Effect of polymer microstructure on the docetaxel release and stability of polyurethane formulation.

Eur J Pharm Biopharm

Centre for Pharmaceutical Innovation and Development (CPID), School of Pharmacy and Medical Sciences, University of South Australia, Adelaide, SA 5000, Australia. Electronic address:

Published: April 2016

PurSil®AL20 (PUS), a copolymer of 4,4'-dicyclohexylmethane diisocyanate (HMDI), 1,4-butane diol (BD), poly-tetramethylene oxide (PTMO) and poly-dimethyl siloxane (PDMS) was investigated for stability as a vehicle for Docetaxel (DTX) delivery through oesophageal drug eluting stent (DES). On exposure to stability test conditions, it was found that DTX release rate declined at 4 and 40 °C. In order to divulge reasons underlying this, changes in DTX solid state as well as PUS microstructure were followed. It was found that re-crystallization of DTX in PDMS rich regions was reducing the drug release at both 4 °C and 40 °C samples. So far microstructural features have not been correlated with stability and drug release, and in this study we found that at 40 °C increase in microstructural domain sizes and the inter-domain distances (from ∼85 Å to 129 Å) were responsible for hindering the DTX release in addition to DTX re-crystallization.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.ejpb.2016.01.015DOI Listing

Publication Analysis

Top Keywords

dtx release
8
drug release
8
dtx
6
release
5
polymer microstructure
4
microstructure docetaxel
4
docetaxel release
4
stability
4
release stability
4
stability polyurethane
4

Similar Publications

Early diagnosis of pancreatic ductal adenocarcinoma (PDAC) is challenging because of its depth, which often leads to misdiagnosis during ultrasound examinations. The unique PDAC tumor microenvironment (TME) is characterized by significant fibrous tissue growth, and high interstitial pressure hinders drug penetration into tumors. Additionally, hypoxia and immune suppression within the tumor contribute to poor responses to radiotherapy and chemotherapy, ultimately leading to an unfavorable prognosis.

View Article and Find Full Text PDF

PSMA-targeted delivery of docetaxel in prostate cancer using small-sized PDA-based micellar nanovectors.

J Control Release

January 2025

Asymmetric Synthesis and Functional Nanosystems Group (Art&Fun), Institute of Chemical Research (IIQ), CSIC-University of Seville, C/ Américo Vespucio 49, 41092 Seville, Spain. Electronic address:

In this study, we present the first comparative analysis of active and passive drug delivery systems for docetaxel (DTX) in prostate cancer using supramolecular self-assembled micellar nanovectors. Specifically, we developed two novel micelles based on polydiacetylenic amphiphiles (PDA) for passive and active targeting. The active targeting micelles were designed with a prostate-specific membrane antigen (PSMA) ligand, ACUPA, to facilitate recognition by PSMA-positive cancer cells.

View Article and Find Full Text PDF

Effects of linkers on the development of liposomal docetaxel-glutathione prepared by active click loading.

Int J Pharm

January 2025

Department of Pharmaceutics, College of Pharmacy, Chongqing Medical University, Chongqing 400016 China. Electronic address:

Loading drug-maleimide (MAL) conjugates into liposomes preloaded with glutathione (GSH) can prepare the liposome encapsulating GSH-conjugated prodrugs, which serve as a feasible way to construct liposomal formulation. However, the effects ofthelinker on the development of this liposomal system remained unclear. Herein, docetaxel (DTX)-MAL conjugates linked by various linkers were used for such studies.

View Article and Find Full Text PDF

Objective: The objective of the study was to tackle the recurrence of prostate cancer (PCa) post-surgery and to re-sensitize the docetaxel (DTX)-resistant PC-3 cells to chemo-therapy using NIC.

Significance: Prolonged DTX therapy leads to the emergence of chemo-resistance by overexpression of PI3K-AKT pathway in PCa along with tumor recurrence post-surgery. Suppression of this pathway could be essential in improving the anticancer activity of DTX and re-sensitizing the resistant cells.

View Article and Find Full Text PDF

Ultrasound-triggered drug-loaded nanobubbles for enhanced T cell recruitment in cancer chemoimmunotherapy.

Biomaterials

January 2025

Department of Ultrasound, Southwest Hospital, Army Medical University, Chongqing, 400038, China. Electronic address:

Chemotherapy combined with immunotherapy is a highly promising approach for treating tumors. However, chemotherapeutic drugs often fail to accumulate effectively at the tumor site after systemic administration and they lack sufficient immunogenicity to activate adaptive immunity, making an effective T-cell immune response within the tumor microenvironment difficult to achieve. Here, this work developed drug-loaded nanobubbles (DTX-R837@NBs) that encapsulate the chemotherapy drug docetaxel and the immune adjuvant R837 via a thin-film hydration method.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!