Synthesis and therapeutic delivery approaches for praziquantel: a patent review (2010-present)

ABSTRACT

Introduction

: Among all the anti-schistosomal drugs, praziquantel has been the most widely used. However, some major challenges have been faced using the drug in the treatment of schistosome infections.

Areas covered

: Several approaches used in the synthesis of praziquantel aimed at reducing the time and cost of production, the toxicity and experimental harsh conditions are discussed. Also, patented methods involved in the pharmaceutical reformulation of praziquantel in the treatment of diverse endoparasitic infestations are reported. Additionally, future perspectives in terms of nanomedicine approach in the formulation of praziquantel are highlighted.

Expert Opinion

: Lipid-based nanosystems (LBNSs) formulations can be used to overcome the shortcomings associated with the use of praziquantel in the schistosomiasis treatment due to their amphipathic nature. This could be a promising vehicle for the delivery of praziquantel, which could in turn improve the bioavailability, as well as reduce the frequent dose of the drug and improve patient compliance. This may sustain the release of the drug and improve the rapid conversion of the drug into inactive metabolite due to rapid metabolism. Additionally, LBNSs approach could increase and improve the lipophilicity of the drug, which could make it easier to interact with the hydrophobic cores of the worm tegument.

KEYWORDS:

• Praziquantel
• schistosomiasis
• drug delivery
• lipid-based nanosystems
• patent
• synthesis

Article highlights

• Praziquantel (PZQ) is currently the only available drug against all forms of schistosomes.

• Even though PZQ is effective against adult worms.

• PZQ has two main drawbacks; the fast metabolism that reduces the bioavailability of the drug in the circulation, the minimal level of effectiveness against immature forms of Schistosoma worm due to less bioavailability.

• Lipid-based nanodelivery systems have the potential to overcome bioavailability and solubility problem faced by bioactive molecules. It can help to bypass multidrug resistance mechanisms.

• It can help to improve the modification and the target rate of PZQ thereby enhancing the absorption of the drug across the biological barriers (the worm tegument).

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 in this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This work was supported by the National Research Foundation (NRF) in South Africa.