Abstract
A novel polymer-drug conjugate was prepared by the chemical reaction between the copolymer Pluronic P123 and the docetaxel via a pH sensitive hydrazone bond. These pluronic P123-docetaxel (DTX) conjugates (P123-DTX) could form the stable drug-loaded materials that can self-assemble into the defined nano-micelles in aqueous solution because of their obvious amphiphilic property and low critical micelle concentration. The spherical morphology and particle size of the prepared nano-micelles were characterized by transmission electron microscopy and dynamic light scattering, respectively. Moreover, after the introduction of pH sensitive hydrazone bond, P123-DTX micelle showed a pH dependent drug release behavior. At pH 5.0 (in 48 h), the cumulative release amount of DTX were ~84.9%, which is about six times higher than that at pH 7.4. The prepared novel p123-DTX conjugates may offer a great benefit for drug delivery and controlling the drug release.
Highlights
One purpose to design smart materials is for the sake of its better applications in the field of medicine [1]
It had been reported that the modification of taxanes by levulic acid could be an effective way in forming the pH sensitive conjugate to fulfill the issue of stability and controlled release [20,21,22]
Pluronic P123-DTX conjugates were characterized by 1H NMR, respectively (Figures 2 and 3)
Summary
One purpose to design smart materials is for the sake of its better applications in the field of medicine [1]. Micelles formed by copolymers have shown its huge potential in anticancer drug delivery These self-assembled micellar carriers often expose inadequate in vivo stability, which leads to premature drug release following intravenous injection. Binding with albumin via the acid-sensitive hydrazone contained linker, the INNO-206 conjugates can release doxorubicin selectively at the tumor site, which showed significantly superior antitumor efficacy and a good safety profile over free doxorubicin [17]. At this stage, the INNO-206 conjugates is evaluated for its effective antitumor therapy against different tumor xenograft models and has the potential to be a promising clinical candidate for treating a broad range of solid tumors [18]. The micelles formed by these P123-DTX conjugates were evaluated and investigated to verify its potential to balance the stability and drug release
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