Efficient Entrapment of Amikacin and Teicoplanin in Liposomes

Ravaoarinoro, M.; Toma, Emil; Agbaba, O.; Morisset, R

doi:10.3109/10611869308996076

Cited by 10 publications

(5 citation statements)

References 20 publications

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“…The final pellet was resuspended in 6 ml of distilled water and assayed for drug activity and content. In all experiments, the size and homogeneity of the liposomal suspensions were determined by negative-stain electron microscopy, as reported previously [5], and were found to be uniform (50-100 nm) and reproducible for all formulations tested. Amikacin, netilmicin and tobramycin in lipo somes were measured by the enzyme multiplied im munoassay technique (Syva, Palo Alto, Calif., USA), after disrupting the lipid membranes with 0.2% (v/v) of Triton X-100.…”

Section: Preparation O F Liposomesmentioning

confidence: 69%

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Comparison of the Bactericidal Action of Amikacin, Netilmicin and Tobramycin in Free and Liposomal Formulation against <i>Pseudomonas aeruginosa</i>

Omri¹,

Ravaoarinoro²

1996

Chemotherapy

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The rates at which free, cationic and anionic liposomal forms of amikacin, netilmicin and tobramycin kill Pseudomonas aeruginosa were studied in vitro. Control inocula with no antibiotic yielded 6.76, 9.53 and 9.74 log CFU/ml at 0, 6 and 24 h, respectively. Empty anionic or cationic liposomes had no effect on bacterial growth. The killing rates of free antibiotics against the bacterial strain were not enhanced by the addition of either empty anionic or cationic liposomes. After 6 and 24 h of exposure at 1, 2 and 4 times the minimum inhibitory concentrations, free amikacin, netilmicin and tobramycin demonstrated a more rapid bactericidal effect than encapsulated anionic or cationic liposomes. The killing rates of liposomal aminoglycosides were lower than those of free aminoglycosides at identical concentrations, suggesting that only fractions of the encapsulated drugs were released from liposomes.

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Section: Preparation O F Liposomesmentioning

confidence: 69%

“…Liposomes were prepared as described previously [5]. Briefly, two lipid compositions were employed: egg lecithin, stearylamine and cholesterol (cationic lipo somes), and egg lecithin, dicetyl phosphate and choles terol (anionic liposomes).…”

Section: Preparation O F Liposomesmentioning

confidence: 99%

Comparison of the Bactericidal Action of Amikacin, Netilmicin and Tobramycin in Free and Liposomal Formulation against <i>Pseudomonas aeruginosa</i>

Omri¹,

Ravaoarinoro²

1996

Chemotherapy

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“…Liposomes were prepared as previously described by Ravaoarinoro et al 13 Briefly, three liposomal compositions were formulated: lecithin (egg phosphatidyl chloine), stearylamine and cholesterol (cationic liposomes); lecithin, La-phosphatidyl-DL-glycerol and cholesterol (anionic liposomes); and lecithin and cholesterol (neutral liposomes). The molar ratio was 7:2:1, respectively, for charged liposomes, whereas it was 7:1 for neutral preparations.…”

Section: Preparation Of Liposomesmentioning

confidence: 99%

Treatment of experimental osteomyelitis by liposomal antibiotics

Kadry¹,

Al‐Suwayeh²,

Abd-Allah³

et al. 2004

Journal of Antimicrobial Chemotherapy

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Liposomes sonicated for 40 s gave the highest antibacterial activities in vitro. Since cationic liposomes trapped the highest percentage of antibiotics, and enhanced antibacterial activity above that of the free drugs, they were used for therapeutic trials to treat chronic staphylococcal osteomyelitis induced in rabbits. Therapeutic trials with antibiotics given intravenously revealed that, free ciprofloxacin or vancomycin given alone for 14 days was ineffective in sterilizing bone. Combination therapy with free ciprofloxacin and vancomycin for 14 days was more effective. However, this group showed renal dysfunction and severe diarrhoea, which resulted in loss of 33.3% of treated animals. Treatment with liposomal forms of either drug for 7 days was ineffective. Meanwhile, combination therapy in liposomal form for 7 days was more effective. Complete sterilization of bone tissues on cultures (100% cure) was obtained only in the group treated for 14 days with the combination of both drugs in liposomal form. Moreover, liposomal formulations showed much lower nephrotoxicity and a lower incidence of severe diarrhoea than that induced by free drugs.

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“…Multiple reports of antibiotic encapsulation in liposomes have been published using various lipids. − A review of the literature on liposomal encapsulation of antibiotics, however, can cause confusion and, in some cases, even shows inconsistencies. A clear example of one of these inconsistencies is the encapsulation of the antistaphylococcal antibiotic rifampin.…”

Section: Introductionmentioning

confidence: 99%

Liposomal Nanovesicles for Efficient Encapsulation of Staphylococcal Antibiotics

et al. 2019

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Liposomes are attractive vehicles for localized delivery of antibiotics. There exists, however, a gap in knowledge when it comes to achieving high liposomal loading efficiencies for antibiotics. To address this issue, we investigated three antibiotics of clinical relevance against staphylococcal infections with different hydrophilicity and chemical structure, namely, vancomycin hydrochloride, teicoplanin, and rifampin. We categorized the suitability of different encapsulation techniques on the basis of encapsulation efficiency, lipid requirement (important for avoiding lipid toxicity), and mass yield (percentage of mass retained during the preparation process). The moderately hydrophobic (teicoplanin) and highly hydrophobic (rifampin) antibiotics varied significantly in their encapsulation load (max 23.4 and 15.5%, respectively) and mass yield (max 74.1 and 71.8%, respectively), favoring techniques that maximized partition between the aqueous core and the lipid bilayer or those that produce oligolamellar vesicles, whereas vancomycin hydrochloride, a highly hydrophilic molecule, showed little preference to any of the protocols. In addition, we report significant bias introduced by the choice of analytical method adopted to quantify the encapsulation efficiency (underestimation of up to 24% or overestimation by up to 57.9% for vancomycin and underestimation of up to 61.1% for rifampin) and further propose ultrafiltration and bursting by methanol as the method with minimal bias for quantification of encapsulation efficiency in liposomes. The knowledge generated in this work provides critical insight into the more practical, albeit less investigated, aspects of designing vesicles for localized antibiotic delivery and can be extended to other nanovehicles that may suffer from the same biases in analytical protocols.

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Efficient Entrapment of Amikacin and Teicoplanin in Liposomes

Cited by 10 publications

References 20 publications

Comparison of the Bactericidal Action of Amikacin, Netilmicin and Tobramycin in Free and Liposomal Formulation against <i>Pseudomonas aeruginosa</i>

Comparison of the Bactericidal Action of Amikacin, Netilmicin and Tobramycin in Free and Liposomal Formulation against <i>Pseudomonas aeruginosa</i>

Treatment of experimental osteomyelitis by liposomal antibiotics

Liposomal Nanovesicles for Efficient Encapsulation of Staphylococcal Antibiotics

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