Skip to main content
Log in

PLGA encapsulation effect on Bioquin-HMPAO: radiolabeling and in vitro behaviour on brain and lung cancer cells

  • Published:
Journal of Radioanalytical and Nuclear Chemistry Aims and scope Submit manuscript

Abstract

Bioquin-HMPAO (BH) was previously investigated as a novel brain imaging agent by in vivo biodistribution studies. Present studies are carried out to explore radiolabeling and in vitro behaviour evaluation of poly (lactic-co-glycolic acid) (PLGA) encapsulated BH nanocapsules (BH-PLGA NCs). BH-PLGA NCs were characterized utilizing dynamic light scattering and scanning electron microscope. Encapsulation effect on radiolabeling with 99mTc was examined by stability and lipophilicity studies and effect on in vitro behaviour of 99mTc-BH was evaluated by incorporation studies on DAOY, U87-MG and A549 cells. It is observed that PLGA encapsulation has a positive and reinforcement effect.

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

Access this article

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

Similar content being viewed by others

References

  1. Yurt Kilcar A, Biber Muftuler FZ, Enginar H, Tekin V, Medine EI, Unak P (2014) Synthesis, characterization and biodistribution of 99mTc-Bioquin-HMPAO (99mTc-BH) as a novel brain imaging agent. J Radioanal Nucl Chem 302:563–573

    Article  CAS  Google Scholar 

  2. Kulkarni PV, Roney CA, Antich PP, Bonte FJ, Raghu AV (2010) Quinoline-n-butylcyanoacrylate-based nanoparticles for brain targeting for the diagnosis of Alzheimer’ s disease. WIREs Nanomed Nanobiotechnol 2:35–47

    Article  CAS  Google Scholar 

  3. Duncan R (2003) The dawning era of polymer therapeutics. Nat Rev Drug Discov 2:347–360

    Article  CAS  Google Scholar 

  4. Roney C, Kulkarni P, Arora V, Antich P, Bonte F, Wu A (2005) Targeted nanoparticles for drug delivery through the blood-brain barrier for Alzheimer’s disease. J Control Release 108:193–214

    Article  CAS  Google Scholar 

  5. Gutman RL, Peacock G, Lu DR (2000) Targeted drug delivery for brain cancer treatment. J Control Release 65:31–41

    Article  CAS  Google Scholar 

  6. Roney CA, Arora V, Kulkarni PV, Antich PP, Bonte FJ (2009) Nanoparticulate radiolabelled quinolines detect amyloid plaques in mouse models of Alzheimer’s disease. Int J Alzheimers Dis 2009:1–8

    Article  Google Scholar 

  7. Alexis F, Pridgen E, Molnar LK, Farokhzad OC (2008) Factors affecting the clearance and biodistribution of polymeric nanoparticles. Mol Pharm 5:505–515

    Article  CAS  Google Scholar 

  8. Locatelli E, Comes Franchini M (2012) Biodegradable PLGA-b-PEG polymeric nanoparticles: synthesis, properties, and nanomedical applications as drug delivery system. J Nanoparticle Res 14(1316):1–17

    Google Scholar 

  9. Kreuter J (1996) Nanoparticles and microparticles for drug and vaccine delivery. J Anat 189:503–505

    CAS  Google Scholar 

  10. Acharya S, Sahoo SK (2011) PLGA nanoparticles containing various anticancer agents and tumour delivery by EPR effect. Adv Drug Deliv Rev 63:170–183

    Article  CAS  Google Scholar 

  11. Pereira MA, Mosqueira VCF, Vilela JMC, Andrade MS, Ramaldes GA, Cardoso VN (2008) PLA–PEG nanocapsules radiolabeled with 99mTc-HMPAO: release properties and physicochemical characterization by atomic force microscopy and photon correlation spectroscopy. Eur J Pharm Sci 33:42–51

    Article  CAS  Google Scholar 

  12. Mosqueira VC, Legrand P, Gulik A, Bourdon O, Gref R, Labarre D, Barratt G (2001) Relationship between complement activation, cellular uptake and surface physicochemical aspects of novel PEG-modified nanocapsules. Biomaterials 22:2967–2979

    Article  CAS  Google Scholar 

  13. Singh UV, Bisht KS, Rao S, Devi PU, Udupa N (1996) Plumbagin-loaded PLGA Microspheres with Reduced Toxicity and Enhanced Antitumour Efficacy in Mice. Pharm Pharmacol Commun 2:407–440

    CAS  Google Scholar 

  14. Brannon-Peppas L (1995) Recent advances on the use of biodegradable microparticles and nanoparticles in controlled drug delivery. Int J Pharm 116:1–9

    Article  CAS  Google Scholar 

  15. Peltonen L, Koistinen P, Karjalainen M, Häkkinen A, Hirvonen J (2002) The effect of cosolvents on the formulation of nanoparticles from low-molecular-weight poly(l)lactide. AAPS PharmSciTech 3:52–58

    Article  Google Scholar 

  16. Cu Y, Saltzman WM (2009) Controlled surface modification with poly(ethylene)glycol enhances diffusion of PLGA nanoparticles in human cervical mucus. Mol Pharm 6:173–181

    Article  CAS  Google Scholar 

  17. Yurt Kilcar A, Tekin V, Biber Muftuler FZ, Medine EI (2015) 99mTc labeled plumbagin: estrogen receptor dependent examination against breast cancer cells and comparison with PLGA encapsulated form. J Radioanal Nucl Chem. doi:10.1007/s10967-015-4284-1

    Google Scholar 

  18. Musumeci T, Ventura CA, Giannone I, Ruozi B, Montenegro L, Pignatello R, Puglisi G (2006) PLA/PLGA nanoparticles for sustained release of docetaxel. Int J Pharm 325:172–179

    Article  CAS  Google Scholar 

  19. Zhen W, Han H, Anguiano M, Lemere CA, Cho CG, Lansbury PT (1999) Synthesis and amyloid binding properties of rhenium complexes: preliminary progress toward a reagent for SPECT imaging of Alzheimer’s disease brain. J Med Chem 42:2805–2815

    Article  CAS  Google Scholar 

  20. Mele’ndez-Alafort LM, Riondato M, Nadali A, Mele L, Banzato A, Camporese D, Boccaccio P, Uzunov N, Rosato A, Mazzi U (2006) Bioavailability of 99mTc-Ha-paclitaxel complex [99mTc-ONCOFID-P] in mice using four different administration routes. Nucl Med Biol 49:939–950

    Google Scholar 

  21. Mirahmadi N, Babaei MH, Vali AM, Daha FJ, Kobarfard F, Dadashzadeh S (2008) 99mTc-HMPAO-labeled liposomes: an investigation into the effects of some formulation factors on labeling efficiency and in vitro stability. Nucl Med Biol 35:387–392

    Article  CAS  Google Scholar 

  22. Mora-Huertas CE, Fessi H, Elaissari A (2010) Polymer-based nanocapsules for drug delivery. Int J Pharm 385:113–142

    Article  CAS  Google Scholar 

  23. Ballinger JR, Duncan J, Hua AH, Ichise M (1997) Accumulation of 99mTc-HMPAO and 99mTc-ECD in rodent and human breast tumor cell lines in vitro. Ann Nucl Med 11:95–99

    Article  CAS  Google Scholar 

  24. Chattopadhyay S, Das MK, Vanaja R, Ramamoorthy N (2001) Purification and stabilization of 99mTc-d, l-HMPAO: role of organic extractants. Nucl Med Biol 28:741–744

    Article  CAS  Google Scholar 

  25. Schwochau K (2000) Technetium chemistry and radiopharmaceutical applications. Wiley-VCH, Winheim

    Google Scholar 

  26. Dischino DD, Welch JM, Kilbourn RM, Raichle EM (1983) Relationship Between Lipophilicity and Brain Extraction of C-11-Radiopharmaceuticals. J Nucl Med 24:1030–1038

    CAS  Google Scholar 

  27. Zolle I (2007) 99mTc pharmaceuticals preparation and quality control in nuclear medicine. Springer, New York

    Google Scholar 

Download references

Acknowledgments

Current work is supported by Ege University Research Fund (contract no 2011 NBE 003). The authors thank to Cansu Uzaras and Çiğdem İçhedef for the technical assistance during the assays.

Author information

Authors and Affiliations

Authors

Corresponding author

Correspondence to Ayfer Yurt Kilcar.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Yurt Kilcar, A., Biber Muftuler, F.Z., Medine, E.I. et al. PLGA encapsulation effect on Bioquin-HMPAO: radiolabeling and in vitro behaviour on brain and lung cancer cells. J Radioanal Nucl Chem 310, 155–164 (2016). https://doi.org/10.1007/s10967-016-4746-0

Download citation

  • Received:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s10967-016-4746-0

Keywords

Navigation