Drug delivery for bioactive polysaccharides to improve their drug-like properties and curative efficacy

Abstract

Over several decades, natural polysaccharides (PSs) have been actively exploited for their wide bioactivities. So far, many PS-related reviews have been published; however, none focused on the delivery of bioactive PSs as therapeutic molecules. Herein, we summarized and discussed general pharmacokinetic properties of PSs and drug delivery systems (DDSs) developed for them, together with the challenges and prospects. Overall, most bioactive PSs suffer from undesirable pharmacokinetic attributes, which negatively affect their efficacy and clinical use. Various DDSs therefore have been being utilized to improve the drug-like properties and curative efficacy of bioactive PSs by means of improving oral absorption, controlling the release, enhancing the in vivo retention ability, targeting the delivery, exerting synergistic effects, and so on. Specifically, nano-sized insoluble DDSs were mainly applied to improve the oral absorption and target delivery of PSs, among which liposome was especially suitable for immunoregulatory and/or anti-ischemic PSs due to its synergistic effects in immunoregulation and biomembrane repair. Chemical conjugation of PSs was mainly utilized to improve their oral absorption and/or prolong their blood residence. With formulation flexibility, in situ forming systems alone or in combination with drug conjugation could be used to achieve day(s)-or month(s)-long sustained delivery of PSs per dosing. ARTICLE HISTORY

Preparation of Bioactive Polysaccharide Nanoparticles with Enhanced Radical Scavenging Activity and Antimicrobial Activity

“…Thus, there is growing interest among researchers regarding the benefits of bioactive polysaccharides for human health and other areas. , However, bioactive polysaccharides belong to Class III of the Biopharmaceutics Classification System, which means that the oral absorption of polysaccharides is poor and erratic. Furthermore, because of their hydrophilic and uncharged nature, neutral polysaccharides demonstrate low bioavailability and clearance by the reticuloendothelial system, which indicates their restricted bioactivity in vivo …”

“…Furthermore, because of their hydrophilic and uncharged nature, neutral polysaccharides demonstrate low bioavailability and clearance by the reticuloendothelial system, which indicates their restricted bioactivity in vivo. 7 To improve the bioavailability and bioactivity of functional ingredients, various nanoparticle delivery systems have been developed such as nanomicelle, nanovesicle, nanoliposome, and nanogels. 8−11 Because bioactive polysaccharides provide a wide range of benefits for various biological processes, 12,13 nanocarriers loaded with bioactive polysaccharides have become a prevalent research topic.…”

Polysaccharide‐modified liposomes and their application in cancer research

“…Examples used as carriers include chitosan, alginate, hyaluronic acid (HA), pectin, and cyclodextrin; most of these are used as stabilizers and thickeners (Torres et al, 2019). Their low toxicity and excellent structural stability, biocompatibility, biodegradability, flexibility, non‐immunogenicity, and targetability have stimulated their selection for drug delivery (Kim et al, 2017; Li, Wang, et al, 2017). Their adhesiveness and aforementioned properties can compensate for the shortcomings of liposomes.…”

Potential of Dietary HDAC2i in Breast Cancer Patients Receiving PD-1/PD-L1 Inhibitors

“…Pharmaceuticals and Medicinal Products Some bioactive compounds can be isolated and developed into pharmaceutical drugs to efficiently improve their therapeutic effect [129]. For instance, curcumin, a bioactive compound that has been found to possess multiple biological regulatory functions, has been successfully isolated from plant curcuma aromatica salisb for treating different types of cancer, including BC [130,131].…”