Patrick Knoll
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View article: Thiolated Cellulose: A Dual-Acting Mucoadhesive and Permeation-Enhancing Polymer
Thiolated Cellulose: A Dual-Acting Mucoadhesive and Permeation-Enhancing Polymer Open
This study aims to design an anionic, thiolated cellulose derivative and to evaluate its mucoadhesive and permeation-enhancing properties utilizing enoxaparin as a model drug. 2-Mercaptosuccinic acid-modified cellulose (cellulose-mercaptos…
View article: Development and in vivo evaluation of nanoemulsions for oral delivery of low molecular weight heparin
Development and in vivo evaluation of nanoemulsions for oral delivery of low molecular weight heparin Open
The aim of this study was the development and in vivo evaluation of different types of nanoemulsions for oral delivery of low molecular weight heparin (LMWH). Nanoemulsions (NE) were developed consisting of mainly non-digestible components…
View article: Oral drug delivery: Influence of mucus on cellular interactions and uptake of lipid-based nanocarriers in Caco-2 cells
Oral drug delivery: Influence of mucus on cellular interactions and uptake of lipid-based nanocarriers in Caco-2 cells Open
This study aimed to investigate the impact of the mucus gel barrier on intestinal mucosal uptake of lipid-based nanocarriers (NCs). Zwitterionic- (ZW), polyglycerol- (PG) and polyethylene glycol- (PEG) surfactant-based o/w nanoemulsions we…
View article: Three generations of thiolated cyclodextrins: A direct comparison of their mucus permeating and mucoadhesive properties
Three generations of thiolated cyclodextrins: A direct comparison of their mucus permeating and mucoadhesive properties Open
Three generations of thiolated cyclodextrins (CDs) with different types of thiol ligands have been synthesized to improve mucus interaction. 1st generation of thiolated CDs was synthesized by converting hydroxyl groups into thiols by react…
View article: Thiolated α-cyclodextrin: The likely smallest drug carrier providing enhanced cellular uptake and endosomal escape
Thiolated α-cyclodextrin: The likely smallest drug carrier providing enhanced cellular uptake and endosomal escape Open
This study aimed to evaluate the effect of thiolated α-cyclodextrin (α-CD-SH) on the cellular uptake of its payload. For this purpose, α-CD was thiolated using phosphorous pentasulfide. Thiolated α-CD was characterized by FT-IR and 1H NMR …
View article: PEG vs. zwitterions: How these surface decorations determine cellular uptake of lipid-based nanocarriers
PEG vs. zwitterions: How these surface decorations determine cellular uptake of lipid-based nanocarriers Open
The replacement of PEG surfactants with zwitterionic surfactants is a promising approach to overcome the drawbacks of conventional PEGylated lipid-based NCs regarding intracellular drug delivery.
View article: Lipid-based nanoparticles: Enhanced cellular uptake via surface thiolation
Lipid-based nanoparticles: Enhanced cellular uptake via surface thiolation Open
The aim of this study was to evaluate the uptake mechanism of thiolated nanostructured lipid carriers (NLCs). NLCs were decorated with a short-chain polyoxyethylene(10)stearyl ether with a terminal thiol group (NLCs-PEG10-SH) or without (N…
View article: Biodegradable arginine based steroid-surfactants: Cationic green agents for hydrophobic ion-pairing
Biodegradable arginine based steroid-surfactants: Cationic green agents for hydrophobic ion-pairing Open
The aim of this study was to evaluate the safety and efficacy for hydrophobic ion-pairing of surfactants based on arginine (Arg). The prepared Arg-cholesteryl ester (ACE) and Arg-diosgenyl ester (ADE) were characterized regarding solubilit…
View article: Iminated aminoglycosides in self-emulsifying drug delivery systems: Dual approach to break down the microbial defense
Iminated aminoglycosides in self-emulsifying drug delivery systems: Dual approach to break down the microbial defense Open
Successful synthesis of imine derivatives with almost entirely masked amine groups was confirmed by NMR, FT-IR, TLC and MS. Imines exhibited a marked elevation in logP value of 8 units for kanamycin and 7.7 units for tobramycin. They showe…
View article: Charge-Converting Nanoemulsions as Promising Retinal Drug and Gene Delivery Systems
Charge-Converting Nanoemulsions as Promising Retinal Drug and Gene Delivery Systems Open
Polyphosphate-coated CPP-decorated NEs triggered by ALP could be a promising nanosystem to efficiently deliver drugs and genetic materials to photoreceptor-like cells and other retinal cells for potential treatments of retinal diseases.
View article: Charge converting nanostructured lipid carriers containing a cell-penetrating peptide for enhanced cellular uptake
Charge converting nanostructured lipid carriers containing a cell-penetrating peptide for enhanced cellular uptake Open
All NLCs were obtained in a size range between 146 nm and 152 nm and a polydispersity index of 0.2. Incubation of PP coated PP-R9SA-NLCs with IAP led to a charge conversion from -41.8 mV to 6.4 mV (Δ48.2 mV). After four hours of incubation…
View article: Design of nanostructured lipid carriers and solid lipid nanoparticles for enhanced cellular uptake
Design of nanostructured lipid carriers and solid lipid nanoparticles for enhanced cellular uptake Open
In this study PEG-free and zeta potential changing lipid-based nanocarriers providing enhanced cellular uptake were developed. Nanostructured lipid carriers (NLC), consisting of paraffin wax, caprylic/ capric triglyceride, cetyltrimethylam…
View article: SEDDS-loaded mucoadhesive fiber patches for advanced oromucosal delivery of poorly soluble drugs
SEDDS-loaded mucoadhesive fiber patches for advanced oromucosal delivery of poorly soluble drugs Open
To date, buccal administration of lipophilic drugs is still a major challenge due to their poor solubility in saliva and limited penetration into mucosal tissues. To overcome these limitations, we developed electrospun patches combining th…
View article: Digestion of lipid excipients and lipid-based nanocarriers by pancreatic lipase and pancreatin
Digestion of lipid excipients and lipid-based nanocarriers by pancreatic lipase and pancreatin Open
The digestion behaviour of lipid-based nanocarriers (LNC) has a great impact on their oral drug delivery properties. In this study, various excipients including surfactants, glycerides and waxes, as well as various drug-delivery systems, n…
View article: Emerging technologies to increase gastrointestinal transit times of drug delivery systems
Emerging technologies to increase gastrointestinal transit times of drug delivery systems Open
Apart from already established technologies to increase gastrointestinal transit times, including devices rapidly increasing in size once they have reached the stomach in order to retard the passage through the pylorus, formulations that f…
View article: Synthesis and evaluation of sulfosuccinate-based surfactants as counterions for hydrophobic ion pairing
Synthesis and evaluation of sulfosuccinate-based surfactants as counterions for hydrophobic ion pairing Open
Hydrophobic ion pairing is a promising strategy to raise the lipophilic character of therapeutic peptides and proteins. In past studies, docusate, an all-purpose surfactant with a dialkyl sulfosuccinate structure, showed highest potential …
View article: Thiolated Hydroxypropyl-β-cyclodextrin: A Potential Multifunctional Excipient for Ocular Drug Delivery
Thiolated Hydroxypropyl-β-cyclodextrin: A Potential Multifunctional Excipient for Ocular Drug Delivery Open
The goal of this study was the design and evaluation of a thiolated cyclodextrin providing high drug solubilizing and mucoadhesive properties for ocular drug delivery. Hydroxypropyl-β-cyclodextrin (HP-β-CD) was thiolated via a microwave-as…
View article: In Vitro Investigation of Thiolated Chitosan Derivatives as Mucoadhesive Coating Materials for Solid Lipid Nanoparticles
In Vitro Investigation of Thiolated Chitosan Derivatives as Mucoadhesive Coating Materials for Solid Lipid Nanoparticles Open
In the present study, chitosan (CS) was thiolated by introducing l-cysteine via amide bond formation. Free thiol groups were protected with highly reactive 6-mercaptonicotinic acid (6-MNA) and less-reactive l-cysteine, respectively, via th…
View article: Nanostructured Lipid Carriers (NLCs) for Oral Peptide Drug Delivery: About the Impact of Surface Decoration
Nanostructured Lipid Carriers (NLCs) for Oral Peptide Drug Delivery: About the Impact of Surface Decoration Open
This study was aimed to evaluate the impact of surfactants used for nanostructured lipid carriers (NLCs) to provide enzymatic protection for incorporated peptides. Insulin as a model peptide was ion paired with sodium dodecyl sulfate to im…
View article: Thiolated pectins: In vitro and ex vivo evaluation of three generations of thiomers
Thiolated pectins: In vitro and ex vivo evaluation of three generations of thiomers Open
In recent decades, three generations of thiomers have been developed with the main purpose of obtaining enhanced interactions with mucosal tissues. Therefore, many different types of thiolated ligands have been generated and attached to po…
View article: Thiolated cyclodextrins: Mucoadhesive and permeation enhancing excipients for ocular drug delivery
Thiolated cyclodextrins: Mucoadhesive and permeation enhancing excipients for ocular drug delivery Open
Thiolated β-cyclodextrin (β-CD) has the potential to enhance mucoadhesive and permeation enhancing properties on ocular mucosa. Thiolated β-CD was synthesized via replacement of all primary hydroxyl groups on β-CD backbone by halogen follo…