Hossein Danafar
1,2,3, Soodabeh Davaran
1*, Kobra Rostamizadeh
2,3, Hadi Valizadeh
4, Mehrdad Hamidi
3,51 Faculty of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
2 Zanjan Pharmaceutical Nanotechnology Research Center, Zanjan University of Medical Sciences, Zanjan, Iran.
3 Department of Medicinal Chemistry, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
4 Department of Pharmaceutics, School of Pharmacy, Tabriz University of Medical Sciences, Tabriz, Iran.
5 Department of Pharmaceutics, School of Pharmacy, Zanjan University of Medical Sciences, Zanjan, Iran.
Abstract
Purpose: Among the potent anticancer agents, curcumin is known as a very
efficacious against many different types of cancer cells, but its
clinical applications has been limited because of hydrophobicity, low
gastrointestinal absorption, poor bioavailability and rapid metabolism.
In this way, a novel micellar delivery system with mPEG–PCL was
synthesized and the release profile of the curcumin from the drug-loaded
micelles was evaluated.
Methods: In this study, curcumin was encapsulated within
monomethoxypoly(ethylene glycol)-poly(ε-caprolactone) (mPEG-PCL)
micelles through a single-step nano-precipitation method, leading to
creation of curcumin-loaded mPEG-PCL (Cur/mPEG-PCL) micelles. Di-block
mPEG-PCL copolymers were synthesized and used to prepare micelles.
mPEG-PCL copolymer was characterized in vitro by HNMR, FTIR, DSC and GPC
techniques. Then, mPEG–PCL copolymers with curcumin were self-assembled
into micelles in aqueous solution. The resulting micelles were
characterized further by various techniques such as dynamic light
scattering (DLS) and atomic force microscopy (AFM).
Results: The findings showed the successful formation of smooth and
spherical curcumin-loaded micelles. The encapsulation efficiency of
curcumin was 88 ± 3.32%. The results of AFM revealed that the micelles
have spherical shapes with size of 73.8 nm. The release behavior of
curcumin from micelles was compared in different media. In vitro release
of curcumin from curcumin-entrapped micelles was followed remarkably
sustained profile. The sustained release of drug was hypothetically due
to the entrapment of curcumin in core of micelles.
Conclusion: The results indicate the successful formulation of curcumin
loaded m-PEG/PCL micelles. From the results, iIt can be concluded that
curcumin m-PEG-PCL micelles may be considered as an effective treatment
strategy for cancer in the future.