Cepharanthine (CEP) exhibits antibacterial properties but faces limitations like poor solubility and short half-life.
- Novel drug delivery systems are crucial for overcoming challenges in treating resistant bacterial infections.
Purpose of the Study:
- To develop a chitosan-coated Poly Lactic-co-Glycolic Acid (PLGA) nanoemulsion (CCPN) for enhanced delivery of cepharanthine (CEP).
- To evaluate the physicochemical properties, in vitro antibacterial activity, and in vivo efficacy of CCPN against S. aureus and MRSA.
- To address the limitations of conventional CEP therapy for bacterial pneumonia.
Main Methods:
- Developed a chitosan-coated PLGA nanoemulsion (CCPN) encapsulating CEP using the double-emulsion solvent evaporation method.
- Optimized CCPN for particle size (588.13 nm) and zeta potential (48.60 mV) for stability.
- Conducted in vitro assays for hemolysis, biofilm inhibition/disruption, and antibacterial activity.
- Performed in vivo studies using a murine pneumonia model to assess lung damage, bacterial load, inflammation, and survival rates.
Main Results:
- CCPN exhibited optimal physicochemical properties, ensuring formulation stability.
- In vitro studies showed CCPN effectively inhibited hemolysis, suppressed and disrupted S. aureus biofilms, and demonstrated potent antibacterial activity.
- In vivo studies revealed CCPN significantly reduced lung damage, bacterial load, and inflammation, while improving survival rates in a murine pneumonia model.
Conclusions:
- The developed CCPN formulation is a promising therapeutic strategy for treating bacterial pneumonia caused by S. aureus and MRSA.
- CCPN enhances CEP's solubility, stability, and antibacterial efficacy, overcoming key limitations of traditional antimicrobial therapy.
- This novel nanoemulsion holds significant potential for combating antibiotic-resistant infections and treating pulmonary diseases.
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