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Lipid drug conjugate nanoparticle as a novel lipid nanocarrier for the oral delivery of decitabine: ex vivo gut permeation studies

The purpose of this study was to develop lipid drug conjugate (LDC) nanoparticles of decitabine (DCB) using stearic acid as a lipid to increase the permeability of the drug along with its protection from chemical degradation. The LDC was prepared by salt formation of DCB with stearic acid and follow... Full description

Journal Title: Nanotechnology 2013-10-18, Vol.24 (41), p.415102-415102
Main Author: Neupane, Yub Raj
Other Authors: Sabir, M D , Ahmad, Nafees , Ali, Mushir , Kohli, Kanchan
Format: Electronic Article Electronic Article
Language: English
Subjects:
Quelle: Alma/SFX Local Collection
Publisher: Bristol: IOP Publishing
ID: ISSN: 0957-4484
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recordid: cdi_pascalfrancis_primary_27812453
title: Lipid drug conjugate nanoparticle as a novel lipid nanocarrier for the oral delivery of decitabine: ex vivo gut permeation studies
format: Article
creator:
  • Neupane, Yub Raj
  • Sabir, M D
  • Ahmad, Nafees
  • Ali, Mushir
  • Kohli, Kanchan
subjects:
  • Antimetabolites, Antineoplastic - administration & dosage
  • Azacitidine - administration & dosage
  • Azacitidine - analogs & derivatives
  • Biological and medical sciences
  • Biotechnology
  • Condensed matter: structure, mechanical and thermal properties
  • Cross-disciplinary physics: materials science
  • rheology
  • Drug Carriers - chemistry
  • Drugs
  • Exact sciences and technology
  • Fundamental and applied biological sciences. Psychology
  • Kinetics
  • Low-dimensional structures (superlattices, quantum well structures, multilayers): structure, and nonelectronic properties
  • Materials science
  • Methods. Procedures. Technologies
  • Nanocrystalline materials
  • Nanoparticles - chemistry
  • Nanoparticles - ultrastructure
  • Nanoscale materials and structures: fabrication and characterization
  • Nanoscale materials: clusters, nanoparticles, nanotubes, and nanocrystals
  • Others
  • Permeability
  • Physics
  • Stearic Acids - chemistry
  • Structure of solids and liquids
  • crystallography
  • Surface-Active Agents - chemistry
  • Surfaces and interfaces
  • thin films and whiskers (structure and nonelectronic properties)
  • Various methods and equipments
ispartof: Nanotechnology, 2013-10-18, Vol.24 (41), p.415102-415102
description: The purpose of this study was to develop lipid drug conjugate (LDC) nanoparticles of decitabine (DCB) using stearic acid as a lipid to increase the permeability of the drug along with its protection from chemical degradation. The LDC was prepared by salt formation of DCB with stearic acid and followed by cold homogenization technique to produce the LDC nanoparticles. The role of key independent variables influencing on dependent variables were determined by using a Box-Behnken design. The optimized batch revealed spherical morphology under TEM analysis with particle size of 202.6 ± 1.65 nm and 0.334 ± 0.987 PDI. The zeta potential and %EE were found to be −33.6 ± 0.845 mV and 68.89% ± 0.59 respectively. Lyophilized powder showed the crystalline structure under DSC analysis. In vitro release studies showed the initial burst release followed by a sustained release up to 24 h in PBS pH 7.4 and the data were further studied using release kinetic models which revealed the first-order model as a best-fitting model. Ex vivo gut permeation studies proved that the formulation containing lipid and surfactants has a higher permeability than the plain drug solution with nearly fourfold increase in the apparent permeability coefficients. Finally, LDC nanoparticles prepared by using stearic acid as a lipid and surfactants as Tween 80, Poloxamer 188, and Labrasol in equal ratio possess high potential for the oral delivery of hydrophilic drugs.
language: eng
source: Alma/SFX Local Collection
identifier: ISSN: 0957-4484
fulltext: fulltext
issn:
  • 0957-4484
  • 1361-6528
url: Link


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titleLipid drug conjugate nanoparticle as a novel lipid nanocarrier for the oral delivery of decitabine: ex vivo gut permeation studies
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creatorNeupane, Yub Raj ; Sabir, M D ; Ahmad, Nafees ; Ali, Mushir ; Kohli, Kanchan
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descriptionThe purpose of this study was to develop lipid drug conjugate (LDC) nanoparticles of decitabine (DCB) using stearic acid as a lipid to increase the permeability of the drug along with its protection from chemical degradation. The LDC was prepared by salt formation of DCB with stearic acid and followed by cold homogenization technique to produce the LDC nanoparticles. The role of key independent variables influencing on dependent variables were determined by using a Box-Behnken design. The optimized batch revealed spherical morphology under TEM analysis with particle size of 202.6 ± 1.65 nm and 0.334 ± 0.987 PDI. The zeta potential and %EE were found to be −33.6 ± 0.845 mV and 68.89% ± 0.59 respectively. Lyophilized powder showed the crystalline structure under DSC analysis. In vitro release studies showed the initial burst release followed by a sustained release up to 24 h in PBS pH 7.4 and the data were further studied using release kinetic models which revealed the first-order model as a best-fitting model. Ex vivo gut permeation studies proved that the formulation containing lipid and surfactants has a higher permeability than the plain drug solution with nearly fourfold increase in the apparent permeability coefficients. Finally, LDC nanoparticles prepared by using stearic acid as a lipid and surfactants as Tween 80, Poloxamer 188, and Labrasol in equal ratio possess high potential for the oral delivery of hydrophilic drugs.
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languageeng
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subjectAntimetabolites, Antineoplastic - administration & dosage ; Azacitidine - administration & dosage ; Azacitidine - analogs & derivatives ; Biological and medical sciences ; Biotechnology ; Condensed matter: structure, mechanical and thermal properties ; Cross-disciplinary physics: materials science; rheology ; Drug Carriers - chemistry ; Drugs ; Exact sciences and technology ; Fundamental and applied biological sciences. Psychology ; Kinetics ; Low-dimensional structures (superlattices, quantum well structures, multilayers): structure, and nonelectronic properties ; Materials science ; Methods. Procedures. Technologies ; Nanocrystalline materials ; Nanoparticles - chemistry ; Nanoparticles - ultrastructure ; Nanoscale materials and structures: fabrication and characterization ; Nanoscale materials: clusters, nanoparticles, nanotubes, and nanocrystals ; Others ; Permeability ; Physics ; Stearic Acids - chemistry ; Structure of solids and liquids; crystallography ; Surface-Active Agents - chemistry ; Surfaces and interfaces; thin films and whiskers (structure and nonelectronic properties) ; Various methods and equipments
ispartofNanotechnology, 2013-10-18, Vol.24 (41), p.415102-415102
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descriptionThe purpose of this study was to develop lipid drug conjugate (LDC) nanoparticles of decitabine (DCB) using stearic acid as a lipid to increase the permeability of the drug along with its protection from chemical degradation. The LDC was prepared by salt formation of DCB with stearic acid and followed by cold homogenization technique to produce the LDC nanoparticles. The role of key independent variables influencing on dependent variables were determined by using a Box-Behnken design. The optimized batch revealed spherical morphology under TEM analysis with particle size of 202.6 ± 1.65 nm and 0.334 ± 0.987 PDI. The zeta potential and %EE were found to be −33.6 ± 0.845 mV and 68.89% ± 0.59 respectively. Lyophilized powder showed the crystalline structure under DSC analysis. In vitro release studies showed the initial burst release followed by a sustained release up to 24 h in PBS pH 7.4 and the data were further studied using release kinetic models which revealed the first-order model as a best-fitting model. Ex vivo gut permeation studies proved that the formulation containing lipid and surfactants has a higher permeability than the plain drug solution with nearly fourfold increase in the apparent permeability coefficients. Finally, LDC nanoparticles prepared by using stearic acid as a lipid and surfactants as Tween 80, Poloxamer 188, and Labrasol in equal ratio possess high potential for the oral delivery of hydrophilic drugs.
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0Antimetabolites, Antineoplastic - administration & dosage
1Azacitidine - administration & dosage
2Azacitidine - analogs & derivatives
3Biological and medical sciences
4Biotechnology
5Condensed matter: structure, mechanical and thermal properties
6Cross-disciplinary physics: materials science; rheology
7Drug Carriers - chemistry
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9Exact sciences and technology
10Fundamental and applied biological sciences. Psychology
11Kinetics
12Low-dimensional structures (superlattices, quantum well structures, multilayers): structure, and nonelectronic properties
13Materials science
14Methods. Procedures. Technologies
15Nanocrystalline materials
16Nanoparticles - chemistry
17Nanoparticles - ultrastructure
18Nanoscale materials and structures: fabrication and characterization
19Nanoscale materials: clusters, nanoparticles, nanotubes, and nanocrystals
20Others
21Permeability
22Physics
23Stearic Acids - chemistry
24Structure of solids and liquids; crystallography
25Surface-Active Agents - chemistry
26Surfaces and interfaces; thin films and whiskers (structure and nonelectronic properties)
27Various methods and equipments
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24Structure of solids and liquids; crystallography
25Surface-Active Agents - chemistry
26Surfaces and interfaces; thin films and whiskers (structure and nonelectronic properties)
27Various methods and equipments
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abstractThe purpose of this study was to develop lipid drug conjugate (LDC) nanoparticles of decitabine (DCB) using stearic acid as a lipid to increase the permeability of the drug along with its protection from chemical degradation. The LDC was prepared by salt formation of DCB with stearic acid and followed by cold homogenization technique to produce the LDC nanoparticles. The role of key independent variables influencing on dependent variables were determined by using a Box-Behnken design. The optimized batch revealed spherical morphology under TEM analysis with particle size of 202.6 ± 1.65 nm and 0.334 ± 0.987 PDI. The zeta potential and %EE were found to be −33.6 ± 0.845 mV and 68.89% ± 0.59 respectively. Lyophilized powder showed the crystalline structure under DSC analysis. In vitro release studies showed the initial burst release followed by a sustained release up to 24 h in PBS pH 7.4 and the data were further studied using release kinetic models which revealed the first-order model as a best-fitting model. Ex vivo gut permeation studies proved that the formulation containing lipid and surfactants has a higher permeability than the plain drug solution with nearly fourfold increase in the apparent permeability coefficients. Finally, LDC nanoparticles prepared by using stearic acid as a lipid and surfactants as Tween 80, Poloxamer 188, and Labrasol in equal ratio possess high potential for the oral delivery of hydrophilic drugs.
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