Polyaminoacid-based nanocarriers: a review of the latest candidates for oral drug delivery

ABSTRACT

Introduction

The oral route is one of the most attractive modalities of drug delivery, providing easy administration and great patient compliance. However, enzymatic degradation and physiological barriers in the gastrointestinal tract are still unsolved obstacles for many drugs. The physico-chemical characteristics of biopharmaceuticals and the resulting low stability and poor penetration capacity across biological barriers represent current challenges that need to be overcome in oral delivery. The use of polyaminoacids and polypeptides, including cell-penetrating peptides as delivery carriers is an attractive strategy to improve the oral bioavailability of therapeutics. These biopolymers are positioned as potential biomaterials due to their low toxicity and their capacity to enhance the stability of biomolecules while increasing their transport through biological barriers.

Areas covered

In this review, we present an update of the current approaches and strategies carried out in the design of nanosystems and penetration-enhancing oral delivery strategies based on polyaminoacids.

Expert opinion

Polyaminoacids and polypeptides are functional and versatile biomaterials which have received significant attention for the design of oral drug delivery platforms. Even though only a few prototypes have yet entered clinical trials, a number of promising strategies can be found in advanced preclinical investigation for the delivery of biopharmaceuticals.

KEYWORDS:

• Arginine
• cell-penetrating peptide
• nanomedicine
• oral delivery
• gastrointestinal barrier
• polyaminoacid

Article highlights

• Specific pharmaceutical strategies are required to maximize the absorption of biomacromolecular therapeutics by non-invasive pathways.

• The presence of polyaminoacid-based products on the market indicates their potential for drug delivery.

• Their low toxicity and capacity to enhance the stability and uptake of biomolecules make PAA attractive as biomaterials for oral drug delivery.

• PAA with high arginine content are particularly promising in terms of their capacity to enhance the intestinal absorption of drugs.

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.

Supplementary material

Supplemental data for this article can be accessed here.

Additional information

Funding

We acknowledge Ministerio de Ciencia e Innovación, Gobierno de España – FEDER (SAF2016-79230-R and ERC2018-092841) and Consellería de Cultura, Educación e Ordenación Universitaria, Xunta de Galicia - FEDER (ED431C 2017/09).