Assessing the pharmacokinetics and toxicology of polymeric micelle conjugated therapeutics

ABSTRACT

Introduction: Analogous to nanocarriers such as nanoparticles, liposomes, nano lipoidal carriers, niosomes, and ethosomes, polymeric micelles have gained significance in the field of drug delivery. They have attracted scientists worldwide by their nanometric size, wide range of polymers available for building block synthesis, stability and potential to enhance the targeting and safety of drugs. Incorporation of drugs within the interior of polymeric micelles alters the drug pharmacokinetics, which generally results in increased efficiency.

Areas covered: This review deals with the pharmacokinetics of various anti-neoplastic drugs loaded into micelles. The structure of polymeric micelles, polymers employed in their development and techniques involved will be discussed. This is followed by discussion on the pharmacokinetics of anti-cancer drugs loaded into polymeric micelles and the toxicity concerns associated.

Expert opinion: Polymeric micelles are nanometeric carriers, with higher stability, polymeric flexibility and higher drug loading of poorly water-soluble drugs. These nanosystems help in increasing the bioavailability of drugs by encapsulating them within the hydrophobic core. The proper selection and design of the amphiphilic polymer for micelles is a crucial step as it decides the toxicity and the biocompatibility.

KEYWORDS:

• Amphiphilic polymers
• drug Delivery
• hydrophobic drugs
• targeting
• solubilization

Article highlights

• Brief description of the basic structure of micelles and polymers employed in their preparation

• Techniques for the formulation of polymeric micelles have been reviewed, and the data is disclosed

• The effect of the polymeric micelles on the pharmacokinetic parameters of the encapsulated drug is discussed in detail

• Toxicology and the factors responsible for the toxicology and biocompatible carriers to overcome these issues of micellar systems are reviewed.

• The potential applicability of polymeric micelles in drug delivery is discussed, including the assessment of polymeric micelles and the validation of pharmacokinetics along with toxicity parameters.

• This box summarizes key points contained in the article.

Declaration of interest

The authors have no relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript. This includes employment, consultancies, honoraria, stock ownership or options, expert testimony, grants or patents received or pending, or royalties.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.