Combination of SEDDS and Preactivated Thiomer Technology: Incorporation of a Preactivated Thiolated Amphiphilic Polymer into Self-Emulsifying Delivery Systems

Hetényi, Gergely; Griesser, Janine; Nardin, Isabelle; Bernkop‐Schnürch, Andreas

doi:10.1007/s11095-017-2131-5

Cited by 14 publications

(6 citation statements)

References 25 publications

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“…Coating via lipophilic anchors Mucoadhesive [71] formation of thiolate anions representing the reactive species of thiols for oxidation at a minimum or the preparation process is performed under inert conditions. Alternatively, S-protected thiolated surfactants such as S-protected thiolated palmitic acid can be used.…”

Section: Lipid-based Nanoparticles Coating Materials Type Of Surface Coating Function Referencementioning

confidence: 99%

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Thiolated Nanoparticles for Biomedical Applications: Mimicking the Workhorses of Our Body

Hock¹,

Racaniello

Aspinall

et al. 2021

Advanced Science

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Advances in nanotechnology have generated a broad range of nanoparticles (NPs) for numerous biomedical applications. Among the various properties of NPs are functionalities being related to thiol substructures. Numerous biological processes that are mediated by cysteine or cystine subunits of proteins representing the workhorses of the bodies can be transferred to NPs. This review focuses on the interface between thiol chemistry and NPs. Pros and cons of different techniques for thiolation of NPs are discussed. Furthermore, the various functionalities gained by thiolation are highlighted. These include overall bio-and mucoadhesive, cellular uptake enhancing, and permeation enhancing properties. Drugs being either covalently attached to thiolated NPs via disulfide bonds or being entrapped in thiolated polymeric NPs that are stabilized via inter-and intrachain crosslinking can be released at the diseased tissue or in target cells under reducing conditions. Moreover, drugs, targeting ligands, biological analytes, and enzymes bearing thiol substructures can be immobilized on noble metal NPs and quantum dots for therapeutic, theranostic, diagnostic, biosensing, and analytical reasons. Within this review a concise summary and analysis of the current knowledge, future directions, and potential clinical use of thiolated NPs are provided.

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Section: Lipid-based Nanoparticles Coating Materials Type Of Surface Coating Function Referencementioning

confidence: 99%

“…A thiolated acrylate crosspolymer with C10‐30 alkyl side chains, for instance, was used to coat SEDDS. [ 71 ]…”

Section: Thiolation Of Nanoparticlesmentioning

confidence: 99%

Thiolated Nanoparticles for Biomedical Applications: Mimicking the Workhorses of Our Body

Hock¹,

Racaniello

Aspinall

et al. 2021

Advanced Science

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“…Little research has been carried out to attach -SH containing groups to the outside of drug delivery systems in order to cleave the mucin disulphide bridges and completely penetrate the mucus layer. Most research has concentrated on a thiomer strategy [29] using the pH gradient in the small intestine, an acid microclimate, pH 6.0 in the lumen to pH 7.4 close to the epithelial cell surface, which is the same microclimate that powers absorption of peptides. The reactive species generated from thiol groups is S -(thiolate anion) and it is this that can drive disulphide exchange forming disulphide bridges between the nanoparticle and the mucin molecules.…”

Section: Reduction Of Disulphide Bridgesmentioning

confidence: 99%

“…Two delivery systems have been combined by Hetenyi et al [29] (SEDDS and thiomers), in this case a thiolated amphiphilic polymer. This combination was seen to improve permeation and increased residency time on/or close to the mucosa.…”

Section: Safety Concerns Of Mucus Modulating Delivery Systems/agentsmentioning

confidence: 99%

Efficacy and safety concerns over the use of mucus modulating agents for drug delivery using nanoscale systems

Chater

Wilcox

Pearson

2018

Advanced Drug Delivery Reviews

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Drug delivery to the mucus covered mucosae is fraught with difficulties and many different approaches have been developed to permeate the mucus barrier. Generally by modifying the delivery system to avoid interaction with the mucus. These modifications are reviewed here in terms of efficacy and safety. These are particular problems for oral delivery the pharmaceutical industry's favoured route for drug administration. For effective delivery through the gastrointestinal tract a drug must pass through three barriers in sufficient amounts to yield a biological effect. These barriers are the digestive barrier in the lumen, the mucus barrier, and the epithelial barrier. Other approaches involve mucolytic agents added with or prior to the delivery system or agents regulating mucus production and are reviewed here. In terms of safety, a key property of a mucus modulating delivery system is that it must not damage the protective function of the mucus layer.

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“…As CIP has been characterized as biopharmaceutical classification system (BCS class IV) drug (low solubility/low permeability), the development of oral formulations capable of crossing multi-barriers with high penetration, specific distribution and targeted/selective delivery against Salmonella typhi infection remains challenging [ 12 , 13 ]. Driven by these needs, in the present study we develop mucopermeating and HA functionalized SNEDDS for the sustained release as well as for improved solubility and oral bioavailability of CIP [ 14 ]. SNEDDS has recently emerged as an effective and suitable alternative for the controlled and targeted delivery of a wide range of drugs [ 15 , 16 ].…”

Section: Introductionmentioning

confidence: 99%

A Hyaluronic Acid Functionalized Self-Nano-Emulsifying Drug Delivery System (SNEDDS) for Enhancement in Ciprofloxacin Targeted Delivery against Intracellular Infection

et al. 2021

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Ciprofloxacin (CIP), a potent anti-bacterial agent of the fluroquinolone family, shows poor solubility and permeability, thus leading to the development of intracellular pathogens induced multi-drug resistance and biofilms formation. To synergistically improve the biopharmaceutical parameters of CIP, a hyaluronic acid (FDA approved biocompatible polymer) functionalized self-nano emulsifying drug delivery system (HA-CIP-SNEDDS) was designed in the present study. SNEDDS formulations were tested via solubility, droplet size, zeta potential, a polydispersity index, thermodynamic stability, surface morphology, solid-state characterization, drug loading/release, cellular uptake, and biocompatibility. The final (HA-CIP-SNEDDS) formulation exhibited a mean droplet size of 50 nm with the 0.3 poly dispersity index and negative zeta potential (−11.4 mV). HA-based SNEDDS containing CIP showed an improved ability to permeate goat intestinal mucus. After 4 h, CIP-SNEDDS showed a 2-fold and HA-CIP-SNEDDS showed a 4-fold permeation enhancement as compared to the free CIP. Moreover, 80% drug release of HA-CIP-SNEDDS was demonstrated to be superior and sustained for 72 h in comparison to free CIP. However, anti-biofilm activity of HA-CIP-SNEDDS against Salmonella typhi was higher than CIP-SNEDDS and free CIP. HA-CIP-SNEDDS exhibited increased biocompatibility and improved oral pharmacokinetics as compared to free CIP. Taken together, HA-CIP-SNEDDS formulation seems to be a promising agent against Salmonella typhi with a strong targeting potential.

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Combination of SEDDS and Preactivated Thiomer Technology: Incorporation of a Preactivated Thiolated Amphiphilic Polymer into Self-Emulsifying Delivery Systems

Abstract: The novel developed SEDDS with incorporated thiomers might be a promising tool for mucoadhesive oral drug delivery.

Cited by 14 publications

References 25 publications

Thiolated Nanoparticles for Biomedical Applications: Mimicking the Workhorses of Our Body

Thiolated Nanoparticles for Biomedical Applications: Mimicking the Workhorses of Our Body

Efficacy and safety concerns over the use of mucus modulating agents for drug delivery using nanoscale systems

A Hyaluronic Acid Functionalized Self-Nano-Emulsifying Drug Delivery System (SNEDDS) for Enhancement in Ciprofloxacin Targeted Delivery against Intracellular Infection

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