Skip to main content

Advertisement

SpringerLink
Log in

Improvement of cellular uptake of hydrophilic molecule, calcein, formulated by liposome

  • Original Article
  • Published:
Journal of Pharmaceutical Investigation Aims and scope Submit manuscript

Abstract

The aim of this study was to prepare the liposome with 1,2-distearoyl-sn-glycero-3-phosphocholine, 1.2 dioleoyl-sn-glycero-3-phosphoethanolamine, cholesteyl hemisuccinate, calcein as a drug model and evaluate physicochemical characteristics such as particle size, polydispersity index (PDI), encapsulation efficiency (EE). Also, the morphology of the blank liposome (without calcein) and the calcein-loaded liposome was observed by a transmission electron microscope (TEM). The particle size and PDI of the blank liposome and the calcein-loaded liposome without tween 80 were 139.8 ± 4.497, 0.31 ± 0.03 and 150.8 ± 8.45, 0.29 ± 0.03 nm, respectively. In addition, it was confirmed that the particle size of the calcein-loaded liposome increased from 294. 6 ± 17.8 to 466.4 ± 78.4 nm when tween 80 was used from 1 to 6%. EE of the calcein-loaded liposome was 66.0 ± 0.58%, independent of the concentration of tween 80. TEM images showed that the shape of the blank liposome and the calcein-loaded liposome was round. In vitro drug release test, calcein from the liposome released approximately 20–25 and 40–50% in pH 7.4 and 4.0, respectively, with a sustained release pattern. The cellular uptake of calcein from the calcein-loaded liposome was about 1.08-fold than that from the calcein solution at 10 µM for a 2 h incubation time. These results suggest that the calcein-loaded liposome was successfully prepared, and could be an application for a hydrophilic drug in further study.

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

Similar content being viewed by others

References

  • Allen TM, Hansen C, Martin F, Redemann C, YanYoung A (1991) Liposome containing synthetic lipid derivatives of poly(ethylene glycol) show prolonged circulation half- lives in vivo. Bicochim Biophys Acta 1006:29–36

    Article  Google Scholar 

  • Bergstrand N (2003) Liposomes for drug delivery from physico-chemical studies to applications. Comprehensive Summaries of Uppsala Dissertations from the Faculty of Science and Technology

  • Chena Y, Minh LV, Liua J, Angelov B, Drechsler M, Garamus VM, Willumeit-Römerd R, Zoua A (2016) Baicalin loaded in folate-PEG modified liposomes for enhanced stability and tumor targeting. Colloids Surface B 140:74–82

    Article  CAS  Google Scholar 

  • Cho SM, Lee HY, Kim JC (2008) pH-dependent release property of dioleoylphosphadiylcholine ethanolamine liposome. Korean J Chem Eng 25:390–393

    Article  CAS  Google Scholar 

  • Cullis PR, Kruijff BDE (1979) Lipid polymorphism and the functional roles of lipids in biological Membranes. Biochim Biophys Acta 559:339–420

    Article  Google Scholar 

  • Ducat E, Evrard B, Peulen O, Piel G (2011a) Cellular uptake of liposomes monitored by confocal microscopy and flow cytometry. J Drug Del Sci Tech 21:469–477

    Article  CAS  Google Scholar 

  • Ducat E, Deprez J, Gillet A, Noël A, Evrard B, Peulen P, Piel G (2011b) Nuclear delivery of a therapeutic peptide by long circulating pH-sensitive liposomes: benefits over classical vesicles. Int J Pharm 420:319–332

    Article  PubMed  CAS  Google Scholar 

  • Ellens H, Bentz J, Szoka FC (1984) pH-induced destabilization of phosphatidylethanolamine-containing liposomes: role of bilayer contact. Biochemistry 23:1532–1538

    Article  PubMed  CAS  Google Scholar 

  • Eloy JO, de Souza MC, Petrilli R, Barcellos JPA, Lee RJ, Marchetti JM (2014) Liposomes as carriers of hydrophilic small molecule drugs: strategies to enhance encapsulation and delivery. Colloids Surf B 123:345–363

    Article  CAS  Google Scholar 

  • Jiang M, Gan L, Zhu C, Dong Y, Liu J, Gan Y (2012) Cationic core–shell liponanoparticles for ocular gene delivery. Biomaterials 33:7621–7630

    Article  PubMed  CAS  Google Scholar 

  • Jin S, Ye K (2007) Nanoparticle-mediated drug delivery and gene therapy. Biotechnol Prog 23:32–41

    Article  PubMed  CAS  Google Scholar 

  • Kim JS (2016) Liposomal drug delivery system. J Pharm Investig 46:387–392

    Article  CAS  Google Scholar 

  • Lee RJ, Low PS (1995) Folate-mediated tumor cell targeting of liposome-entrapped doxorubicin in vitro. Biochim Biophys Acta 1233:134–144

    Article  PubMed  Google Scholar 

  • Lee Y, Graeser R, Kratz F, Geckeler (2011) Paclitaxel loaded polymer nanoparticle for the reversal of multidrug in breast cancer cells. Adv Funt Mater 21:4211–4218

    Article  CAS  Google Scholar 

  • Litzinger DC, Huang L (1992) Phosphatodylethanolamine liposomes: drug delivery, gene transfer and immunodiagnostic applications. Biochim Biophys Acta 1113:201–227

    Article  PubMed  CAS  Google Scholar 

  • Liu D, Huang L (1990) pH-sensitive, plasma-stable liposomes with relatively prolonged residence in circulation. Biochim Biophys Acta 1022:348–354

    Article  PubMed  CAS  Google Scholar 

  • Liu X, Sun W, Zhang B, Tian B, Tang X, Qi N, He H, Li H, Jin X (2013) Clarithromycin-loaded liposomes offering high drug loading and less irritation. Int J Pharm 443:318–327

    Article  PubMed  CAS  Google Scholar 

  • Maheswaran A, Brindha P, Mullaicharam AR, Masilamani K (2013) Liposomal drug delivery systems—a review. Int J Pharm Sci Rev Res 23:295–301

    CAS  Google Scholar 

  • Needham D, Nunn RS (1990) Elastic deformation and failure of lipid bilayer membranes containing cholesterol. Biophys J 58:997–1009

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Seddon JM (1990) Structure of the inverted hexagonal (HII) phase, and non-lamellar phase transition of lipids. Biochim Biophys Acta 1031:1–69

    Article  PubMed  CAS  Google Scholar 

  • Smaby JM, Momsen MM, Brockman HL, Brown RE (1997) Phosphatidylcholine acyl unsaturation modulates the decrease in interfacial elasticity induced by cholesterol. Biophys J 73:1492–1505

    Article  PubMed  PubMed Central  CAS  Google Scholar 

  • Straubinger RM, Düzgünes N, Papahadjopoulos D (1984) pH-sensitive liposomes mediate cytoplasmic delivery of encapsulated macromolecules. FEBS Lett 179:148–154

    Article  Google Scholar 

  • Voinea M, Simionescu M (2002) Designing of ‘intelligent’ liposomes for efficient delivery of drug. J Cellular Mol Med 6:465–474

    Article  CAS  Google Scholar 

  • Xu H, James W, Wu Z (2015) Enhanced pH- responsiveness, cellular trafficking, cytotoxicity and long-circulation of PEGylated liposomes with post-insertion technique using gemictabine as a model drug. Pharm Res 32:2428–2438

    Article  PubMed  CAS  Google Scholar 

Download references

Acknowledgements

This article does not contain any studies with human and animal subjects performed by any of the authors. All authors (S.M Han, Y.G. Na, H.S. Lee, G.H. Son, S.H. Jeon, K.H. Bang, S.J. kim, H.J. Lee, C.W. Cho) declare that they have no conflict of interest. This work was supported by the research fund of Chungnam National University. We’d like to thank Ms. Youngjoo Sul for proofreading this manuscript.

Author information

Authors and Affiliations

  1. College of Pharmacy and Institute of Drug Research and Development, Chungnam National University, 99 Daehak-ro, Yuseong-gu, Daejeon, 34134, South Korea

    Su-Min Han, Young-Guk Na, Han-Sol Lee, Gi-Ho Son, Seong-Hoon Jeon, Ki-Hyun Bang, Sung-Jin Kim, Hye-Jin Lee & Cheong-Weon Cho

Authors
  1. Su-Min Han
    View author publications

    You can also search for this author in PubMed Google Scholar

  2. Young-Guk Na
    View author publications

    You can also search for this author in PubMed Google Scholar

  3. Han-Sol Lee
    View author publications

    You can also search for this author in PubMed Google Scholar

  4. Gi-Ho Son
    View author publications

    You can also search for this author in PubMed Google Scholar

  5. Seong-Hoon Jeon
    View author publications

    You can also search for this author in PubMed Google Scholar

  6. Ki-Hyun Bang
    View author publications

    You can also search for this author in PubMed Google Scholar

  7. Sung-Jin Kim
    View author publications

    You can also search for this author in PubMed Google Scholar

  8. Hye-Jin Lee
    View author publications

    You can also search for this author in PubMed Google Scholar

  9. Cheong-Weon Cho
    View author publications

    You can also search for this author in PubMed Google Scholar

Corresponding author

Correspondence to Cheong-Weon Cho.

Rights and permissions

Reprints and permissions

About this article

Check for updates. Verify currency and authenticity via CrossMark

Cite this article

Han, SM., Na, YG., Lee, HS. et al. Improvement of cellular uptake of hydrophilic molecule, calcein, formulated by liposome. J. Pharm. Investig. 48, 595–601 (2018). https://doi.org/10.1007/s40005-017-0358-0

Download citation

  • Received:

  • Accepted:

  • Published:

  • Issue Date:

  • DOI: https://doi.org/10.1007/s40005-017-0358-0

Keywords

Search

Navigation