Development and Performance Evaluation of Amphotericin B Transfersomes Against Resistant and Sensitive Clinical Isolates of Visceral Leishmaniasis

Singodia, Deepak; Gupta, Gaurav; Verma, Ayushi; Singh, Vishram; Shukla, P.K.; Misra, Pragya; Sundar, Sham; Dube, Anuradha; Mishra, Prabhat Ranjan

doi:10.1166/jbn.2010.1121

Cited by 24 publications

(23 citation statements)

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“…Liposomes in the proper formulation and size, pass through stratum corneum of the intact skin and reach the dermis where Leishmania parasite normally lodge and multiply. In previous studies using sub-micron size liposomes as vehicles for paromomycin and AmB, the formulations showed to be effective against some Leishmania species (Ahsan et al, 2002; Devi et al, 2011; El Maghraby et al, 2008; Huang et al, 2009; Manosroi et al, 2004; Mauël, 1990; Singodia et al, 2010).…”

Section: Introductionmentioning

confidence: 99%

Development of a topical liposomal formulation of Amphotericin B for the treatment of cutaneous leishmaniasis

Jaafari

Hatamipour

Alavizadeh

et al. 2019

International Journal for Parasitology: Drugs and Drug Resistan

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BackgroundCurrently, there is no topical treatment available for any form of cutaneous leishmaniasis (CL) in most of the endemic areas. The aim of the current study was to develop a topical nano-liposomal Amphotericin B (AmB) for the treatment of CL.Methodology/principal findingsLiposomes containing 0.1, 0.2 and 0.4% AmB (Lip-AmB) were formulated and characterized for the size, entrapment efficiency, long term stability, and skin penetration properties using Franz diffusion cells. Liposomes diameters were around 100 nm with no change during more than 20 months’ storage either at 4 °C or at room temperature. Franz diffusion cells studies showed that almost 4% of the applied formulations penetrated across the skin and the highest skin retention (73.92%) observed with Lip-AmB 0.4%. The median effective doses (ED50), the doses of AmB required to kill 50% of L. major amastigotes were 0.151, 0.151, and 0.0856 (μg/mL) in Lip-AmB 0.1, 0.2, 0.4%, respectively. Lip-AmB 0.4% caused 80% reduction in fluorescence intensity of GFP+ L. tropica infected macrophages at 5 μg/mL of AmB concentration. Topical Lip-AmB was applied twice a day for 4 weeks to the skin of BALB/c mice to treat lesions caused by L. major. Results showed the superiority of Lip-AmB 0.4% compared to Lip-AmB 0.2 and 0.1%. The parasite was completely cleared from the skin site of infection and spleens at week 8 and 12 post-infection in mice treated with Lip-AmB 0.4%. The results suggest that topical Lip-AmB 0.4% may be a useful tool in the treatment of CL and merits further investigation.

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Section: Introductionmentioning

confidence: 99%

Development of a topical liposomal formulation of Amphotericin B for the treatment of cutaneous leishmaniasis

Jaafari

Hatamipour

Alavizadeh

et al. 2019

International Journal for Parasitology: Drugs and Drug Resistan

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“…8,9 Surface-active agents can be inserted into the lipid bilayers of flexible liposomes and create a "softened" bilayer membrane, thus making liposomes more flexible and permeable than ordinary liposomes. [10][11][12] The highly deformable membranes of flexible liposomes facilitate their rapid distribution into the skin. Further, the osmotic gradient created by the difference in water concentration between the surface and interior of the skin has been identified as the major driving force for penetration of flexible liposomes into the skin.…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy

Li¹,

Zhang²,

Huang³

et al. 2013

IJN

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Abstract:The purpose of this study was to investigate flexible nanoliposomes for mediating topical delivery of daptomycin, and to document permeation rates and bacteriostatic activity towards skin infections. Response surface methodology was used to optimize the daptomycinloaded flexible nanoliposomes (DAP-FL), and the amount of drug loaded into the particles was evaluated as the investigation index. The optimal lipid ratio was lecithin to sodium cholate 17:1 (w/w) and the lipid to drug ratio was 14:1 (w/w). The hydration temperature was set at 37°C and the duration of treatment with ultrasound was 20 minutes. The DAP-FL obtained had a small mean particle size (55.4 nm) with a narrow size distribution (polydispersity index 0.15). The mean entrapment efficiency was 87.85% ± 2.15% and the mean percent drug loading was 5.61% ± 0.14%. Using skin mounted between the donor and receptor compartments of a modified Franz diffusion cell, the percentage and quantity of cumulative daptomycin permeation from DAP-FL within 12 hours were measured at 96.28% ± 0.70% and (132.23 ± 17.73) μg/cm 2 *5 = 661.15 ± 88.65 μg/cm 2 , directly, showing rapid and efficient antibacterial activity against Staphylococcus aureus. Following local administration of DAP-FL, daptomycin was detected in multilayer tissues within the skin and underlying structures in the dorsal skin of the mouse. Effective therapeutic concentrations were maintained for several hours, and significantly inhibited bacterial growth and injury-induced biofilms. These results demonstrate that the DAP-FL can enhance the ability of daptomycin to permeate the skin efficiently, where it has a powerful antibacterial action and activity against biofilms. This novel formulation of daptomycin has potential as a new approach in the clinical application of daptomycin.

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“…The multilamellar lipid vesicles (MLV) are then sonicated at room temperature to get small vesicles [Table 1]. [161826]…”

Section: Methods Of Preparationmentioning

confidence: 99%

Transferosomes - A vesicular transdermal delivery system for enhanced drug permeation

Rajan¹,

Jose²,

Mukund³

et al. 2011

J Adv Pharm Technol Res

177

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Transdermal administration of drugs is generally limited by the barrier function of the skin. Vesicular systems are one of the most controversial methods for transdermal delivery of active substances. The interest in designing transdermal delivery systems was relaunched after the discovery of elastic vesicles like transferosomes, ethosomes, cubosomes, phytosomes, etc. This paper presents the composition, mechanisms of penetration, manufacturing and characterization methods of transferosomes as transdermal delivery systems of active substances. For a drug to be absorbed and distributed into organs and tissues and eliminated from the body, it must pass through one or more biological membranes/barriers at various locations. Such a movement of drug across the membrane is called as drug transport. For the drugs to be delivered to the body, they should cross the membranous barrier. The concept of these delivery systems was designed in an attempt to concentrate the drug in the tissues of interest, while reducing the amount of drug in the remaining tissues. Hence, surrounding tissues are not affected by the drug. In addition, loss of drug does not happen due to localization of drug, leading to get maximum efficacy of the medication. Therefore, the phospholipid based carrier systems are of considerable interest in this era.

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Development and Performance Evaluation of Amphotericin B Transfersomes Against Resistant and Sensitive Clinical Isolates of Visceral Leishmaniasis

Cited by 24 publications

References 0 publications

Development of a topical liposomal formulation of Amphotericin B for the treatment of cutaneous leishmaniasis

Development of a topical liposomal formulation of Amphotericin B for the treatment of cutaneous leishmaniasis

Preparation and characterization of flexible nanoliposomes loaded with daptomycin, a novel antibiotic, for topical skin therapy

Transferosomes - A vesicular transdermal delivery system for enhanced drug permeation

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