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Pharmaceutical Research

, Volume 33, Issue 7, pp 1682–1695 | Cite as

A Comparative Study of Orally Delivered PBCA and ApoE Coupled BSA Nanoparticles for Brain Targeting of Sumatriptan Succinate in Therapeutic Management of Migraine

  • Priti Girotra
  • Shailendra Kumar Singh
Research Paper

ABSTRACT

Purpose

The present investigation aimed at brain targeting of sumatriptan succinate (SS) for its optimal therapeutic effect in migraine through nanoparticulate drug delivery system using poly (butyl cyanoacrylate) (PBCA) and bovine serum albumin linked with apolipoprotein E3 (BSA-ApoE).

Method

The study involved formulation optimization of PBCA nanoparticles (NPs) using central composite design for achieving minimum particle size, maximum entrapment efficiency along with sustained drug release. SS incorporated in BSA-ApoE NPs (S-AA-NP) were prepared by desolvation technique and compared with SS loaded polysorbate 80 coated optimized PBCA NPs (FPopt) in terms of their brain uptake potential, upon oral administration in male Wistar rats. The NPs were characterized by FTIR, thermal, powder XRD and TEM analysis.

Results

The in vivo studies of FPopt and S-AA-NP on male Wistar rats demonstrated a fairly high brain/plasma drug ratio of 9.45 and 12.67 respectively 2 h post oral drug administration. The behavioural studies on male Swiss albino mice affirmed the enhanced anti-migraine potential of S-AA-NP than FPopt (P < 0.001).

Conclusion

The results of this work, therefore, indicate that BSA-ApoE NPs are significantly better than polysorbate 80 coated PBCA NPs for brain targeting of SS (P < 0.05) and also offer an improved therapeutic strategy for migraine management.

KEY WORDS

apolipoprotein brain targeting BSA PBCA sumatriptan succinate 

ABBREVIATIONS

AA-NP

Dummy Apolipoprotein E coupled bovine serum albumin nanoparticles (without drug)

ApoE

Apolipoprotein E

BBB

Blood Brain Barrier

BSA

Bovine Serum Albumin

BSA-ApoE

Bovine Serum Albumin covalently linked with Apolipoprotein E

DSC

Differential Scanning Calorimetry

FCopt

Sumatriptan succinate loaded polysorbate 80 coated chitosan solid lipid nanoparticles

FPopt

Sumatriptan succinate loaded polysorbate 80 coated optimized Poly (butyl cyanoacrylate) nanoparticles

FTIR

Fourier-Transform Infrared Spectroscopy

HPLC

High-Performance Liquid Chromatography

mmol

Millimoles

nBCA

n-Butyl-2-cyanoacrylate

NPs

Nanoparticles

PBCA

Poly (butyl cyanoacrylate) (PBCA)

pXRD

Powder X-Ray Diffraction

S-AA-NP

Sumatriptan succinate loaded apolipoprotein E coupled BSA nanoparticles

SLN

Solid lipid nanoparticles

SS

Sumatriptan Succinate

TEM

Transmission Electron Microscopy

TGA

Thermogravimetric analysis

Notes

ACKNOWLEDGMENTS AND DISCLOSURES

The authors acknowledge the Coordinator, DST FIST, Department of Pharmaceutical Sciences (GJU S&T, Hisar) and SAIF, Panjab University (Chandigarh) for providing particle size analysis and TEM analysis facility respectively. The authors are thankful to Department of Science & Technology, New Delhi for providing DST-INSPIRE fellowship as financial assistance. The contribution of Dr. Tikva Vogel in providing the gift sample of ApoE is gratefully acknowledged. The authors also wish to thank Dr. A.K. Mohanty, (Animal Biotechnology Centre, National Dairy Research Institute, Karnal, India) for kindly helping in the thiolation of apolipoprotein E. The authors report no conflict of interest and are solely responsible for the content and writing of the paper.

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Copyright information

© Springer Science+Business Media New York 2016

Authors and Affiliations

  1. 1.Department of Pharmaceutical SciencesG. J. University of Sci. & Tech.HisarIndia

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