Docetaxel in cationic lipid nanocapsules for enhanced in vivo activity

The usefulness of Docetaxel (DT) as an anti-cancer agent is limited to parenteral route owing to its very poor oral bioavailability. Thus, to improve its oral efficacy, DT was loaded in novel cationic lipid nanocapsules (DT CLNC). The DT CLNC possessed size of 130-150 nm, zeta potential of +72mV, ad...

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Published inPharmaceutical development and technology Vol. 21; no. 1; p. 76
Main Authors Jain, Ankitkumar S, Makhija, Dinesh T, Goel, Peeyush N, Shah, Sanket M, Nikam, Yuvraj, Gude, Rajiv P, Jagtap, Aarti G, Nagarsenker, Mangal S
Format Journal Article
LanguageEnglish
Published England 02.01.2016
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Abstract The usefulness of Docetaxel (DT) as an anti-cancer agent is limited to parenteral route owing to its very poor oral bioavailability. Thus, to improve its oral efficacy, DT was loaded in novel cationic lipid nanocapsules (DT CLNC). The DT CLNC possessed size of 130-150 nm, zeta potential of +72mV, adequate DT loading and over 95% encapsulation efficiency. TEM revealed capsular structure of DT CLNC. Lipolysis study indicated improved solubilization of DT by nanocapsules in comparison to DT solution. DT CLNC exhibited significantly higher release of DT in comparison to DT solution during in vitro permeation studies employing non-reverted rat-intestinal sac. Superior uptake of DT in zebra fishes exposed to DT CLNC resulted in greater apoptosis-based cell death as compared to those exposed to DT solution. This correlated well with the significantly superior (p < 0.05) anti-angiogenic activity of DT CLNC system over DT solution, in zebra fish model. DT CLNC also inhibited tumor growth in melanoma cell line induced tumors in C57BL/6 mice significantly, as compared to DT solution (p < 0.05). The DT CLNC system demonstrated adequate stability, with tremendous potential to improve oral efficacy of DT and can serve as an alternative to existing DT formulations available commercially for parenteral use.
AbstractList The usefulness of Docetaxel (DT) as an anti-cancer agent is limited to parenteral route owing to its very poor oral bioavailability. Thus, to improve its oral efficacy, DT was loaded in novel cationic lipid nanocapsules (DT CLNC). The DT CLNC possessed size of 130-150 nm, zeta potential of +72mV, adequate DT loading and over 95% encapsulation efficiency. TEM revealed capsular structure of DT CLNC. Lipolysis study indicated improved solubilization of DT by nanocapsules in comparison to DT solution. DT CLNC exhibited significantly higher release of DT in comparison to DT solution during in vitro permeation studies employing non-reverted rat-intestinal sac. Superior uptake of DT in zebra fishes exposed to DT CLNC resulted in greater apoptosis-based cell death as compared to those exposed to DT solution. This correlated well with the significantly superior (p < 0.05) anti-angiogenic activity of DT CLNC system over DT solution, in zebra fish model. DT CLNC also inhibited tumor growth in melanoma cell line induced tumors in C57BL/6 mice significantly, as compared to DT solution (p < 0.05). The DT CLNC system demonstrated adequate stability, with tremendous potential to improve oral efficacy of DT and can serve as an alternative to existing DT formulations available commercially for parenteral use.
Author Jain, Ankitkumar S
Jagtap, Aarti G
Goel, Peeyush N
Shah, Sanket M
Nikam, Yuvraj
Makhija, Dinesh T
Gude, Rajiv P
Nagarsenker, Mangal S
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  surname: Nagarsenker
  fullname: Nagarsenker, Mangal S
  organization: a Department of Pharmaceutics
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CitedBy_id crossref_primary_10_3390_genes8120349
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crossref_primary_10_1208_s12249_016_0522_2
crossref_primary_10_1080_10837450_2016_1212879
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Keywords zebra fish
non-everted rat-intestinal sac
cationic nanocapsule
Anti-tumor
docetaxel
Language English
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Snippet The usefulness of Docetaxel (DT) as an anti-cancer agent is limited to parenteral route owing to its very poor oral bioavailability. Thus, to improve its oral...
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StartPage 76
SubjectTerms Animals
Cations
Female
Lipids - administration & dosage
Lipids - chemistry
Lipids - pharmacokinetics
Melanoma, Experimental - drug therapy
Melanoma, Experimental - metabolism
Mice
Mice, Inbred C57BL
Nanocapsules - administration & dosage
Nanocapsules - chemistry
Particle Size
Rats
Taxoids - administration & dosage
Taxoids - chemistry
Taxoids - pharmacokinetics
Zebrafish
Title Docetaxel in cationic lipid nanocapsules for enhanced in vivo activity
URI https://www.ncbi.nlm.nih.gov/pubmed/25329444
Volume 21
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