Abstract
Amphotericin B (Amb) is a broad-spectrum polyene macrolide antibiotic which has been a drug of choice for fatal conditions like fungal splenic abscess. Hence a drug delivery system with splenotropic potencial might be of great significance for further therapeutic effectiveness. Present manuscript proposes development of Irregular shaped polymer lipid hybrid nanostructures (LIPOMER) of Amb with enhanced splenic uptake. Amb LIPOMER (~400 nm) was prepared using poly(methylvinylether-co-maleic anhydride) [Gantrez® AN119] and glyceryl monosterarate (GMS) as matrix material. Conditions for preparation of formulation were optimized using 23 factorial design and effect of the concentration of excipients on the particle size and entrapment efficiency was evaluated. Optimized formulation was further characterized using Transmission electron microscopy (TEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transformed infrared spectroscopy (FTIR) techniques. Amb LIPOMER exhibited acceptable haemolysis when assessed for In-vitro hemolytic potential in comparison to Fungisome TM. The high splenic uptake of Amb LIPOMER was verified using gamma scintigraphic technique in small animal model. Results of our study indicated that LIPOMER system can be a smart drug delivery platform for Amb to eradicate splenic infections effectively.
Keywords: Amphotericin B, enhanced splenic uptake, LIPOMER, nano-system, scintigraphy, splenic abscess.
Drug Delivery Letters
Title:Amphotericin B LIPOMER for Enhanced Splenic Delivery
Volume: 4 Issue: 3
Author(s): Kalpa S. Nagarsekar, Chandrakant N. Galdhar, Rajiv V. Gaikwad, Abdul Samad and Padma V. Devarajan
Affiliation:
Keywords: Amphotericin B, enhanced splenic uptake, LIPOMER, nano-system, scintigraphy, splenic abscess.
Abstract: Amphotericin B (Amb) is a broad-spectrum polyene macrolide antibiotic which has been a drug of choice for fatal conditions like fungal splenic abscess. Hence a drug delivery system with splenotropic potencial might be of great significance for further therapeutic effectiveness. Present manuscript proposes development of Irregular shaped polymer lipid hybrid nanostructures (LIPOMER) of Amb with enhanced splenic uptake. Amb LIPOMER (~400 nm) was prepared using poly(methylvinylether-co-maleic anhydride) [Gantrez® AN119] and glyceryl monosterarate (GMS) as matrix material. Conditions for preparation of formulation were optimized using 23 factorial design and effect of the concentration of excipients on the particle size and entrapment efficiency was evaluated. Optimized formulation was further characterized using Transmission electron microscopy (TEM), X-ray diffraction (XRD), differential scanning calorimetry (DSC) and Fourier transformed infrared spectroscopy (FTIR) techniques. Amb LIPOMER exhibited acceptable haemolysis when assessed for In-vitro hemolytic potential in comparison to Fungisome TM. The high splenic uptake of Amb LIPOMER was verified using gamma scintigraphic technique in small animal model. Results of our study indicated that LIPOMER system can be a smart drug delivery platform for Amb to eradicate splenic infections effectively.
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Cite this article as:
Nagarsekar Kalpa S., N. Galdhar Chandrakant, V. Gaikwad Rajiv, Samad Abdul and V. Devarajan Padma, Amphotericin B LIPOMER for Enhanced Splenic Delivery, Drug Delivery Letters 2014; 4 (3) . https://dx.doi.org/10.2174/2210303104666140807232823
DOI https://dx.doi.org/10.2174/2210303104666140807232823 |
Print ISSN 2210-3031 |
Publisher Name Bentham Science Publisher |
Online ISSN 2210-304X |
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