Abstract
Stimuli-responsive systems for controlled drug release have been extensively explored in recent years. In this work, we developed a reduction-responsive camptothecin (CPT) nanocapsule (CPT-NC) by combining nanoprecipitation and in situ polymerization using a polymerized surface ligand and a disulfide bond-containing crosslinker. Dissolution rate studies proved that the CPT-NCs have robust drug-release profiles in the presence of glutathione (GSH) owing to the division of the disulfide bond crosslinker which triggers the collapse of the polymer layer. Furthermore, the in vitro investigations demonstrated that the CPT-NCs exhibited a high-cellular uptake efficiency and cytotoxicity for cancer cells of squamous cell carcinoma (SCC-15). Our approach thus presents an effective intracellular drug delivery strategy for anticancer therapy.
Highlights
Polymer nanocarriers, including amphiphilic copolymer micelles/ polymersomes, polyester-based polymer nanoparticles, and polymer nanogels/nanocapsules, have been extensively explored for cancer chemotherapy aimed at enhancing drug solubility in aqueous phase, prolonging in vivo blood circulation time, improving passive tumor targeting by the enhanced permeability and retention (EPR) effect, and reducing side effects [1–5]
In situ polymerization was initiated on the surface of NanoCPTs using the OP-AC surface ligand, and by utilizing BIS and bis(acryloyl) cystamine (BAC) crosslinkers, both the nonresponsive CPT-NCs-A and the reduction-responsive CPT-NCs-B were successfully prepared
The drug release studies proved that CPT nanocapsules that contained disulfide bond crosslinkers exhibited sensitive drug release behaviors at high-levels of GSH, which could lead to the rapid release of the encapsulated CPT in the cell cytoplasm
Summary
Polymer nanocarriers, including amphiphilic copolymer micelles/ polymersomes, polyester-based polymer nanoparticles, and polymer nanogels/nanocapsules, have been extensively explored for cancer chemotherapy aimed at enhancing drug solubility in aqueous phase, prolonging in vivo blood circulation time, improving passive tumor targeting by the enhanced permeability and retention (EPR) effect, and reducing side effects [1–5]. Amphiphilic polymer micelles/polymersomes constitute some of the most important candidates and have often been used to deliver anticancer drugs with low water solubility by incorporating them into their hydrophobic cores [6–10] These conventional polymer micelles are unstable in the circulating blood in vivo, resulting in serious side effects owing to the premature leakage of the loaded drugs [11,12]. The applications of these nanoparticles are always limited by the slow drug release profiles and poor stability in water To address this tissue, covalently crosslinking strategies have been utilized to fabricate novel polymer nanocarriers, referred to as polymer nanocapsules/nanogels [13–16]. Covalently crosslinking strategies have been utilized to fabricate novel polymer nanocarriers, referred to as polymer nanocapsules/nanogels [13–16] In these polymer nanocapsules, the crosslinked zone cannot only retain their structural integrity, and acts as a physical barrier for preventing premature release of the loaded drugs, and reduces drug side effects during blood circulation
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