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Pharmaceutical Research

, Volume 32, Issue 3, pp 1002–1016 | Cite as

Liposome Encapsulated Albumin-Paclitaxel Nanoparticle for Enhanced Antitumor Efficacy

  • Hima Bindu Ruttala
  • Young Tag Ko
Research Paper

ABSTRACT

Purpose

Albumin nanoparticles have been explored as a promising delivery system for various therapeutic agents. One limitation of such formulations is their poor colloidal stability in vivo. Present study aimed at enhancing the chemotherapeutic potential of paclitaxel by improving the colloidal stability and pharmacokinetic properties of albumin-paclitaxel nanoparticles (APNs) such as Abraxane®.

Methods

This was accomplished by encapsulating the preformed APNs into PEGylated liposomal bilayer by thin-film hydration/extrusion technique.

Results

The resulting liposome-encapsulated albumin-paclitaxel hybrid nanoparticles (L-APNs) were nanosized (~200 nm) with uniform spherical dimensions. The successful incorporation of albumin-paclitaxel nanoparticle (NP) in liposome was confirmed by size exclusion chromatography analysis. Such hybrid NP showed an excellent colloidal stability even at 100-fold dilutions, overcoming the critical drawback associated with simple albumin-paclitaxel NP system. L-APNs further showed higher cytotoxic activity towards B16F10 and MCF-7 cells than APN; this effect was characterized by arrest at the G2/M phase and a higher prevalence of apoptotic subG1 cells. Finally, pharmacokinetic and biodistribution studies in tumor mice demonstrated that L-APNs showed a significantly enhanced plasma half-life, and preferential accumulation in the tumor.

Conclusions

Taken together, the data indicate that L-APNs can be promising therapeutic vehicles for enhanced delivery of PTX to tumor sites.

KEY WORDS

albumin nanoparticle colloidal stability liposome paclitaxel pharmacokinetic 

Abbreviations

APNs

Albumin-paclitaxel nanoparticles

CLSM

Confocal laser scanning microscopy

DLS

Dynamic light scattering

DSC

Differential scanning calorimetry

FACS

Fluorescence Activated Cell Sorting (Flow Cytometry)

HPLC

High performance liquid chromatography

L-APNs

Liposome-encapsulated albumin-paclitaxel hybrid nanoparticles

LC-MS/MS

Liquid chromatography-tandem mass spectrometry

NP

Nanoparticle

PTX

Paclitaxel

XRD

X-ray diffraction

Notes

ACKNOWLEDGMENTS AND DISCLOSURES

This research was supported by the Basic Science Research Program of Korean National Research Foundation (NRF-20110007794).

Supplementary material

11095_2014_1512_MOESM1_ESM.docx (595 kb)
ESM 1 (DOCX 594 kb)

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Copyright information

© Springer Science+Business Media New York 2014

Authors and Affiliations

  1. 1.College of PharmacyGachon UniversityIncheonRepublic of Korea

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