Amphotericin B (AmB) is an effective drug to treat visceral leishmaniasis but its use is limited by its poor oral bioavailability. This article describes the in-vivo evaluation of AmB-loaded, lipid-based cochleate systems designed for the oral route. Two different cochleate formulations were studied: one based on the synthetic phospholipid dioleoylphosphatidylserine (DOPS) and another optimized formulation based on a naturally occurring phosphatidylserine (Lipoid PSP70) that would render the formulation more affordable in developing countries.
View Article and Find Full Text PDFThere is a need for new, cost-effective drugs to treat leishmaniasis. A strategy based on traditional medicine practiced in Bolivia led to the discovery of the 2-substituted quinoline series as a source of molecules with antileishmanial activity and low toxicity. This review documents the development of the series from the first isolated natural compounds through several hundred synthetized molecules to an optimized compound exhibiting an in vitro IC value of 0.
View Article and Find Full Text PDFTreatment of acute myeloid leukaemia (AML) relies on decades-old drugs, and while recent years have seen some breakthroughs, AML is still characterised by poor prognosis and survival rate. Drug repurposing can expedite the preclinical development of new therapies, and by nanocarrier encapsulation, the number of potentially viable drug candidates can be further expanded. The anti-psychotic drug chlorpromazine (CPZ) has been identified as a candidate for repurposing for AML therapy.
View Article and Find Full Text PDFCochleate systems formed from phospholipids have very useful properties as drug delivery systems with sustained release capabilities, which are able to improve bioavailability and efficacy, reduce toxicity and increase the shelf-life of encapsulated molecules. These nanometric or micrometric structures are usually obtained after interaction of negatively charged liposomes with a positively charged bridging agent. Many different methods are now available to prepare cochleates and there are also numerous techniques that can be used to characterize them, some of which can be easily applied while others require more sophisticated equipment or analysis.
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