Intraoral Drug Delivery: Highly Thiolated κ-Carrageenan as Mucoadhesive Excipient.

Aim: This study aims to design a novel thiolated κ-carrageenan (κ-CA-SH) and evaluate its potential as an excipient for the design of mucoadhesive drug delivery systems.

Methods: Native κ-carrageenan (κ-CA) was thiolated with phosphorous pentasulfide in sulfolane and characterized via H NMR, FTIR, as well as Ellman's test. Cytotoxicity was assessed via resazurin assay.

Thiolated cyclodextrins: A comparative study of their mucoadhesive properties.

Aim: The aim of this study was the comparison of the mucoadhesive properties of nonionic, negatively, and positively charged thiolated cyclodextrins (CDs), including α-, β-, and γ-CDs of low and high degree of thiolation.

Methods: Native α-, β-, and γ-CDs were thiolated with phosphorous pentasulfide in sulfolane (CD-SH) (i), via reductive amination with cysteamine after oxidative ring opening (CD-Cya) (ii), and via esterification with mercaptosuccinic acid (CD-MSA) (iii). These thiolated CDs were characterized via H NMR and Ellman's test.

Betaine-modified hydroxyethyl cellulose (HEC): A biodegradable mucoadhesive polysaccharide exhibiting quaternary ammonium substructures.

The aim of this study was to improve the mucoadhesive properties of hydroxyethyl cellulose (HEC) via the covalent attachment of betaine. Synthesis was carried out through esterification of HEC utilizing N-chlorobetainyl chloride. Betaine-modified HEC was characterized via FTIR and NMR analyses, ester quantification and zeta potential measurements.

Phosphate decorated lipid-based nanocarriers providing a prolonged mucosal residence time.

The aim of this study was to develop phosphate decorated lipid-based nanocarriers including self-emulsifying drug delivery systems (SEDDS), solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) to extend their mucosal residence time. All nanocarriers contained tetradecyltrimethylammonium bromide (TTAB) and polyoxyethylene (9) nonylphenol monophosphate ester (PNPP) for surface decoration. Zeta potential, cytotoxicity, charge conversion and phosphate release studies using isolated intestinal alkaline phosphatase (IAP) and Caco-2 cells were performed.

Imine bond formation as a tool for incorporation of amikacin in self-emulsifying drug delivery systems (SEDDS).

Aim: The aim was to develop a self-emulsifying drug delivery system (SEDDS) for amikacin via imine bond formation with hydrophobic aldehydes.

Methods: Trans-2, cis-6-nonadienal, trans-cinnamaldehyde, citral and benzaldehyde were conjugated to amikacin at pH 8.5.

Imine bond formation: A novel concept to incorporate peptide drugs in self-emulsifying drug delivery systems (SEDDS).

Hypothesis: Because of its hydrophilic character the peptide drug Polymyxin B (PMB) cannot be incorporated in lipophilic nanocarrier systems such as self-emulsifying drug delivery systems (SEDDS) for oral administration. Due to the formation of imine conjugates between the primary amino groups of PMB and the carbonyl group of cinnamaldehyde, however, drug lipophilicity might be sufficiently raised for incorporation in SEDDS.

Methods: Imine bonds were formed between the primary amino groups of PMB and the carbonyl group of cinnamaldehyde.

Improved Intestinal Mucus Permeation of Vancomycin via Incorporation Into Nanocarrier Containing Papain-Palmitate.

The aim of this study was to improve intestinal mucus permeation of a peptide antibiotic via incorporation into papain-palmitate-modified self-emulsifying drug delivery systems (SEDDS) as nanocarrier. Vancomycin as a peptide antibiotic was lipidized by hydrophobic ion pair formation using sodium bis-2-ethylhexyl-sulphosuccinate before incorporation in SEDDS comprising Capmul MCM, propylenglycol, and Kolliphor EL (2:1:2). As mucolytic agent, 0.

Oral self-emulsifying delivery systems for systemic administration of therapeutic proteins: science fiction?

The aim of this study was to develop self-emulsifying drug delivery systems (SEDDS) for oral delivery of therapeutic proteins through hydrophobic ion pairing. Horseradish peroxidase (HRP), a model protein, was ion paired with sodium docusate to increase its hydrophobicity. The formed enzyme - surfactant complex was incorporated into SEDDS, followed by permeation studies across Caco-2 cell monolayer and freshly excised rat intestine.

Trypsin decorated self-emulsifying drug delivery systems (SEDDS): Key to enhanced mucus permeation.

It was the aim of this study to prepare trypsin decorated mucus permeating self-emulsifying drug delivery systems (SEDDS). Lipophilicity of enzyme was increased by hydrophobic ion pairing (HIP) with the anionic surfactants sodium dodecyl sulfate (SDS), sodium taurocholate (ST) and sodium deoxycholate (SDO) to facilitate its incorporation in SEDDS. Blank SEDDS and trypsin decorated SEDDS were characterized regarding droplet size, polydispersity index (PI), zeta potential and proteolytic activity using Nα-benzoyl-l-arginine ethyl ester (BAEE) assay.

Mucus permeating self-emulsifying drug delivery systems (SEDDS): About the impact of mucolytic enzymes.

This study aimed to improve the mucus permeating properties of self-emulsifying drug delivery systems (SEDDS) by anchoring lipidized bromelain, papain and trypsin using palmitoyl chloride. SEDDS containing enzyme-palmitate conjugates were characterized regarding droplet size and zeta potential. Their mucus permeating properties were evaluated by Transwell diffusion and rotating tube method using fluorescein diacetate (FDA) as marker.

Improved mucoadhesive properties of self-nanoemulsifying drug delivery systems (SNEDDS) by introducing acyl chitosan.

This study was aimed to improve the mucoadhesive properties of SNEDDS by the incorporation of acyl chitosan including octanoyl chitosan (OC), lauroyl chitosan (LC) and palmitoyl chitosan (PC). SNEDDS and acyl chitosan SNEDDS were characterized regarding droplet size and zeta potential. Their mucoadhesivity on porcine intestinal mucosa was evaluated by falling liquid film technique using Sudan Red G as marker.

Cell-penetrating self-nanoemulsifying drug delivery systems (SNEDDS) for oral gene delivery.

Objective: The aim of study was to investigate whether cell-penetrating peptides could amplify cellular uptake of plasmid DNA (pDNA) loaded self-nanoemulsifying drug delivery systems (SNEDDS) by mucosal epithelial cells, thereby enhancing transfection efficiency.

Methods: HIV-1 Tat peptide-oleoyl conjugate (TAT-OL) was synthesized through amide bond formation between HIV-1 Tat-protein 49-57 (TAT) and oleoyl-chloride (OL). SNEDDS formulation contained 29.