Miltefosine and BODIPY-labeled alkylphosphocholine with leishmanicidal activity: Aggregation properties and interaction with model membranes

Nanocarriers Provide Sustained Antifungal Activity for Amphotericin B and Miltefosine in the Topical Treatment of Murine Vaginal Candidiasis

“…One possibility is the difference in the drug release profile. However, we were not able to compare drug release from the formulations due to methodological difficulties; both drugs AMB and MFS aggregate in waterbased solvents, hindering drug transport across semi-permeable membranes (employed to separate the nanocarrier from the bulk release medium), and underestimating release (Barioni et al, 2015). Further studies for method adaptation are necessary to address this issue.…”

In Vitro Activities of Miltefosine and Antibacterial Agents from the Macrolide, Oxazolidinone, and Pleuromutilin Classes against Pythium insidiosum and Pythium aphanidermatum

“…The mechanism of action of miltefosine against microorganisms is not fully understood. In vitro models demonstrated that miltefosine could cause fluidization and loss of integrity of vesicles and aggregates with lipids, in dose-dependent concentrations (43). Several mechanisms of action described for miltefosine against Leishmania spp.…”

“…may be related to increased cellular permeability. Avis and Belanger (49) reported that Pythium aphanidermatum and Phytophthora infestans were the microorganisms that were most sensitive to cis-9-heptadecenoic acid, an antifungal fatty acid that has surfactant activity similar to that of miltefosine (43). This antimicrobial activity was related to the low proportion (or absence) of ergosterol in the membrane, since sterols are known to buffer stress-induced modifications in membrane fluidity (50), protecting the microorganism from the toxic effects of fatty acids.…”

Biophysical Characterization of cubosomal nanoparticles intended for drug delivery applications and its interaction with a model drug: the miltefosine case

“…MILT while a very interesting molecule for medicine, it presents high gastrointestinal toxicity and high hemolytic potential, limiting its applications and administered dose (DA GAMA BITENCOURT et al, 2016). MILT is also a very hydrophobic molecule, its critical micellar concentration (CMC) is approximately ~ 50µM (BARIONI et al, 2015) and LogP 6.7 (from Pubchem). Hence, it is important to study this molecule interaction with nanoparticles in order to make its use more efficient, preventing side effects while enhancing the drug efficiency.…”

“…It also presents a strong antineoplastic effect(MUNOZ et al, 2013) and potency against leishmanial activity(RÍOS- MARCO et al, 2017). Since its approval, by the FDA in 1992, MILT has been used for oral treatment of visceral and cutaneous leishmaniosis in a maximum single dose of 20 mg/kg(EISSA et al, 2015) in the following countries: India, Germany, Colombia and United States(BARIONI et al, 2015). For cancer treatment, it has only been approved for topical treatment in breast skin cancer metastases cancer and cutaneous lymphoma (ALONSO; ALONSO, 2016).…”