Current approaches in lipid-based nanocarriers for oral drug delivery

Abstract

Graphical abstract Lipid-based nanocarriers have gained much interest as carriers of drugs with poor oral bioavailability because of their remarkable advantages like low toxicity, affordable scale-up manufacture, strong biocompatibility or high drug loading efficiency. The potential of these nanocarriers lies in their ability to improve the gastrointestinal stability, solubility and permeability of their cargo drugs. However, achieving efficient oral drug delivery through lipid-based nanocarriers is a challenging task, since they encounter multiple physicochemical barriers along the gastrointestinal tract, e.g. the gastric acidic content, the intestinal mucus layer or the enzymatic degradation, that they must surmount to reach their target. These limitations may be turned into opportunities through a rational design of lipid-based nanocarriers. For that purpose, this review focuses on the main challenges of the oral route indicating the strategies undertaken for lipid-based nanocarriers in order to overcome them. Understanding their shortcomings and identifying their strengths will determine the future clinical success of lipid-based nanocarriers.

Current Nanocarrier Strategies Improve Vitamin B12 Pharmacokinetics, Ameliorate Patients’ Lives, and Reduce Costs

“…It is an ATP-dependent transporter in the apical surface of enterocytes and is responsible for the efflux of xenobiotics from the cell to the intestinal lumen. To elude Pgp, different strategies have been used including the co-administration of Pgp inhibitors [79].…”

Taking Particle Tracking into Practice by Novel Software and Screening Approach: Case-Study of Oral Lipid Nanocarriers

“…Certainly, R 2 is defined as the variation of the y axis variable (MSD) regarding the x axis variable (τ). In the case of adhesive particles, MSD does not tend to significantly increase along time, so the expected linear fitting is a close to horizontal line and therefore if RSS → TSS , R 2 would be~0 (see Equation (5) and its corresponding explanation). This is especially relevant when designing novel oral drug nanocarriers, as discriminating non-fitting and mucus-stuck particles is required for not overestimating the potential of the nanocarriers.…”

“…Under this scenario, it is mandatory to work with experimental tools that properly analyze the mucodiffusion capacity of each individual particle. Those particles would be the ones that reach the intestinal epithelial cells, an additional biological barrier for the local treatment or for achieving systemic drug levels [5].…”

“…One of the main strengths of PT relies on its capacity to track individual particles. This makes it feasible to identify and characterize heterogeneity in the behavior of the different particles that constitute the sample, which is particularly relevant when designing novel nanocarriers [5,14,15]. The oil/water interface composition of each particle will determine its individual interaction with the intestinal mucus, being possible to classify them into the different populations that form a batch [3,6,9,10].…”

Agricultural Residues as a Source of Bioactive Substances—Waste Management with the Idea of Circular Economy

“…Liposomes are carriers composed of phospholipid layer (one or more) and aqueous core with hydrophilic substances dissolved in it [22]. Due to their high affinity to biological cell membranes and ability to transport substances (encapsulation), liposomes easily penetrate the skin or are absorbed through both the oral mucosal lining and through the intestinal wall, wherein they then release the material contained therein [23]. The most popular techniques used for the preparation of nanoliposomes containing bioactive compounds are extrusion, sonification, and microfluidization [24].…”