Novel methods for the encapsulation of meglumine antimoniate into liposomes

Frézard, Frédéric; Michalick, Marilene Suzan Marques; Soares, Camille Flores; Demicheli, Cynthia

doi:10.1590/s0100-879x2000000700016

Cited by 44 publications

(25 citation statements)

References 13 publications

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“…Meglumine antimoniate was encapsulated in freeze-dried liposomes as previously described (4,5). Briefly, small unilamellar vesicles were prepared in water from L-α-distearoylphosphatidylcholine, cholesterol and dicetylphosphate (molar ratio of 5:4:1) at a final lipid concentration of 55 g/L.…”

Section: Da Schettini Et Almentioning

confidence: 99%

Pharmacokinetic and parasitological evaluation of the bone marrow of dogs with visceral leishmaniasis submitted to multiple dose treatment with liposome-encapsulated meglumine antimoniate

Schettini

Val

Souza

et al. 2005

Braz J Med Biol Res

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The aim of the present study was to evaluate the impact of a multiple dose regimen of a liposomal formulation of meglumine antimoniate (LMA) on the pharmacokinetics of antimony in the bone marrow of dogs with visceral leishmaniasis and on the ability of LMA to eliminate parasites from this tissue. Dogs naturally infected with Leishmania chagasi received 4 intravenous doses of either LMA (6.5 mg antimony/kg body weight, N = 9), or empty liposomes (at the same lipid dose as LMA, N = 9) at 4-day intervals. A third group of animals was untreated (N = 8). Before each administration and at different times after treatment, bone marrow was obtained and analyzed for antimony level (LMA group) by electrothermal atomic absorption spectrometry, and for the presence of Leishmania parasites (all groups). There was a significant increase of antimony concentration from 0.76 µg/kg wet organ (4 days after the first dose) to 2.07 µg/kg (4 days after the fourth dose) and a half-life of 4 days for antimony elimination from the bone marrow. Treatment with LMA significantly reduced the number of dogs positive for parasites (with at least one amastigote per 1000 host cells) compared to controls (positive dogs 30 days after treatment: 0 of 9 in the LMA group, 3 of 9 in the group treated with empty liposomes and 3 of 8 in the untreated group). However, complete elimination of parasites was not achieved. In conclusion, the present study showed that multiple dose treatment with LMA was effective in improving antimony levels in the bone marrow of dogs with visceral leishmaniasis and in reducing the number of positive animals, even though it was not sufficient to achieve complete elimination of parasites.

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Section: Da Schettini Et Almentioning

confidence: 99%

Pharmacokinetic and parasitological evaluation of the bone marrow of dogs with visceral leishmaniasis submitted to multiple dose treatment with liposome-encapsulated meglumine antimoniate

Schettini

Val

Souza

et al. 2005

Braz J Med Biol Res

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“…For drug encapsulation the lipid film was dispersed in 20 mM phosphate-buffered saline (PBS; pH 7.0) containing 1 mg of SAG (Gluconate Health Limited, Calcutta, India)/ml and sonicated for 30 s in an ultrasonicator. To remove free drug, liposomes with entrapped SAG were washed in PBS with centrifugation (10,000 ϫ g, 30 min, 4°C) (15). Approximately 300 to 400 g of SAG was associated with 22 mg of lipid, estimated as described previously (2,17).…”

mentioning

confidence: 99%

Combination Therapy Using Sodium Antimony Gluconate in Stearylamine-Bearing Liposomes against Established and Chronic Leishmania donovani Infection in BALB/c Mice

Pal

Ravindran

Ali

2004

Antimicrob Agents Chemother

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“…In contrast, free meglumine antimoniate was inefficient when administered at a comparable dose of antimony. 88) …”

Section: Current Applications Of Liposomesmentioning

confidence: 99%

Liposomal Delivery Systems: Design Optimization and Current Applications

Lila

Ishida

2017

Biological & Pharmaceutical Bulletin

268

124

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The liposome, a closed phospholipid bilayered vesicular system, has received considerable attention as a pharmaceutical carrier of great potential over the past 30 years. The ability of liposomes to encapsulate both hydrophilic and hydrophobic drugs, coupled with their biocompatibility and biodegradability, make liposomes attractive vehicles in the field of drug delivery. In addition, great technical advances such as remote drug loading, triggered release liposomes, ligand-targeted liposomes, liposomes containing combinations of drugs, and so on, have led to the widespread use of liposomes in diverse areas as delivery vehicles for anticancer, bio-active molecules, diagnostics, and therapeutic agents. In this review, we summarize design optimization of liposomal systems and invaluable applications of liposomes as effective delivery systems.

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Novel methods for the encapsulation of meglumine antimoniate into liposomes

Cited by 44 publications

References 13 publications

Pharmacokinetic and parasitological evaluation of the bone marrow of dogs with visceral leishmaniasis submitted to multiple dose treatment with liposome-encapsulated meglumine antimoniate

Pharmacokinetic and parasitological evaluation of the bone marrow of dogs with visceral leishmaniasis submitted to multiple dose treatment with liposome-encapsulated meglumine antimoniate

Combination Therapy Using Sodium Antimony Gluconate in Stearylamine-Bearing Liposomes against Established and Chronic Leishmania donovani Infection in BALB/c Mice

Liposomal Delivery Systems: Design Optimization and Current Applications

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