Skip to main content
SpringerLink
Log in

Controlled release of huperzine-A from biocompatible copolymer microspheres

  • Published:
Bulletin of Materials Science Aims and scope Submit manuscript

Abstract

Huperzine-A (Hup-A) is a reversible acetylcholinesterase inhibitor used for patients suffering from Alzheimer’s disease. Hup-A has to be administered daily because of its short half-life time and narrow therapeutic range, making it less suitable for clinical use. In the present study, we studied its controlled drug delivery using biodegradable microspheres to avoid frequent dosing. Hup-A-loaded microspheres were prepared by an emulsion crosslinking method using a mixture of water and oil. Calcium chloride was used as a crosslinker. Primarily, we prepared sodium alginate (NaAlg) microspheres and investigated the in vitro release. The in vitro release studies were carried out successively at three different pH (1.2, 6.8 and 7.4) values for 2 h. To increase the durability of the NaAlg microspheres, NaAlg was blended with acrylamide (AAm)-grafted poly(vinyl alcohol) (PVA). It was determined that the presence of the PVA-g-AAm increased the physical resistance of the microspheres and also increased the amount of Hup-A loading and release. Additionally, the effect of the NaAlg/PVA-g-AAm (w/w) blend ratio, drug/polymer (w/w) ratio, crosslinker concentration and crosslinking period on the release of Hup-A was investigated. The prepared microspheres were characterized using Fourier transform infrared spectroscopy, differential scanning calorimetry and scanning electron microscopy.

This is a preview of subscription content, log in via an institution to check access.

Access this article

Log in via an institution

Price excludes VAT (USA)
Tax calculation will be finalised during checkout.

Instant access to the full article PDF.

Institutional subscriptions

Fig. 1
Fig. 2
Fig. 3
Fig. 4
Fig. 5
Fig. 6
Fig. 7

Similar content being viewed by others

References

  1. Cai X, Luan Y, Jiang Y, Song A, Shao W, Li Z et al 2012 Int. J. Pharm. 433 102

    Article  CAS  Google Scholar 

  2. Ma X, Tan C, Zhu D, Gang D R and Xiao P 2007 J. Ethnopharmacol. 113 15

    Article  CAS  Google Scholar 

  3. Zhang Z X, Wang X D, Chen Q T, Liang S, Zuo W J and Liang D G 2002 Natl. Med. J. China  14 941

    Google Scholar 

  4. Jiang Y B, Huang C S and Huang L A 2002 Clin. Med. China 18 802

    CAS  Google Scholar 

  5. Ye J C, Zeng S, Zheng G L and Chen G S 2008 Int. J Pharm. 356 187

    Article  CAS  Google Scholar 

  6. Wang C, Zhang T, Ma H, Liu J, Fu F and Liu K 2007 Basic Clin. Pharm. Toxicol. 100 190

    Article  CAS  Google Scholar 

  7. Gao P, Xu H, Ding P T, Gao Q, Sun J and Chen D 2007 Int. J. Pharm. 330 1

    Article  CAS  Google Scholar 

  8. Chu D F, Fu X Q, Liu W H, Liu K and Li Y X 2006 Int. J. Pharm. 325 116

    Article  CAS  Google Scholar 

  9. Kweon D K and Kang D W 1999 J. Appl. Polym. Sci. 74 458

    Article  CAS  Google Scholar 

  10. Adoor S G, Prathab B L, Manjeshwar S and Aminabhavi T M 2007 Polymer 48 5417

    Article  CAS  Google Scholar 

  11. Zhang J, Zhang L M and Li Z M 2000 J. Appl. Polym. Sci. 78 537

    Article  Google Scholar 

  12. Babu V R, Sairam M, Hosamani K M and Aminabhavi T M 2007 Carbohydr. Polym. 69 241

    Article  Google Scholar 

  13. Kulkarni R V, Baraskar V V, Alange V V, Naikawadi A A and Sa B 2013 J. Macromol. Sci., Part B, Phys. 52 1636

    Article  Google Scholar 

  14. Lu A, Salabas E L and Schuth F 2007 Angew. Chem. Int. Ed. Engl. 46 1222

    Article  CAS  Google Scholar 

  15. Loh J W, Saunders M and Lim L Y 2012 Toxicol. Appl. Pharmacol. 262 273

    Article  CAS  Google Scholar 

  16. Peng Z, Li Z and Shen Y 2012 J. Macromol. Sci., Part B, Phys. 51 1117

  17. Mody V V, Cox A, Shah S, Singh A, Beving W and Parihar H 2014 Appl. Nanosci. 4 385

    Article  CAS  Google Scholar 

  18. Zhou Z, Zhou J, Liu L, Yi Q, Liu Q, Zeng W and Yang Z 2012 J. Macromol. Sci., Part B, Phys. 51 777

    Article  Google Scholar 

  19. Loh J W, Yeoh G, Saunders M and Lim L Y 2010 Toxicol. Appl. Pharm. 249 148

    Article  CAS  Google Scholar 

  20. Saikia C, Hussain A, Ramteke A, Sharma H K and Maji T K 2014 Artif. Cells Nanomed. B 4 1

    Google Scholar 

  21. Trapani A, Sitterberg J, Bakowsky U and Kissel T 2009 Int. J. Pharm. 375 97

    Article  CAS  Google Scholar 

  22. Changez M, Koul V, Burugapalli K and Dinda A K 2004 Biomaterials 25 139

    Article  CAS  Google Scholar 

  23. Conti S, Maggi L, Segale L, Ochoa M E, Conte U, Grenier P and Vergnault G 2007 Int. J Pharm. 333 136

    Article  CAS  Google Scholar 

  24. Aminabhavi T M 2006 J. Appl. Polym. Sci. 99 2671

    Article  Google Scholar 

  25. Shang Y, Ding F, Xiao L, Deng H, Du Y and Shi X 2014 Carbohydr. Polym. 102 413

    Article  CAS  Google Scholar 

  26. Rassu G, Salis A, Porcu EP, Giunchedi P, Roldo M and Gavini E 2016 Carbohydr. Polym. 136 1338

    Article  CAS  Google Scholar 

  27. Noppakundilograt S, Piboon P, Graisuwan W, Nuisin R and Kiatkamjornwong S 2015 Carbohydr. Polym. 131 23

    Article  CAS  Google Scholar 

  28. Diaz-Rodriquez P and Landin M 2015 Int. J. Pharm. 480 92

    Article  Google Scholar 

  29. Kumbar S G and Aminabhavi T M 2002 J. Appl. Polym. Sci. 84 552

    Article  CAS  Google Scholar 

  30. Kim S J, Yoon S G and Kim S I 2004 J. Appl. Polym. Sci. 91 3705

    Article  CAS  Google Scholar 

  31. Srinivas Murthy B R, Ramanathan G and Tirichurapalli Sivagnanam U 2017 Bull. Mater. Sci. 40 645

    Article  Google Scholar 

  32. Pandima Devi M, Sekar M, Chamundeswari M, Moorthy A, Krithiga G, Selva Murugan N et al 2012 Bull. Mater. Sci. 35 1157

    Article  CAS  Google Scholar 

  33. Soppimath K S and Aminabhavi T M 2002 Eur. J. Pharm. Biopharm. 53 87

    Article  Google Scholar 

  34. Yuan Y, Chesnutt B M, Uttukar G, Haggard W O, Yang Y, Ong J L et al 2007 Carbohydr. Polym. 68 561

    Article  CAS  Google Scholar 

  35. Kurkuri M D and Aminabhavi T M 2004 J. Control. Release 96 9

    Article  CAS  Google Scholar 

  36. Bajpai J, Mishra S and Bajpai A K 2007 J. Appl. Polym. Sci. 106 961

    Article  CAS  Google Scholar 

  37. Şanlı O and Solak E K 2009 J. Appl. Polym. Sci. 112 2057

    Article  Google Scholar 

Download references

Acknowledgements

We are grateful to the Gazi University Scientific Research Foundation (41-2009/07) for support to this study.

Author information

Authors and Affiliations

  1. Technical Sciences Vocational School, Department of Chemistry and Chemical Engineering Technologies, Ostim, Gazi University, Ankara, 06374, Turkey

    Ebru Kondolot Solak

  2. Faculty of Science, Department of Chemistry, Gazi University, 06500, Teknikokullar, Ankara, Turkey

    Gülsen Asman

  3. Technical Sciences Vocational School, Department of Material and Material Processing Technologies, Gazi University, Ankara, 06374, Turkey

    Sinan Mithat Muhammet

Authors
  1. Ebru Kondolot Solak
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Gülsen Asman
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Sinan Mithat Muhammet
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Ebru Kondolot Solak.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Solak, E.K., Asman, G. & Muhammet, S.M. Controlled release of huperzine-A from biocompatible copolymer microspheres. Bull Mater Sci 42, 55 (2019). https://doi.org/10.1007/s12034-019-1759-7

Download citation

  • Received:

  • Accepted:

  • Published:

  • DOI: https://doi.org/10.1007/s12034-019-1759-7

Keywords

Search

Navigation