Misra Ranjita, Sahoo Sanjeeb K
Institute of Life Sciences, Chandrasekharpur, Bhubaneswar, Orissa, India.
Methods Enzymol. 2012;509:61-85. doi: 10.1016/B978-0-12-391858-1.00004-6.
Doxycycline is a tetracycline antibiotic with a potent antibacterial activity against a wide variety of bacteria. However, poor cellular penetration limits its use for the treatment of infectious disease caused by intracellular pathogens. One potential strategy to overcome this problem is the use of nanotechnology that can help to easily target the intracellular sites of infection. The antibacterial activity of these antibiotics is enhanced by encapsulating it in polymeric nanoparticles. In this study, we describe the improvement of the entrapment efficiency of doxycycline hydrochloride (doxycycline)-loaded PLGA:PCL nanoparticles up to 70% with variation of different formulation parameters such as polymer ratio, amount of drug loading (w/w), solvent selection, electrolyte addition, and pH alteration in the formulation. We have evaluated the efficacy of these nanoparticles over native doxycycline against a strain of Escherichia coli (DH5α) through growth inhibition and colony counting. The results indicate that doxycycline-loaded nanoparticles have superior effectiveness compared to native doxycycline against the above bacterial strain, resulting from the sustained release of doxycycline from nanoparticles. These results are encouraging for the use of these doxycycline-loaded nanoparticles for the treatment of infections caused by doxycycline-sensitive bacteria.
强力霉素是一种四环素类抗生素,对多种细菌具有强大的抗菌活性。然而,其较差的细胞穿透性限制了它在治疗由细胞内病原体引起的传染病方面的应用。克服这一问题的一种潜在策略是使用纳米技术,该技术有助于轻松靶向感染的细胞内位点。通过将这些抗生素包裹在聚合物纳米颗粒中可增强其抗菌活性。在本研究中,我们描述了通过改变不同的制剂参数,如聚合物比例、载药量(w/w)、溶剂选择、电解质添加以及制剂中的pH值变化,将载盐酸强力霉素(强力霉素)的聚乳酸-羟基乙酸共聚物(PLGA):聚己内酯(PCL)纳米颗粒的包封率提高至70%。我们通过生长抑制和菌落计数评估了这些纳米颗粒相对于天然强力霉素对大肠杆菌(DH5α)菌株的疗效。结果表明,与天然强力霉素相比,载强力霉素纳米颗粒对上述细菌菌株具有更优异的效果,这是由于强力霉素从纳米颗粒中持续释放所致。这些结果对于使用这些载强力霉素纳米颗粒治疗由强力霉素敏感细菌引起的感染是令人鼓舞的。