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Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell.

Abstract Topical drug delivery against cutaneous leishmaniasis (CL) signifies an effective alternate for improving the availability and reducing the toxicity associated with the parenteral administration of conventional sodium stibogluconate (SSG) injection. The basic aim of the study was to develop... Full description

Journal Title: Drug delivery November 2018, Vol.25(1), pp.1595-1606
Main Author: Dar, M Junaid
Other Authors: Din, Fakhar Ud , Khan, Gul Majid
Format: Electronic Article Electronic Article
Language: English
Subjects:
ID: E-ISSN: 1521-0464 ; DOI: 10.1080/10717544.2018.1494222
Link: http://search.proquest.com/docview/2088294159/?pq-origsite=primo
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title: Sodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell.
format: Article
creator:
  • Dar, M Junaid
  • Din, Fakhar Ud
  • Khan, Gul Majid
subjects:
  • Administration, Topical–Administration & Dosage
  • Animals–Metabolism
  • Antimony Sodium Gluconate–Administration & Dosage
  • Antiprotozoal Agents–Metabolism
  • Dose-Response Relationship, Drug–Methods
  • Drug Delivery Systems–Drug Therapy
  • Female–Metabolism
  • Leishmaniasis–Drug Effects
  • Liposomes–Metabolism
  • Macrophages–Administration & Dosage
  • Mice–Metabolism
  • Mice, Inbred Balb C–Drug Effects
  • Nanoparticles–Physiology
  • Organ Culture Techniques–Physiology
  • Rats–Physiology
  • Skin Absorption–Physiology
  • Treatment Outcome–Physiology
  • Antiprotozoal Agents
  • Liposomes
  • Antimony Sodium Gluconate
  • Cutaneous Leishmaniasis
  • Macrophage Uptake
  • Nano-Deformable Liposomes
  • Sodium Stibogluconate
  • Transfersomes
ispartof: Drug delivery, November 2018, Vol.25(1), pp.1595-1606
description: Abstract Topical drug delivery against cutaneous leishmaniasis (CL) signifies an effective alternate for improving the availability and reducing the toxicity associated with the parenteral administration of conventional sodium stibogluconate (SSG) injection. The basic aim of the study was to develop nano-deformable liposomes (NDLs) for the dermal delivery of SSG against CL. NDLs were formulated by a modified thin film hydration method and optimized via Box–Behnken statistical design. The physicochemical properties of SSG-NDLs were established in terms of vesicle size (195.1 nm), polydispersity index (0.158), zeta potential (−32.8 mV), and entrapment efficiency (35.26%). Moreover, deformability index, in vitro release, and macrophage uptake studies were also accomplished. SSG-NDLs were entrapped within Carbopol gel network for the ease of skin application. The ex vivo skin permeation study revealed that SSG-NDLs gel provided 10-fold higher skin retention towards the deeper skin layers, attained without use of classical permeation enhancers. Moreover, in vivo skin irritation and histopathological studies verified safety of the topically applied formulation. Interestingly, the cytotoxic potential of SSG-NDLs (1.3 mg/ml) was higher than plain SSG (1.65 mg/ml). The anti-leishmanial activity on intramacrophage amastigote model of Leishmania tropica showed that IC 50 value of the SSG-NDLs was ∼ fourfold lower than the plain drug solution with marked increase in the selectivity index. The in vivo results displayed higher anti-leishmanial activity by efficiently healing lesion and successfully reducing parasite burden. Concisely, the outcomes indicated that the targeted delivery of SSG could be accomplished by using topically applied NDLs for the effective treatment of CL.
language: eng
source:
identifier: E-ISSN: 1521-0464 ; DOI: 10.1080/10717544.2018.1494222
fulltext: fulltext
issn:
  • 15210464
  • 1521-0464
url: Link


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titleSodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell.
creatorDar, M Junaid ; Din, Fakhar Ud ; Khan, Gul Majid
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ispartofDrug delivery, November 2018, Vol.25(1), pp.1595-1606
identifierE-ISSN: 1521-0464 ; DOI: 10.1080/10717544.2018.1494222
subjectAdministration, Topical–Administration & Dosage ; Animals–Metabolism ; Antimony Sodium Gluconate–Administration & Dosage ; Antiprotozoal Agents–Metabolism ; Dose-Response Relationship, Drug–Methods ; Drug Delivery Systems–Drug Therapy ; Female–Metabolism ; Leishmaniasis–Drug Effects ; Liposomes–Metabolism ; Macrophages–Administration & Dosage ; Mice–Metabolism ; Mice, Inbred Balb C–Drug Effects ; Nanoparticles–Physiology ; Organ Culture Techniques–Physiology ; Rats–Physiology ; Skin Absorption–Physiology ; Treatment Outcome–Physiology ; Antiprotozoal Agents ; Liposomes ; Antimony Sodium Gluconate ; Cutaneous Leishmaniasis ; Macrophage Uptake ; Nano-Deformable Liposomes ; Sodium Stibogluconate ; Transfersomes
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descriptionAbstract Topical drug delivery against cutaneous leishmaniasis (CL) signifies an effective alternate for improving the availability and reducing the toxicity associated with the parenteral administration of conventional sodium stibogluconate (SSG) injection. The basic aim of the study was to develop nano-deformable liposomes (NDLs) for the dermal delivery of SSG against CL. NDLs were formulated by a modified thin film hydration method and optimized via Box–Behnken statistical design. The physicochemical properties of SSG-NDLs were established in terms of vesicle size (195.1 nm), polydispersity index (0.158), zeta potential (−32.8 mV), and entrapment efficiency (35.26%). Moreover, deformability index, in vitro release, and macrophage uptake studies were also accomplished. SSG-NDLs were entrapped within Carbopol gel network for the ease of skin application. The ex vivo skin permeation study revealed that SSG-NDLs gel provided 10-fold higher skin retention towards the deeper skin layers, attained without use of classical permeation enhancers. Moreover, in vivo skin irritation and histopathological studies verified safety of the topically applied formulation. Interestingly, the cytotoxic potential of SSG-NDLs (1.3 mg/ml) was higher than plain SSG (1.65 mg/ml). The anti-leishmanial activity on intramacrophage amastigote model of Leishmania tropica showed that IC 50 value of the SSG-NDLs was ∼ fourfold lower than the plain drug solution with marked increase in the selectivity index. The in vivo results displayed higher anti-leishmanial activity by efficiently healing lesion and successfully reducing parasite burden. Concisely, the outcomes indicated that the targeted delivery of SSG could be accomplished by using topically applied NDLs for the effective treatment of CL.
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titleSodium stibogluconate loaded nano-deformable liposomes for topical treatment of leishmaniasis: macrophage as a target cell.
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