关键词: antibacterial activity cyclodextrin–oligolactide electrospinning enrofloxacin nanofibers

来  源:   DOI:10.3390/pharmaceutics16070903   PDF(Pubmed)

Abstract:
Enrofloxacin (ENR), a member of the fluoroquinolone class of antibiotics, is widely used in veterinary medicine to treat bacterial infections. Like many antibiotics, ENR has limited water solubility and low bioavailability. To address these challenges, drug formulations using solid dispersions, nanosuspensions, surfactants, cocrystal/salt formation, and inclusion complexes with cyclodextrins may be employed. The approach described herein proposes the development of ENR formulations by co-electrospinning ENR with custom-prepared cyclodextrin-oligolactide (CDLA) derivatives. This method benefits from the high solubility of these derivatives, enabling polymer-free electrospinning. The electrospinning parameters were optimized to incorporate significant amounts of ENR into the CDLA nanofibrous webs, reaching up to 15.6% by weight. The obtained formulations were characterized by FTIR and NMR spectroscopy methods and evaluated for their antibacterial activity against Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. This study indicates that the presence of CDLA derivative does not inhibit the antibacterial activity of ENR, recommending these formulations for further development.
摘要:
恩诺沙星(ENR),氟喹诺酮类抗生素的一员,在兽医学中广泛用于治疗细菌感染。像许多抗生素一样,ENR具有有限的水溶性和低生物利用度。为了应对这些挑战,使用固体分散体的药物制剂,纳米悬浮液,表面活性剂,共晶/盐形成,并且可以使用与环糊精的包合复合物。本文所述的方法提出了通过将ENR与定制制备的环糊精-低聚丙交酯(CDLA)衍生物共电纺丝来开发ENR制剂。这种方法得益于这些衍生物的高溶解度,实现无聚合物静电纺丝。优化静电纺丝参数以将大量的ENR掺入到CDLA纳米纤维网中。达到15.6%的重量。通过FTIR和NMR光谱方法对获得的制剂进行表征,并评估其对金黄色葡萄球菌的抗菌活性。大肠杆菌,还有铜绿假单胞菌.这项研究表明,CDLA衍生物的存在不会抑制ENR的抗菌活性,推荐这些配方进行进一步开发。
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