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[In vitro study of leishmanicidal agents with drug carriers]
1Laboratoire de Parasitologie, Faculté de Médecine, Paris XII, Créteil.
Annales De Parasitologie Humaine Et Comparee
|January 1, 1993
Summary
Targeting pentamidine with nanoparticles significantly enhances its antileishmanial activity against Leishmania major parasites within macrophages. This novel drug delivery system proved 25 times more effective than the free drug in vitro.
Area of Science:
- Parasitology
- Nanotechnology
- Drug Delivery
Context:
- Leishmaniasis chemotherapy faces challenges due to parasite sequestration within host cell lysosomes.
- Limited bioavailability of antileishmanial drugs hinders effective treatment.
- Macrophages serve as reservoirs for Leishmania parasites.
Purpose:
- To evaluate the antileishmanial efficacy of pentamidine delivered via methacrylate polymer nanoparticles.
- To assess the effectiveness of polyisoalkylcyanoacrylate nanospheres against Leishmania major.
- To compare the activity of targeted versus free pentamidine in an in vitro model.
Summary:
- Pentamidine-loaded methacrylate polymer nanoparticles demonstrated a 25-fold increase in antileishmanial activity compared to free pentamidine.
- The 50% effective concentration (EC50) for targeted pentamidine was 0.10 µg/ml, versus 2.7 µg/ml for the free drug.
- Unloaded polyisoalkylcyanoacrylate nanospheres showed activity against intracellular amastigotes but approached cytotoxic levels.
Impact:
- Nanoparticle-mediated drug delivery offers a promising strategy to overcome bioavailability issues in antileishmanial chemotherapy.
- Targeted delivery enhances drug potency, potentially reducing required dosages and side effects.
- This approach could lead to more effective treatments for leishmaniasis by improving drug targeting to infected macrophages.