AAPS PharmSciTech

, Volume 16, Issue 4, pp 973–985 | Cite as

The Anti-Melanoma Efficiency of the Intratumoral Injection of Cucurbitacin-Loaded Sustained Release Carriers: In Situ-Forming Implants

  • Jianbo Guo
  • Junwei Wang
  • Chenchen Cai
  • Jinghua Xu
  • Hongdan Yu
  • Hui Xu
  • Tang Xing
Research Article

Abstract

Our previous studies revealed that the PLGA-based particulate systems loaded with cucurbitacin showed limited anti-melanoma efficiency in xenograft animal models after intratumoral injection, which was due to the undesirable initial burst release and the leakage of the particulate carriers from the injection site through the pinhole. In this paper, two categories of in situ-forming implants (ISFIs) for intratumoral injection, PLGA ISFIs and SAIB ISFIs, were systemically evaluated for their potentials for on solid tumor treatment via intratumoral injection. The in vitro drug release profiles of these two ISFIs were different due to the different sol–gel transition properties. The pharmacodynamics results revealed that SAIB ISFIs displayed obvious therapeutic efficiencies to melanoma, and multi-points injection of SASIB ISFIs displayed better efficiency than single-point injection. The different sol–gel transition properties and mechanism for PLGA ISFIs and SAIB ISFIs affected both the drug release and strongly impacted the pharmacokinetic parameters and pharmacodynamic effectiveness. Also, the adhesive property of SAIB to the local tissue could extend the retention and inhibit the leakage of the SAIB ISFIs, thus enhanced the anticancer effectiveness. Comparison of the various intratumoral injection systems, appropriate drug release profiles (lower initial burst and steady release) and good retention (minimum leakage from the injection site) would benefit to the antitumor effects of the intratumoral depots.

KEY WORDS

anti-melanoma efficiency cucurbitacin drug release in situ-forming implants (ISFIs) intratumoral injection 

Notes

Acknowledgments

We thank Prof. Deng Yihui, Shenyang Pharmaceutical University, for his helpful comments on animal studies, Mr. Tian Han, Zhongshan School of Medicine, SUN YAT-SEN University, for his help on cellular experiments and results explanations, and Prof. Takshi Ikejima, Shenyang Pharmaceutical University, who kindly provided the A375.S2 human melanoma cell.

Supplementary material

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Copyright information

© American Association of Pharmaceutical Scientists 2015

Authors and Affiliations

  • Jianbo Guo
    • 1
    • 2
  • Junwei Wang
    • 3
  • Chenchen Cai
    • 1
  • Jinghua Xu
    • 4
  • Hongdan Yu
    • 1
  • Hui Xu
    • 1
  • Tang Xing
    • 1
  1. 1.School of PharmacyShenyang Pharmaceutical UniversityShenyangChina
  2. 2.Shanxi Institute for Food and Drug ControlXi’anChina
  3. 3.School of Traditional Chinese MedicineShenyang Pharmaceutical UniversityShenyangChina
  4. 4.School of Life Science and BiopharmaceuticsShenyang Pharmaceutical UniversityShenyangChina

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