Article
Pharmacology & Pharmacy
Amandeep Kaur, Parveen Kumar, Loveneet Kaur, Rohit Sharma, Preeti Kush
Summary: This study optimized the preparation of Gem-TCh-NPs nanoparticles, which showed a small particle size, high encapsulation efficiency, and biphasic release pattern. The formulation exhibited superior mucoadhesion, permeation, and cytotoxicity compared to native Gem. In vivo pharmacokinetic analysis indicated that Gem-TCh-NPs could be a promising formulation for enhanced oral therapy.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2021)
Review
Polymer Science
Syed Sarim Imam, Sultan Alshehri, Mohammed M. Ghoneim, Ameeduzzafar Zafar, Omar Awad Alsaidan, Nabil K. Alruwaili, Sadaf Jamal Gilani, Md. Rizwanullah
Summary: The review discusses the loading of phytochemicals in biodegradable and biocompatible nanoparticles based on chitosan for improved bioavailability and bioactivity. Chitosan's properties such as mucoadhesiveness, non-toxicity, stability in harsh gastrointestinal conditions, and enhanced intestinal permeability make it suitable for oral delivery of phytochemicals.
Article
Engineering, Biomedical
Soheil Haddadzadegan, Patrick Knoll, Richard Wibel, Gergely Kali, Andreas Bernkop-Schnuerch
Summary: This study compared the mucus permeating and mucoadhesive properties of three generations of thiolated cyclodextrins. Thiolated CDs were protected with different compounds, leading to improved viscosity, mucus diffusion, and mucoadhesion. The results suggest that S-protection of thiolated CDs can enhance their mucus penetrating and mucoadhesive properties.
ACTA BIOMATERIALIA
(2023)
Review
Chemistry, Multidisciplinary
Carmen Milian-Guimera, Reece Mccabe, Lasse Hojlund Eklund Thamdrup, Mahdi Ghavami, Anja Boisen
Summary: Oral dosage forms are the preferred solution for systemic treatment and prevention of diseases, but traditional forms face challenges. Research on novel formulation strategies for oral drug delivery has bloomed in the last decade to overcome these challenges, with approaches based on drug release and mucus interfacing showing promising results in personalized medicine and improved bioavailability.
JOURNAL OF CONTROLLED RELEASE
(2023)
Article
Biochemistry & Molecular Biology
Mariacristina Gagliardi, Sara Chiarugi, Chiara De Cesari, Giulia Di Gregorio, Alessandra Diodati, Laura Baroncelli, Marco Cecchini, Ilaria Tonazzini
Summary: The study presents a method to obtain stable and cytocompatible crosslinked chitosan nanoparticles for intranasal drug delivery. The nanoparticles showed a stable size and surface charge, and exhibited good cytocompatibility in vitro. This synthetic system has potential as a drug carrier for intranasal delivery.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Chemistry, Multidisciplinary
Nathalie Hock, Giuseppe Francesco Racaniello, Sam Aspinall, Nunzio Denora, Vitaliy V. Khutoryanskiy, Andreas Bernkop-Schnuerch
Summary: This review discusses the interface between thiol chemistry and nanoparticles, highlighting the various functionalities gained by thiolation. These include enhanced bio- and mucoadhesive properties, improved cellular uptake, and permeation enhancement. Various applications such as drug delivery, targeted therapy, and diagnostics can benefit from thiolated nanoparticles.
Review
Chemistry, Multidisciplinary
Simona Summonte, Giuseppe Francesco Racaniello, Angela Lopedota, Nunzio Denora, Andreas Bernkop-Schnuerch
Summary: Thiomers, such as thiolated hyaluronic acid and chitosan, are widely studied for their high reactivity in hydrogel synthesis. They exhibit in situ gelling properties and can undergo various click reactions, making them versatile materials for tissue engineering, regenerative medicine, and drug delivery.
JOURNAL OF CONTROLLED RELEASE
(2021)
Article
Biochemistry & Molecular Biology
Renas Rzgar Jalal, Twana Mohammed M. Ways, Mahmoud H. Abu Elella, Diyar Ahmed Hassan, Vitaliy V. Khutoryanskiy
Summary: Mucoadhesive nanoparticles based on methacrylated chitosan (MeCHI) were designed and compared with unmodified chitosan nanoparticles for the delivery of ciprofloxacin. The MeCHI nanoparticles showed smaller particle size, lower polydispersity index, higher encapsulation efficiency, and sustained drug release compared to their chitosan counterpart. The mucoadhesion study also demonstrated that the ciprofloxacin-loaded MeCHI nanoparticles had better retention on the mucosal surface.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Article
Biochemistry & Molecular Biology
Theodore Ebenezer Leonard, Alvaro Filbert Liko, Marsia Gustiananda, Agus Budiawan Naro Putra, Ario Betha Juanssilfero, Pietradewi Hartrianti
Summary: Mucoadhesive drug delivery systems (DDS) can enhance localized drug distribution and retention, promoting safer chemotherapy for colorectal cancer (CRC). Carbohydrate polymers, such as pectin (P) and chitosan (CS), are potential biomaterials for CRC-targeted DDS due to their gelling ability, mucoadhesive property, colonic digestibility, and anticancer activity. Thiolation can augment polymer mucoadhesion, while the P-CS polyelectrolyte complex improves structural stability. TP-CS composites show superior mucoadhesive properties compared to single- or dual-crosslinked counterparts, making them promising biomaterials for CRC-targeted DDS.
INTERNATIONAL JOURNAL OF BIOLOGICAL MACROMOLECULES
(2023)
Review
Pharmacology & Pharmacy
Kwadwo Mfoafo, Rahul Mittal, Adrien Eshraghi, Yadollah Omidi, Hossein Omidian
Summary: Thiolated polymers, known as thiomers, have unique mucoadhesive properties and can form strong covalent bonds with cysteine-rich subdomains of mucus glycoproteins. This makes them suitable for drug delivery systems (DDSs) for dry mucosal surface diseases. Thiomers offer higher adhesion and retention time compared to non-thiolated polymers, leading to increased bioavailability and reduced patient noncompliance. They can also inhibit enzymes, increase permeability, and protect protein and peptide drugs from digestive enzymes. Thiolated polymers have potential applications in adhesion, controlled drug release, and tissue engineering.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Article
Pharmacology & Pharmacy
Ayca Gungor Ak, Inci Turan, Hale Sayan Ozacmak, Aysegul Karatas
Summary: This study aimed to enhance the oral bioavailability and gastrointestinal stability of berberine chloride (BER) by preparing chitosan nanoparticles using an ionotropic gelation method. The BER-loaded chitosan nanoparticles showed an encapsulation efficiency of 31.5%, a zeta potential of 41.6 mV, a particle size of 406 nm, and a polydispersity index of 0.462. Stability studies demonstrated that the nanoparticles improved the stability of BER in simulated gastrointestinal fluids.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Review
Biochemistry & Molecular Biology
Vanessa Falchetti Lopes, Camila Nascimento Giongo, Lais de Almeida Campos, Wolf-Rainer Abraham, Rubiana Mara Mainardes, Najeh Maissar Khalil
Summary: The development of biodegradable nanoparticles, particularly chitosan-based systems, has shown promising results in improving the biological transport of chemical compounds. These nanoencapsulated systems enhance the properties of loaded drugs, including permeation, stability, and bioactivity, offering potential benefits for targeted drug delivery.
CURRENT MEDICINAL CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Richard Wibel, Doris E. Braun, Laurenz Haemmerle, Arne M. Joergensen, Patrick Knoll, Willi Salvenmoser, Christian Steinbring, Andreas Bernkop-Schnuerch
Summary: In this study, thiolated chitosan was used as a coating material for solid lipid nanoparticles, with the protection of thiol groups playing a key role in their interaction with mucosa. Different coating materials showed varying effects on mucus interaction and diffusion behavior on intestinal mucosa.
Article
Chemistry, Applied
Zheng Jin, Gaowei Hu, Kai Zhao
Summary: This study demonstrated that the synthesized M-N-2-HACC/N-CMCS nanoparticles showed high efficiency in mucosal delivery by utilizing the interaction with mucosal sites for drug release and delivery.
CARBOHYDRATE POLYMERS
(2022)
Article
Instruments & Instrumentation
Giovanna Rassu, Antonella Obinu, Carla Serri, Sandra Piras, Antonio Carta, Luca Ferraro, Elisabetta Gavini, Paolo Giunchedi, Alessandro Dalpiaz
Summary: In this study, PLGA nanoparticles (SS13NP) and solid lipid nanoparticles (SS13SLN) loaded with SS13 were prepared. SS13NP showed higher drug bioavailability and shorter time to reach peak concentration in oral administration compared with SS13SLN. These results confirm that the chemical composition of nanoparticles significantly affects the in vivo fate of a BCS IV drug. Moreover, PLGA nanoparticles appear more efficient and rapid than SLN in allowing drug absorption and transport to systemic circulation.
DRUG DELIVERY AND TRANSLATIONAL RESEARCH
(2023)
Review
Pharmacology & Pharmacy
Soheil Haddadzadegan, Farid Dorkoosh, Andreas Bernkop-Schnuerch
Summary: The oral administration of therapeutic peptides and proteins faces various barriers, which can be overcome by using lipid-based nanocarriers. These nanocarriers enhance the lipophilic character of the drugs and protect them from enzymatic degradation. They can penetrate mucus and absorption membranes, enabling systemic delivery of the therapeutic molecules. Lipid-based nanocarriers show promising stability and delivery efficacy.
ADVANCED DRUG DELIVERY REVIEWS
(2022)
Article
Chemistry, Physical
Zeynep Burcu Akkus-Dagdeviren, Andrea Fuerst, Julian David Friedl, Martina Tribus, Andreas Bernkop-Schnuerch
Summary: This study investigates the combined usage of Layer-by-Layer coating and alkaline phosphatase-responsive charge reversal strategies in colloidal drug delivery systems. The findings show that this combination improves cellular internalisation and decreases cytotoxic effects.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2023)
Article
Biochemistry & Molecular Biology
Ahmad Saleh, Zeynep Burcu Akkus-Dagdeviren, Soheil Haddadzadegan, Richard Wibel, Andreas Bernkop-Schnuerch
Summary: The study developed peptide antibiotic-polyphosphatenanoparticles for targeted drug release on the intestinal epithelium. These nanoparticles showed protection against enzymatic degradation, superior mucus permeating properties, and the ability to release drug when triggered by intestinal alkaline phosphatase. The findings suggest that the PMB-PP NPs are promising delivery systems for protecting cationic peptide antibiotics, overcoming the mucus barrier, and providing direct drug release.
Article
Pharmacology & Pharmacy
Victor Claus, Helen Spleis, Christoph Federer, Katrin Zoeller, Richard Wibel, Flavia Laffleur, Camille Dumont, Philippe Caisse, Andreas Bernkop-Schnuerch
Summary: In this study, the lipophilicity of insulin glargine was increased through hydrophobic ion pairing with sodium octadecyl sulfate, enabling its incorporation into self-emulsifying drug delivery systems (SEDDS). Two SEDDS formulations were developed and loaded with the insulin glargine-HIP complex. The results showed that the bioavailability of the complexed insulin glargine in the SEDDS formulations was significantly increased after oral administration in rats.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Nanoscience & Nanotechnology
Bao Le-Vinh, Christian Steinbring, Nguyet-Minh Nguyen Le, Barbara Matuszczak, Andreas Bernkop-Schnurch
Summary: Chitosan and its derivatives with high cell adhesion properties were designed and tested for their suitability as scaffold materials in tissue engineering. The attachment of a thiol group to chitosan significantly improved cell adhesion, with higher modification levels leading to better results. The resulting chitosan-based cryogels showed promise for 3D cell culture and tissue engineering.
ACS APPLIED MATERIALS & INTERFACES
(2023)
Review
Chemistry, Multidisciplinary
Sobia Noreen, Andreas Bernkop-Schnuerch
Summary: Thiolation of poly- and oligosaccharides introduces various favorable properties for tissue engineering and wound healing, including stable 3D networks, enhanced cell adhesion and signaling, and controlled release of active ingredients.
ADVANCED FUNCTIONAL MATERIALS
(2023)
Article
Biochemistry & Molecular Biology
Gergely Kali, Bengi Ozkahraman, Flavia Laffleur, Patrick Knoll, Richard Wibel, Katrin Zoller, Andreas Bernkop-Schnurch
Summary: This study aimed to design and evaluate an anionic, thiolated cellulose derivative for its mucoadhesive and permeation-enhancing properties using enoxaparin as a model drug. The thiolated cellulose exhibited enhanced mucoadhesion on porcine intestinal mucosa and improved permeation in Caco-2 cell monolayer. In vivo studies in rats showed significantly higher oral bioavailability compared to the aqueous solution of the drug.
Article
Pharmacology & Pharmacy
Richard Wibel, Florina Veider, Barbara Hoyer, Joseph Chamieh, Andreas Bernkop-Schnuerch
Summary: Organic solvents have a substantial impact on the solubility and precipitation rate of drugs in self-emulsifying drug delivery systems. This impact is particularly significant for moderately lipophilic drugs.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Victor Claus, Matthias Sandmeier, Nathalie Hock, Helen Spleis, Sera Lindner, Monika Kalb, Andreas Bernkop-Schnuerch
Summary: In this study, the lipophilicity of model proteins was increased by combining various surfactants with insulin, bovine serum albumin, and horseradish peroxidase. The key factors responsible for complex formation were identified. The formed complexes were stable in simulated gastrointestinal fluids and could be incorporated into self-emulsifying drug delivery systems.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Zeynep Burcu Akkus-Dagdeviren, Sema Arisoy, Julian David Friedl, Andrea Fuerst, Ahmad Saleh, Andreas Bernkop-Schnuerch
Summary: The aim of this study was to develop enzyme-activated charge-reversal lipid nanoparticles (LNPs) as novel gene delivery systems. The researchers successfully anchored a transfection promoter on the surfaces of LNPs to achieve high encapsulation and efficient gene delivery. The experiment results showed that the enzyme-triggered charge reversal of LNPs resulted in significantly increased transfection efficiency in human alveolar epithelial cells.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2023)
Article
Pharmacology & Pharmacy
Nathalie Hock, Dennis To, Eva Sanchez Armengol, Simona Summonte, Anna Seybold, Christoph Federer, Andreas Bernkop-Schnuerch
Summary: The aim of this study was to develop biodegradable polyphosphate nanoparticles as long-acting drug delivery systems by utilizing ubiquitarian alkaline phosphatase. The nanoparticles were prepared and characterized, showing good stability and release characteristics. The results also demonstrated their biocompatibility and lack of toxicity. These findings open up new opportunities in parenteral drug delivery.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2023)
Review
Chemistry, Multidisciplinary
Florina Veider, Eva Sanchez Armengol, Andreas Bernkop-Schnuerch
Summary: The past two decades have seen significant progress in the development of surface charge-reversible nanoparticles for drug delivery and diagnosis. These nanoparticles can change their surface charge from negative to positive at the target site, thereby improving drug delivery and diagnostic agent sensitivity. They have also shown potential in overcoming biofilms and delivering antibiotics directly to cell membranes of microorganisms. This review highlights the latest design and emerging applications of charge-reversible nanoparticles in drug delivery and diagnosis.
Article
Engineering, Biomedical
Arne Matteo Joergensen, Christian Steinbring, Daniel Stengel, Dennis To, Pascal Schmid, Andreas Bernkop-Schnuerch
Summary: This study developed self-emulsifying drug delivery systems containing dry reverse micelles (SEDDS-dRMsPMB) loaded with the model peptide drug polymyxin B (PMB) using anionic (AOT), cationic (DODAB), amphoteric (SL), or non-ionic (P85) surfactants. These systems showed high payload, efficient cellular uptake, and maintained antimicrobial activity, suggesting a potential game-changing strategy for oral peptide drug delivery.
ADVANCED HEALTHCARE MATERIALS
(2023)
Article
Materials Science, Biomaterials
Dennis To, Gergely Kali, Soheil Haddadzadegan, Arne Matteo Joergensen, Katharina Nigl, Fabrizio Ricci, Andreas Bernkop-Schnuerch
Summary: Nanoemulsions with enhanced gastro-intestinal retention time can be achieved by incorporating thiolated surfactants into their surface. Two generations of thiolated surfactants were synthesized and characterized, and their incorporation into nanoemulsions improved the mucoadhesiveness. S-protected thiol derivatives showed the highest mucoadhesive properties among all tested surfactants.
ACS BIOMATERIALS SCIENCE & ENGINEERING
(2023)
Article
Chemistry, Physical
Katrin Zoeller, Anna Karlegger, Martyna Truszkowska, Daniel Stengel, Andreas Bernkop-Schnuerch
Summary: This study investigates the cellular uptake of hydrophobic complexes via nanocarriers using hydrophobic ion pairs (HIPs) formed between two fluorescent components. The results show that HIPs increase the lipophilicity of the model drugs and incorporating HIPs into nanoemulsions (NE) further enhances cellular uptake. HIPs serve as a powerful tool to visualize the cellular distribution of hydrophobic complexes and study their cellular uptake.
JOURNAL OF COLLOID AND INTERFACE SCIENCE
(2024)
