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Pharmacokinetic Consequences of PLGA Nanoparticles in Docetaxel Drug Delivery

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Background: Cancer chemotherapy is accompanied with administration of highly potent cytotoxic agents in doses that can result in non-specific drug toxicity and side effects. Chemotherapeutic agents possess limitations such as lack of water solubility, high volume of distribution, poor bioavailability, narrow therapeutic indices, multi-drug resistance, etc. that raise serious matters of concern regarding drug’s pharmaceutical and clinical aspects. However, application of nanoparticles in delivery of anti-cancer agents has been a popular approach to address these concerns. Poly (lactide-co-glycolide) (PLGA), a biocompatible/biodegradable FDA-approved polymer has been widely used as drug carrier to enhance pharmaceutical/therapeutic properties of anticancer agents, prolonging their circulation time, targeting cancer tissues or protecting the drug from rapid elimination/premature degradation. This favourably modifies drug’s pharmacokinetics and pharmacodynamics.

Objective: This paper provides a general perspective on how association of docetaxel to PLGA nanoparticles potentially modifies pharmacokinetics and biodistribution profile of the anticancer agent.

Method: A comprehensive literature search has been conducted and dedicated to compile most relevant and up-to-date material about pharmacokinetic consequences of PLGA nanoparticles in docetaxel drug delivery.

Results: A set of determinants are considered to be influential on biodistribution and fate of docetaxel and PLGA nanoparticles. These are attributed to physicochemical properties of PLGA polymer, docetaxel, nanoparticle, and the set of events imposed to the nanoparticles by the host body.

Conclusion: Association of PLGA nanoparticles and docetaxel has demonstrated to modify the drug’s pharmacokinetic and biodistribution profile.
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Keywords: Pharmacokinetics; biodistribution; docetaxel; poly (lactide-co-glycolide) (PLGA); poly (lactide-co-glycolide)-poly (ethylene glycol) (PLGA-PEG); polymeric nanoparticles

Document Type: Research Article

Publication date: March 1, 2017

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  • Pharmaceutical Nanotechnology publishes original manuscripts, reviews, thematic issues, rapid technical notes and commentaries that provide insights into the synthesis, characterisation and pharmaceutical (or diagnostic) application of materials at the nanoscale. The nanoscale is defined as a size range of below 1 µm. Scientific findings related to micro and macro systems with functionality residing within features defined at the nanoscale are also within the scope of the journal. Manuscripts detailing the synthesis, exhaustive characterisation, biological evaluation, clinical testing and/ or toxicological assessment of nanomaterials are of particular interest to the journal’s readership. Articles should be self contained, centred around a well founded hypothesis and should aim to showcase the pharmaceutical/ diagnostic implications of the nanotechnology approach. Manuscripts should aim, wherever possible, to demonstrate the in vivo impact of any nanotechnological intervention. As reducing a material to the nanoscale is capable of fundamentally altering the material’s properties, the journal’s readership is particularly interested in new characterisation techniques and the advanced properties that originate from this size reduction. Both bottom up and top down approaches to the realisation of nanomaterials lie within the scope of the journal.
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