Abstract
In order to achieve sustained and controlled release of the hydrophobic cargoes, improve the bioavailability, and reduce the side effects of antibiotics, the model drug erythromycin (EM) was used to prepare polycaprolactone-polyethylene glycol (PCL-PEG)/EM micelles. PCL-PEG, a biocompatible and biodegradable amphiphilic polymer, was used as carrier material of micelles to optimize the formulation and preparation process by orthogonal design. The morphology, stability, drug loading, and encapsulation efficiency and the in vitro release behavior of the micelles were investigated. In addition, activity assays of anti-Staphylococcus aureus were performed. The results indicated that PCL-PEG/EM were rod-like micelles with an average particle size of 220 ± 2.6 nm and a zeta potential of +19 mV. The average drug loading and encapsulation efficiency were approximately 6.5% and 97.0%, respectively. The micelles were stable in the serum within three days. At the effective concentration of the drug, the formulation indicated no apparent toxicity to the cells. The micelles were able to rapidly enter Staphylococcus aureus (S. aureus) and to provide sustained release cargoes that effectively inhibited S. aureus proliferation. The present study provided a new platform for the rational and effective use of hydrophobic antibiotics to treat infections.
Highlights
Macrolide antibiotics have a broad antibacterial spectrum, mainly by inhibiting the synthesis of bacterial proteins that possess antibacterial roles
As noted from the tables below, when the mass fraction of PCL2000-PEG2000 ranged between 0% and 50%, the drug loading was approximately 5% to 20%, the rotary steam temperature was between 30°C and 40°C, and the volume ratio of tetrahydrofuran to deionized water was 3 : 1 to 5 : 1. Under these conditions, the micelles with optimal stability could be obtained within three days
The following four main factors were included: mass ratio of different carrier materials (A), drug loading capacity (B), rotary steaming temperature (C), and the amount of THF used during the process (D)
Summary
Macrolide antibiotics have a broad antibacterial spectrum, mainly by inhibiting the synthesis of bacterial proteins that possess antibacterial roles These compounds exhibit apparent antibacterial effects on a variety of Gram-positive, Gram-negative, and anaerobic bacteria [1]. The aforementioned shortcomings severely restrict the effective use of antibacterial drugs and cause unnecessary damage to the human body. Several hydrophobic antibiotics can be assembled into nanoformulations to achieve safe and efficient delivery in the body [14], which can increase the drug concentration in the lesions when the same dose is administered. To develop a stable and long-acting EM injection preparation that reduces local drug side effects, PCL-PEG was selected as a carrier material to prepare EM-loaded micelles.
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