Functionalized Polymers for Enhance Oral Bioavailability of Sensitive Molecules

Abstract

Currently, many sensitive molecules have been studied for effective oral administration. These substances are biologically active compounds that mainly suffer early degradation in the gastrointestinal tract (GIT) and physicochemical instability, inactivation and poor solubility and permeability. The sensibility of the biomolecules has limited their oral administration in the body and today is an important research topic to achieve desired effects in medicine field. Under this perspective, various enhancement approaches have been studied as alternatives to increase their oral bioavailability. Some of these strategies include functionalized polymers to provide specific useful benefits as protection to the intestinal tract by preventing its degradation by stomach enzymes, to increase their absorption, permeability, stability, and to make a proper release in the GIT. Due to specific chemical groups, shapes and sizes, morphologies, mechanical properties, and degradation, recent advances in functionalized polymers have opened the door to great possibilities to improve the physicochemical characteristics of these biopharmaceuticals. Today, many biomolecules are found in basic studies, preclinical steps, and others are late stage clinical development. This review summarizes the contribution of functionalized polymers to enhance oral bioavailability of sensitive molecules and their application status in medicine for different diseases. Future trends of these polymers and their possible uses to achieve different formulation goals for oral delivery are also covered in this manuscript.

Nanoparticles and Controlled Delivery for Bioactive Compounds: Outlining Challenges for New “Smart-Foods” for Health

“…Apart from the control of phytochemicals release, nanoparticles also influence the transport of bioactive compounds through enterocytes (by transcellular endocytosis for particles between 20 and 1000 nm), by modulating residence time, transportation efficiency, and pathways, as well as the metabolic reactions undergone by such compounds within endothelial cells. Hence, for instance, chitosan derivatives have been related to mucoadhesive features and their capacity to open tight junctions, improving paracellular transport [ 137 , 138 , 139 ]. Moreover, the nanoparticle’s charge also influences the formation of hydrogen bonds with the mucosal surface, contributing to a momentary retention [ 140 ].…”

Review of recently used techniques and materials to improve the efficiency of orally administered proteins/peptides

“…These hydrophilic molecules require a certain increase in lipophilicity to penetrate the epithelial cell membrane and thus to cross the cells [89]. Chemical alteration on a reactive amino acid like lysine and cysteine or other amino acids will not only give rise to sustained absorption and reduce the amount of drug required to produce the therapeutic effect but will also improve stability as well as decrease immunogenicity [90,91], and based on the size of the conjugated molecule renal ultrafiltration may be decreased due to the increased molecular size of the polypeptide [92]. The nature of the conjugated molecule may be varied in a wide range such as direct modification by the use of acetylation, C-amidation, N-pyroglutamate conjugation, PEGylation (PEG) or glycosylation [93], or via the sugar part of the glycoprotein [13].…”

Amorphous Form of Carvedilol Phosphate—The Case of Divergent Properties

“…Selected polymers can also provide a protective form, limiting the access of water molecules starting the recrystallization process [ 22 , 23 , 24 ]. In addition, many polymers can modify by improving or delaying the release rate of API from the matrix [ 25 , 26 ]. Due to the proper selection of excipients, the stability of the amorphous form, extending its usefulness, can be ensured, and the API availability can be improved [ 27 , 28 ].…”