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Med J Tabriz Uni Med Sciences. 2021;43(4): 335-345.
doi: 10.34172/mj.2021.060
  Abstract View: 96
  PDF Download: 16

Original Article

Development of polymeric micelles loaded with STAT3 inhibitory, Stattic, for cancer treatment

Hamed Masoumzadeh 1 ORCID logo, Nasrin Hoseinzad 1 ORCID logo, Sevda Jafari 1 ORCID logo, Ali Shayanfar 2 ORCID logo, Haleh Vaez 3 ORCID logo, Ommoleila Molavi 1و4و5* ORCID logo

1 Department of Pharmaceutical Biotechnology, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
2 Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
3 Department of Pharmacology, Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran
4 Biotechnology Research Center, Tabriz University of Medical Science, Tabriz, Iran
5 Molecular Medicine Research Center, Tabriz University of Medical Science, Tabriz, Iran
*Corresponding author; molavio@tbzmed.ac.ir

Abstract

Background. STAT3 is an oncogenic signaling pathway found constitutively active in many types of human malignancies and plays a key role in cancer progression. Stattic is a small molecule, which selectively inhibits the SH2 domain of STAT3. In most studies, stattic has been proposed as a promising strategy STAT3 inhibition in cancer cells harboring constitutively active STAT3. However, the lack of proper formulation due to the poor water solubility and low bioavailability of stattic is a major limitation for its usage in the clinic. This project aimed to develop poly(ethylene glycol)-block-poly(caprolactone) (PEG-b-PCL)-based polymeric micelles loaded with stattic and evaluate drug encapsulation efficiency and release in the developed formulations.

Methods. In this experimental study, to prepare stattic loaded micellar formulations, the co-solvent evaporation method was used. The mean diameter and polydispersity index (PDI) of micelles were defined by the light scattering method. Encapsulated drug levels were measured using high-performance liquid chromatography (HPLC). Data were analyzed using GraphPad Prism software through one-way ANOVA.

Results. Stattic was loaded in the polymeric micelles with encapsulation efficiency ranging from 40% to 73%. Drug loaded micelles were measured between 90 to 130 nm in size. PDI was obtained 0.3-1, and encapsulation of stattic in Polyethylene glycol-block-poly (α-benzyl carboxylate ε-caprolactone (PEG-b-PBCL) micellar formulation resulted in a more than 6-fold increase in the water solubility of stattic (0.36 vs. 0.06 mg/mL). Regarding high encapsulation efficiency, two micellar formulations were selected for further analysis in that both of them released 70-80% of the drug within the first hour, indicating burst release of the drug.

Conclusion. These findings show that PEG-b-PBCL copolymers can be a suitable vehicle for the solubilization of stattic.

Keywords: STAT3 inhibitor, Nanoparticle, Cancer, Stattic
Masoumzadeh H, Hoseinzad N, Jafari S, Shayanfar A, Molavi OL, Vaez H. Development of polymeric micelles loaded with STAT3 inhibitory, Stattic, for cancer treatment. Med J Tabriz Uni Med Sciences. 2021;43(4):335-345. Persian.
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Submitted: 15 Dec 2019
ePublished: 15 Sep 2021
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