Localized delivery of active targeting micelles from nanofibers patch for effective breast cancer therapy

[Display omitted] •Stimuli-responsive core–shell nanofibers release thedrug at target sites.•Core-shell nanofibers prepared using psyllium husk mucilage with coaxial electrospinning.•Maximum erosion of nanofibers in acidic pH causes maximum release of drug in cancer cells.•Nanofibers effectively int...

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Veröffentlicht in:International journal of pharmaceutics 2020-06, Vol.584, p.119412, Article 119412
Hauptverfasser: Mehnath, Sivaraj, Chitra, Karuppannan, Karthikeyan, Kandhasamy, Jeyaraj, Murugaraj
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Sprache:eng
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Zusammenfassung:[Display omitted] •Stimuli-responsive core–shell nanofibers release thedrug at target sites.•Core-shell nanofibers prepared using psyllium husk mucilage with coaxial electrospinning.•Maximum erosion of nanofibers in acidic pH causes maximum release of drug in cancer cells.•Nanofibers effectively internalizes to the skin, biocompatible and cytotoxicity of nanofibers was evaluated.•Compared to paclitaxel, drug loaded nanofibers exhibited higher cytotoxicity. Nanofibers based transdermal drug delivery is a promising platform, and it effectively delivers the drug to tumor sites. The objective of the study was to fabricate stimuli-responsive polymeric nanofibers encapsulated with an active targeting micellar system for in situ drug delivery. Stimuli-responsive core–shell nanofibers release thedrug at target sites with minimum side effects to the other organs, decrease the drug administration concentration. Initially, we prepared CA conjugated PCPP polymeric micelles loaded with PTX. Then, core–shell nanofibers were prepared using PHM with coaxial electrospinning and distinct core–shell nanofibers formation confirm by SEM and TEM. Nanofibers showed a homogenous distribution of micelles inside the fiber mesh, diffusion, and erosion processes lead to a controlled release of PTX.In vitro drug release and swelling, revealed the pH based sustained release of the drug for 180 h from the nanofibers mat. Functional and stimuli-responsive nanofibers highly absorb H+ ions and repulsion of cations promoting maximum swelling to release more drugs in acidic pH. An increased transportation rate of 70% drug release through epidermis for 120 h. Nanofibers effectively internalize to the skin, and it confirmed by confocal microscopy. MCF-7 cells grown and spread over the nanofibers, which show the biocompatibility of nanofibers. Compared to PTX, drug-loaded nanofibers exhibited higher cytotoxicity for 8 days which was confirmed by the flow cytometry. These promising results confirm, the novel stimuli-responsive core–shell nanofibers actively target breast cancer cells and lead the way to safe cancer therapy.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2020.119412