The Parenteral Controlled Release of Liposome Encapsulated Chloroquine in Mice

Titulaer, H. A. C.; Eling, W. M. C.; Crommelin, Daan J.A.; Peeters, Pierre; Zuidema, J.

doi:10.1111/j.2042-7158.1990.tb07052.x

Cited by 24 publications

(4 citation statements)

References 9 publications

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“…1). The results of similar studies performed in different species (Titulaer et al, 1990; Cabanes et al, 1992, 1995; Valladares et al, 1997; Fielding et al, 1999) are in agreement with the findings of this paper. After i.m.…”

Section: Discussionsupporting

confidence: 93%

Comparative Pharmacokinetics of Enrofloxacin and Tissue Concentrations of Parent Drug and Ciprofloxacin after Intramuscular Administrations of Free and Liposome‐Encapsulated Enrofloxacin in Rabbits

Elmas

Yazar

Baş

et al. 2002

Journal of Veterinary Medicine, Series B

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Pharmacokinetic properties and tissue concentrations of enrofloxacin and ciprofloxacin were compared after intramuscular (i.m.) administrations of free and liposome-encapsulated enrofloxacin at the dose of 5 mg/kg body weight (bw). Twelve healthy adult New Zealand white rabbits were used in the experiment. Blood samples were obtained at 10, 20, 40, 60 and 90 min and 2, 4, 6, 8 and 12 h and tissue samples were collected 24 h after injection. Concentrations of drugs in serum were determined by high-performance liquid chromatography. Pharmacokinetics were best described by a two-compartment open model. Results indicated that absorption rate was slow, peak concentration was higher (P < 0.05), and the time to peak concentration (tmax congruent with 1.5 h) was significantly longer (P < 0.05) for liposome-encapsulated enrofloxacin (LEE) when compared with free enrofloxacin. Values of elimination half-life (t1/2beta = 12.9 h) and mean residence time (MRT = 17.6 h) of liposome-encapsulated enrofloxacin were longer (P < 0.05) and total clearance (Cl = 0.43 l/h/kg) was lower than those of free form. Moreover, the distribution volume at steady-state (Vd(ss) = 14.4 l/kg) of enrofloxacin administered encapsulated into liposomes was significantly higher (P < 0.05) than that of free enrofloxacin (FE). The tissue levels of enrofloxacin and ciprofloxacin after LEE injection were not different (P > 0.05) from FE. In conclusion, the result of present study suggest that LEE may be a beneficial and valuable formulation in the treatment of infectious diseases caused by sensitive pathogens in animals, providing sustained drug release from injection side and prolonged therapeutic serum concentrations after i.m. administration.

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Section: Discussionsupporting

confidence: 93%

Comparative Pharmacokinetics of Enrofloxacin and Tissue Concentrations of Parent Drug and Ciprofloxacin after Intramuscular Administrations of Free and Liposome‐Encapsulated Enrofloxacin in Rabbits

Elmas

Yazar

Baş

et al. 2002

Journal of Veterinary Medicine, Series B

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“…Clearly, the spectrum of viruses for which this class of compounds would be useful in vivo will be strongly determined by this factor, as well as by the potency of the compound itself in inhibiting specific steps in viral replication. Improvements in formulation, such as encapsulation within liposomes may also be of utility in modifying the pharmacokinetics of CQ in vivo [36]–[39].…”

Section: Resultsmentioning

confidence: 99%

A Systematic Screen of FDA-Approved Drugs for Inhibitors of Biological Threat Agents

et al. 2013

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BackgroundThe rapid development of effective medical countermeasures against potential biological threat agents is vital. Repurposing existing drugs that may have unanticipated activities as potential countermeasures is one way to meet this important goal, since currently approved drugs already have well-established safety and pharmacokinetic profiles in patients, as well as manufacturing and distribution networks. Therefore, approved drugs could rapidly be made available for a new indication in an emergency.Methodology/Principal FindingsA large systematic effort to determine whether existing drugs can be used against high containment bacterial and viral pathogens is described. We assembled and screened 1012 FDA-approved drugs for off-label broad-spectrum efficacy against Bacillus anthracis; Francisella tularensis; Coxiella burnetii; and Ebola, Marburg, and Lassa fever viruses using in vitro cell culture assays. We found a variety of hits against two or more of these biological threat pathogens, which were validated in secondary assays. As expected, antibiotic compounds were highly active against bacterial agents, but we did not identify any non-antibiotic compounds with broad-spectrum antibacterial activity. Lomefloxacin and erythromycin were found to be the most potent compounds in vivo protecting mice against Bacillus anthracis challenge. While multiple virus-specific inhibitors were identified, the most noteworthy antiviral compound identified was chloroquine, which disrupted entry and replication of two or more viruses in vitro and protected mice against Ebola virus challenge in vivo.Conclusions/SignificanceThe feasibility of repurposing existing drugs to face novel threats is demonstrated and this represents the first effort to apply this approach to high containment bacteria and viruses.

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“…The latter was found to contain a higher chloroquine concentration, indicating a sustained release by the liposome. Although the liposomes acted as “depots” for chloroquine and no toxic effects were found for all the injected liposome encapsulated chloroquine, the intraperitoneal route of administration had the highest blood chloroquine concentration and the muscle depot released faster than the subcutaneous fat layer [ 148 ].…”

Section: Nanodrug Delivery Systemsmentioning

confidence: 99%

Current advances in nanodrug delivery systems for malaria prevention and treatment

Kekani

Witika

2023

Discover Nano

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Malaria is a life-threatening, blood-borne disease with over two hundred million cases throughout the world and is more prevalent in Sub-Saharan Africa than anywhere else in the world. Over the years, several treatment agents have been developed for malaria; however, most of these active pharmaceutical ingredients exhibit poor aqueous solubility and low bioavailability and may result in drug-resistant parasites, thus increasing malaria cases and eventually, deaths. Factors such as these in therapeutics have led to a better appreciation of nanomaterials. The ability of nanomaterials to function as drug carriers with a high loading capacity and targeted drug delivery, good biocompatibility, and low toxicity renders them an appealing alternative to conventional therapy. Nanomaterials such as dendrimers and liposomes have been demonstrated to be capable of enhancing the efficacy of antimalarial drugs. This review discusses the recent development of nanomaterials and their benefits in drug delivery for the potential treatment of malaria.

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The Parenteral Controlled Release of Liposome Encapsulated Chloroquine in Mice

Cited by 24 publications

References 9 publications

Comparative Pharmacokinetics of Enrofloxacin and Tissue Concentrations of Parent Drug and Ciprofloxacin after Intramuscular Administrations of Free and Liposome‐Encapsulated Enrofloxacin in Rabbits

Comparative Pharmacokinetics of Enrofloxacin and Tissue Concentrations of Parent Drug and Ciprofloxacin after Intramuscular Administrations of Free and Liposome‐Encapsulated Enrofloxacin in Rabbits

A Systematic Screen of FDA-Approved Drugs for Inhibitors of Biological Threat Agents

Current advances in nanodrug delivery systems for malaria prevention and treatment

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