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Paromomycin-loaded albumin microspheres: efficacy and stability studies
Wahid Khan1, Rajendra Kumar, Sukhvinder Singh
1National Institute of Pharmaceutical Education & Research (NIPER), Nagar, India.
Abstract:
In the present work, paromomycin-loaded albumin microspheres (PM-MS) have been formulated for passive targeting of paromomycin (PM) to macrophages, for the treatment of visceral leishmaniasis (VL). PM-MS were prepared by spray-drying method with a mean particle size of ≈ 3 µm. Thermal and chemical cross-linking methods were used for controlling drug release from the prepared microspheres (MS). PM-MS were then tested for efficacy and stability studies. In efficacy study, in vitro promastigote assay was carried out to assess the susceptibility of promastigote to PM in the concentration range of 5.0-150 µg/ml; cytotoxicity assay was performed to determine possible toxicity of PM for the host cells (peritoneal macrophages) and intracellular amastigote assay was carried out to determine the efficacy of free PM (PM solution) and encapsulated PM (PM-MS). Results obtained indicated a significant increase in efficacy of PM-MS in comparison to PM solution at equivalent concentration. Subsequently, stability studies of prepared formulation was carried out at various temperature and humidity conditions, these studies provided stability of formulation at all tested conditions including accelerated conditions. Thus, it can be concluded that present work provides an optimized formulation with stability and enhanced efficacy.
Insights
Paromomycin-loaded albumin microspheres effectively target macrophages for visceral leishmaniasis treatment. This optimized formulation demonstrates enhanced efficacy and stability compared to free paromomycin.
Area of Science:
- Nanotechnology in Drug Delivery
- Parasitology and Tropical Diseases
- Pharmaceutical Sciences
Background:
- Visceral leishmaniasis (VL) remains a significant global health challenge requiring effective drug delivery systems.
- Passive targeting of anti-leishmanial drugs to macrophages can improve therapeutic outcomes.
- Albumin microspheres offer a promising platform for encapsulating and delivering therapeutic agents.
Purpose of the Study:
- To formulate paromomycin-loaded albumin microspheres (PM-MS) for enhanced passive targeting to macrophages.
- To evaluate the efficacy and stability of the developed PM-MS formulation for visceral leishmaniasis treatment.
Main Methods:
- Paromomycin-loaded albumin microspheres (PM-MS) were prepared using a spray-drying technique.
- Drug release was controlled using thermal and chemical cross-linking methods.
- In vitro assays included promastigote susceptibility, cytotoxicity, and intracellular amastigote efficacy studies.
Main Results:
- PM-MS exhibited a mean particle size of approximately 3 µm, suitable for passive targeting.
- The encapsulated paromomycin (PM) in microspheres showed significantly enhanced efficacy compared to free PM solution.
- Stability studies confirmed the formulation's robustness under various temperature and humidity conditions, including accelerated testing.
Conclusions:
- The developed paromomycin-loaded albumin microspheres represent an optimized formulation for visceral leishmaniasis treatment.
- The formulation demonstrates improved therapeutic efficacy and excellent stability, suggesting its potential for clinical application.
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