期刊
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
卷 11, 期 1, 页码 118-130出版社
SPRINGER HEIDELBERG
DOI: 10.1007/s13346-020-00712-9
关键词
Amphotericin B; Nanoparticles; Leishmania donovani; Visceral leishmaniasis
资金
- Indian Council of Medical Research (ICMR), New Delhi
- CSIR, New Delhi [IA27607]
- Council of Scientific and Industrial Research Network Project, HOPE [BSC0114]
A nanoformulation of AmB and Pip was developed, with controlled release properties and protection from acidic pH, showing enhanced drug bioavailability, non-nephrotoxic nature, and potential antileishmanial activity up to 96% inhibition of the parasite in vivo in the golden hamster-L. donovani model.
Amphotericin B (AmB) exhibits potential antileishmanial activity, with only a little rate of recurrence. However, low bioavailability and severe nephrotoxicity are among the major shortcomings of AmB-based therapy. Various AmB nanoformulations have been developed, which to an extent, have reduced its toxicity and increased the drug efficacy. To further reduce the nonspecific tissue distribution and the cost of the treatment, the current AmB-based formulations require additional improvements. Combination of natural bioenhancers with AmB is expected to further increase its bioavailability. Therefore, we developed a nanoformulation of AmB and piperine (Pip), a plant alkaloid, known to enhance the bioavailability of various drugs, by entrapping them in guar gum, a macrophage targeting polymer. Owing to the ease of oral delivery, these nanoparticles (NPs) were coated with eudragit to make them suitable for oral administration. The formulated eudragit-coated AmB and Pip-loaded NPs (Eu-HDGG-AmB-Pip-NPs) exhibited controlled release of the loaded therapeutic agents and protected the drug from acidic pH. These NPs exhibited effective suppression of growth of both promastigotes and amastigotes of Leishmania donovani parasite under in vitro. In vivo evaluation of these NPs for therapeutic efficacy in golden hamster-L. donovani model demonstrated enhanced drug bioavailability, non-nephrotoxic nature, and potential antileishmanial activity with up to 96% inhibition of the parasite. Graphical abstract
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