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Preparation and Characterization of Nanoliposomes for the Entrapment of Bioactive Hydrophilic Globular Proteins
Published on: August 31, 2019
Piperacillin Encapsulation in Nanoliposomes Using Modified Freeze-Drying of a Monophase Solution Method: Preparation,
Pouria Savadi1, Telli Taghavi-Fard1, Morteza Milani2
1Student Research Committee, Tabriz University of Medical Sciences, Tabriz, Iran.
Abstract:
Piperacillin (Pip) is a broad spectrum β-lactam against most Gram-positive and Gram-negative aerobic and anaerobic bacteria. However, bacterial resistance restricts its benefits for the treatment of infectious diseases. Recently, nanoliposomal systems have been investigated as encouraging strategies to address this issue owing to their immense potential. We aimed to encapsulate Pip in liposomal nanoparticles and study their antibacterial activities in vitro against Pseudomonas aeruginosa (P. aeruginosa). Different liposomes were prepared based on the freeze-drying of a monophase solution method. Then, they were characterized in terms of size, zeta potential, polydispersity-index, and morphology. For further analysis, spectra of ATR-FTIR and XRD were taken for liposomal Pip. Encapsulation efficiency (EE) was determined via agar diffusion assay. Also, minimum inhibitory concentrations (MICs) were investigated by the standard broth macro-dilution method. The liposomes were from 100.9 to 444.13 nm with z-potential of - 30.70 to - 10.57 mV. EE of the selected formulation was 53.1%. TEM results showed that the liposomes were nanosized and almost spherical. ATR-FTIR results confirmed the full encapsulation of Pip in nanoliposomes. The X-ray pattern indicated that the liposomal Pip was amorphous. The MIC (10.6 µg/ml) of the nanoliposomal Pip against P. aeruginosa was one-half of the MIC (21.25 µg/ml) of free Pip for the same organisms. Considering four aspects (nanosized liposomes, no need for sterilization, suitable EE and enhanced antibacterial effects), this preparation method seems promising and may be used to overcome the bacterial resistance relative to Pip.
Insights
Nanoliposomal encapsulation of piperacillin (Pip) enhanced its antibacterial activity against Pseudomonas aeruginosa. This novel formulation shows promise for overcoming bacterial resistance to this important antibiotic.
Area of Science:
- Pharmaceutical Sciences
- Nanotechnology
- Microbiology
Background:
- Piperacillin (Pip) is a broad-spectrum antibiotic facing challenges due to bacterial resistance.
- Nanoliposomal systems offer a promising strategy to enhance drug delivery and efficacy.
- Addressing antibiotic resistance is crucial for effective infectious disease treatment.
Purpose of the Study:
- To encapsulate piperacillin (Pip) into liposomal nanoparticles.
- To characterize the physicochemical properties of the nanoliposomal formulation.
- To evaluate the in vitro antibacterial activity of nanoliposomal Pip against Pseudomonas aeruginosa.
Main Methods:
- Liposomes were prepared using a freeze-drying method.
- Characterization included size, zeta potential, polydispersity index, and morphology (TEM).
- Encapsulation efficiency (EE) and minimum inhibitory concentrations (MICs) were determined.
Main Results:
- Nanoliposomes ranged from 100.9 to 444.13 nm with a zeta potential of -30.70 to -10.57 mV.
- Encapsulation efficiency of the selected formulation was 53.1%.
- Nanoliposomal Pip showed a twofold lower MIC (10.6 µg/ml) against P. aeruginosa compared to free Pip (21.25 µg/ml).
Conclusions:
- The developed nanoliposomal piperacillin formulation is nanosized, spherical, and exhibits good encapsulation.
- The nanoliposomal formulation significantly enhances antibacterial efficacy against P. aeruginosa.
- This approach shows potential for overcoming piperacillin resistance and improving infectious disease treatment.

