Exploration of docetaxel palmitate and its solid lipid nanoparticles as a novel option for alleviating the rising concern of multi-drug resistance.


Journal

International journal of pharmaceutics
ISSN: 1873-3476
Titre abrégé: Int J Pharm
Pays: Netherlands
ID NLM: 7804127

Informations de publication

Date de publication:
30 Mar 2020
Historique:
received: 01 08 2019
revised: 23 01 2020
accepted: 24 01 2020
pubmed: 1 2 2020
medline: 1 12 2020
entrez: 1 2 2020
Statut: ppublish

Résumé

Docetaxel (DTX), a widely prescribed anticancer agent, is now associated with increased instances of multidrug resistance. Also, being a problematic BCS class IV drug, it poses challenges for the formulators. Henceforth, it was envisioned to synthesize an analogue of DTX with a biocompatible lipid, i.e., palmitic acid. The in-silico studies (molecular docking and simulation) inferred lesser binding of docetaxel palmitate (DTX-PL) with P-gp vis-à-vis DTX and paclitaxel, indicating it to be a poor substrate for P-gp efflux. Solid lipid nanoparticles (SLNs) of the conjugate were prepared using various lipids, viz. palmitic acid, stearic acid, cetyl palmitate and glyceryl monostearate. The characterization studies for the nanocarrier were performed for the surface charge, drug payload, micromeritics, release pattern of drug and surface morphology. From the cytotoxicity assays on resistant MCF-7 cells, it was established that the new analogue offered substantially decreased IC

Identifiants

pubmed: 32001291
pii: S0378-5173(20)30072-7
doi: 10.1016/j.ijpharm.2020.119088
pii:
doi:

Substances chimiques

Antineoplastic Agents 0
Lipids 0
Docetaxel 15H5577CQD
Serum Albumin, Human ZIF514RVZR

Types de publication

Journal Article

Langues

eng

Sous-ensembles de citation

IM

Pagination

119088

Informations de copyright

Copyright © 2020 Elsevier B.V. All rights reserved.

Déclaration de conflit d'intérêts

Declaration of Competing Interest The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.

Auteurs

Lokesh Kaushik (L)

Department of Pharmacy, School of Chemical Sciences & Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan 305817, India.

Shubham Srivastava (S)

Department of Pharmacy, School of Chemical Sciences & Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan 305817, India.

Anshul Panjeta (A)

Department of Biophysics, Panjab University, Chandigarh 160014, India.

Dasharath Chaudhari (D)

Centre for Pharmaceutical Nanotechnology Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Sector 67, S.A.S. Nagar (Mohali), Punjab 160062, India.

Rohan Ghadi (R)

Centre for Pharmaceutical Nanotechnology Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Sector 67, S.A.S. Nagar (Mohali), Punjab 160062, India.

Kaushik Kuche (K)

Centre for Pharmaceutical Nanotechnology Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Sector 67, S.A.S. Nagar (Mohali), Punjab 160062, India.

Ruchi Malik (R)

Department of Pharmacy, School of Chemical Sciences & Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan 305817, India.

Simran Preet (S)

Department of Biophysics, Panjab University, Chandigarh 160014, India.

Sanyog Jain (S)

Centre for Pharmaceutical Nanotechnology Department of Pharmaceutics, National Institute of Pharmaceutical Education & Research (NIPER), Sector 67, S.A.S. Nagar (Mohali), Punjab 160062, India.

Kaisar Raza (K)

Department of Pharmacy, School of Chemical Sciences & Pharmacy, Central University of Rajasthan, Bandarsindri, Ajmer, Rajasthan 305817, India. Electronic address: drkaisar@curaj.ac.in.

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Classifications MeSH