Encapsulation of Enrofloxacin in Liposomes I: Preparation and In Vitro Characterization of LUV

Abstract

Liposomes are effectively used in the treatment of microbial infections. Higher cellular uptake has been reported when antibiotics are encapsulated in liposomes. In this study, enrofloxacin (ENF) was encapsulated in large unilamellar vesicles (LUVs) and the effects of formulation variables on the liposome characteristics were investigated. Liposomes were prepared using dry lipid film method. A number of variables such as molar ratios of phospholipid (DPPC; DL-alpha-phosphatidylcholine dipalmitoyl), cholesterol, ENF and amount of alpha-tocopherol and the volumes of internal (chloroform) and external phases [phosphate buffered saline PBS (pH 7.4)] were studied. In vitro characterization of the liposomes including the encapsulation capacity, size and drug release properties were carried out. Using of this method, spherical LUV liposomes with high drug content could be produced. Particle size of liposomes changed between 3.12 and 4.95 microm. The molar ratios of DPPC, cholesterol and ENF affected the size of the liposome (p < 0.05). The drug encapsulation capacities were high and changed between 37.1% and 79.5%. The highest ENF encapsulation was obtained with the highest cholesterol content. An increase in the drug encapsulation capacity of the liposome was found with increasing molar ratios of DPPC, cholesterol and ENF (p < 0.05). Furthermore, the release of ENF from the liposomes decreased as the molar ratios of DPPC, cholesterol and ENF increased (p < 0.05). In conclusion, a convenient colloidal carrier for the controlled release of ENF can be prepared by changing the formulation parameters of LUVs.

Cytologic-Enzymologic Diagnosis of Experimental Pneumonia Induced by Klebsiella pneumoniae Serotype II in Rats and Its Treatment with Free and Liposomal Enrofloxacin

“…We suggest that increasing the drug encapsulation capacity produced the slow release of ENR. This result was similar to the results found in the literature 3,13,14 . The optimized LUVs with the appropriate particle size and distribution, high surface charge and drug release properties used in the in vitro studies were chosen for use in the in vivo experiments, and the treatment efficacy on rats with experimental pneumonia was partially investigated.…”

“…In this study, ENR-loaded MLVs and LUVs, which were prepared using the optimum formulations of our previous studies 13,14 , were given to rats with experimental pneumonia, and we evaluated the efficiency of the liposomal treatment. The characterization of the liposomes' shape and surface was evaluated using a transmission electron microscope (TEM).…”

“…Preparation and Purification of Liposomes: ENR loaded multilamellar vesicles (MLVs) and large unilamellar vesicles (LUVs) were prepared using a modified dry film method 13,14 . The F-and L-ENR were separated by gel filtration on a Sephadex G-50 column at 25°C (1.0 cm in diameter, a gel bed height of 20 cm, Sigma Chemical Co., USA), and PBS (pH 7.4) was used as the medium 15 .…”

“…The final liposomes were visualized under an electron microscope using a negative staining technique (JEOL, Tokyo, Japan) at 10.000x magnification 13 .…”

Herbal liposome for the topical delivery of ketoconazole for the effective treatment of seborrheic dermatitis

“…The in vitro drug release was carried out in triplicate for each preparation and expressed as Mean ± SD., and then the cumulative drug release (%CDR) was calculated and a plot of time versus %CDR was constructed and shown graphically. In vitro skin permeation studies were conducted for all liposome formulations and reported (Panigrahi et al 2006;Sezer et al 2004;Agarwal et al 2014).…”