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. 2011 May;19(4):239-50.
doi: 10.3109/1061186X.2010.492524. Epub 2010 Jun 14.

Drug targeting to macrophages using paromomycin-loaded albumin microspheres for treatment of visceral leishmaniasis: an in vitro evaluation

Wahid Khan  1 , Neeraj Kumar
Affiliations

Drug targeting to macrophages using paromomycin-loaded albumin microspheres for treatment of visceral leishmaniasis: an in vitro evaluation

Wahid Khan et al. J Drug Target. 2011 May.

Abstract

Background: Leishmania parasite is an obligate intracellular parasite of the mammalian host and lives inside resident macrophages of liver and spleen. A high dose of paromomycin (PM) is required for the treatment.

Purpose: Preparation and in vitro evaluation of PM loaded albumin microspheres (MS) (of size ≤ 5 µm) to target macrophages for treatment of visceral leishmaniasis.

Methods: PM loaded MS were prepared by spray-drying method using albumin as a polymer matrix and stabilized using heat treatment. These MS were evaluated for product yield, encapsulation efficiency, particle size, size distribution, contact angle, drug-polymer interactions, and for in vitro drug release. Fluorescent labeling and in vitro uptake of these MS was assessed in RAW 264.7 cell line.

Results: PM loaded albumin MS were prepared with a mean particle size ≈3 µm. Free albumin content and contact angle study confirmed the stabilization of these MS. Release studies showed biphasic release pattern. Interaction studies ruled out any possibility of drug-polymer interaction. Uptake study in macrophage confirmed the suitability of prepared MS for macrophage targeting.

Conclusion: The proposed drug-delivery system was found suitable for targeting macrophages in vitro and may serve as an optimum carrier to target macrophages where Leishmania parasite resides.

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