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John D. Smart - One of the best experts on this subject based on the ideXlab platform.
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Buccal drug delivery
Expert Opinion on Drug Delivery, 2005Co-Authors: John D. SmartAbstract:Buccal formulations have been developed to allow prolonged localised therapy and enhanced systemic delivery. The buccal mucosa, however, while avoiding first-pass effects, is a formidable barrier to drug absorption, especially for biopharmaceutical products (proteins and oligonucleotides) arising from the recent advances in genomics and proteomics. The buccal route is typically used for extended drug delivery, so formulations that can be attached to the buccal mucosa are favoured. The Bioadhesive polymers used in buccal drug delivery to retain a formulation are typically hydrophilic macro-molecules containing numerous hydrogen bonding groups. Newer second-generation Bioadhesives have been developed and these include modified or new polymers that allow enhanced adhesion and/or drug delivery, in addition to site-specific ligands such as lectins. Over the last 20 years a wide range of formulations has been developed for buccal drug delivery (tablet, patch, liquids and semisolids) but comparatively few have f...
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Recent developments in the use of Bioadhesive systems for delivery of drugs to the oral cavity.
Critical reviews in therapeutic drug carrier systems, 2004Co-Authors: John D. SmartAbstract:The delivery of therapeutic agents to, or via, the oral cavity is limited by the efficient removal mechanisms that exist in this area. Bioadhesive formulations have been developed to allow prolonged localized therapy and enhanced systemic delivery. The oral mucosa however, while avoiding first-pass effects, is a formidable barrier to drug absorption, especially for "biopharmaceutical" products arising from the recent innovations in genomics and proteomics. Bioadhesive polymers are typically hydrophilic macromolecules containing numerous hydrogen-bonding groups. Second-generation Bioadhesives include modified or new polymers that allow enhanced adhesion and/or drug delivery, along with site-specific ligands such as lectins. Over the last 20 years, a range of Bioadhesive formulations have been developed for the oral cavity, but only comparatively few have found their way onto the market. This review will consider some recent developments in the use of Bioadhesive buccal systems, notably the development of new polymers, advanced delivery systems, and the exploitation of the multifunctional properties of some Bioadhesives.
Edith Mathiowitz - One of the best experts on this subject based on the ideXlab platform.
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Time-dependent mucoadhesion of conjugated Bioadhesive polymers
Colloids and Surfaces B: Biointerfaces, 2018Co-Authors: Kenneth M. Estrellas, Bryan Laulicht, Alexis Mancini, Joshua Reineke, Stacia Furtado, Mark Fiecas, Aharon Azagury, Edith MathiowitzAbstract:Abstract The time-dependent Bioadhesive performance of various polymers was evaluated using a texture analyzer apparatus and freshly excised rat small intestinal tissue. A series of novel Bioadhesive polymers were prepared by conjugating L-phenylalanine, L-tyrosine, and L-DOPA to either a low molecular weight poly (butadiene-maleic anhydride) or a high molecular weight poly (ethylene-maleic anhydride). Bioadhesive force was characterized as a function of time relative to polycarbophil, a slightly cross-linked poly (acrylic acid)-derivative, revealing different fracture strengths and tensile work for each of the six backbone-side chain conjugations that were studied. While polycarbophil showed a rapid and significant loss of bioadhesion over the testing period, the newly developed synthetic polymers were able to maintain their Bioadhesive performance over the course of 91 min with the overall magnitude of bioadhesion corresponding to the hydrogen bonding potential of the associated side chains. These results highlight the potential of these polymers for use in the development of more effective Bioadhesive oral drug delivery systems.
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Are in vivo gastric Bioadhesive forces accurately reflected by in vitro experiments
Journal of Controlled Release, 2008Co-Authors: Bryan Laulicht, Peter Cheifetz, Anubhav Tripathi, Edith MathiowitzAbstract:Bioadhesive polymers have been used in oral drug delivery to prolong the contact of dosage forms with the site of drug absorption. Previous investigators have coated oral dosage forms in polymers that demonstrated Bioadhesive properties during in vitro screens in efforts to prolong the gastric residence of drugs absorbed only in the stomach and proximal duodenum without clinical success. To further investigate the Bioadhesive properties of the gastric environment, an in vivo quantitative Bioadhesive fracture strength test was developed. Bioadhesive and non-Bioadhesive bioerodible polymers with potential for use in oral drug delivery were tested for Bioadhesive fracture strength both in vivo and in vitro. Surprisingly, no statistically significant difference was found between the Bioadhesive fracture strength of fast eroding polyanhydride and slowly eroding hydrophobic polymers in vivo. When the same polymers were tested in vitro, the expected difference was observed. The lack of IVIVC (in vitro/in vivo correlation) among Bioadhesive fracture strengths reflects the clinical finding that polymers that produced strong Bioadhesive forces in vitro may not achieve prolonged gastric retention in vivo due to differences between the in vitro screening conditions and the in vivo Bioadhesive environment.
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Bioadhesive Drug Delivery Systems: Fundamentals, Novel Approaches, and Development - Bioadhesive Drug Delivery Systems : Fundamentals, Novel Approaches, and Development
Drugs and the Pharmaceutical Sciences, 1999Co-Authors: Edith Mathiowitz, Donald E. Chickering, Claus-michael LehrAbstract:Fundamentals of Bioadhesion Definitions, Mechanisms, and Theories of Bioadhesion Donald E. Chickering III and Edith Mathiowitz The Role of Water Movement and Polymer Hydration in Mucoadhesion John D. Smart A Rheological Approach to Explain the Mucoadhesive Behavior of Polymer Hydrogels Carla Marcella Caramella, Silvia Rossi, and Maria Cristina Bonferoni Functional Histology of Epithelia Relevant for Drug Delivery: Respiratory Tract, Digestive Tract, Eye, Skin, and Vagina Udo Schumacher and Dietlind Schumacher Biochemical and Functional Aspects of Mucus and Mucin-Type Glycoproteins Barry James Campbell Methods of Evaluating Bioadhesive Interactions Adaptation of a Microbalance to Measure Bioadhesive Properties of Microspheres Donald E. Chickering III, Camilla A. Santos, and Edith Mathiowitz Novel Magnetic Technique to Measure Bioadhesion Benjamin A. Hertzog and Edith Mathiowitz Principles of Skin Adhesion and Methods for Measuring Adhesion of Transdermal Systems Michael Horstmann, Walter Muller, and Bodo Asmussen Force Microscopy of Cells to Measure Bioadhesion E. zur Muhlen, P. Koschinski, S. Gehring, Robert Ros, Louis Tiefenhauer, Eleonore Haltner, Claus-Michael Lehr, Uwe Hartmann, Falk Schwesinger, and A. Pluckthun Direct Measurement of Molecular-Level Forces and Adhesion in Biological Systems James Schneider and Matthew Tirrell A Centrifugation Method for Measurement of Two-Dimensional Binding Characteristics of Receptor-Ligand Interaction Cheng Zhu, James W. Piper, and Robert A. Swerlick Novel Concepts and Strategies for Bioadhesive Drug Delivery Systems Multifunctional Polymers for the Peroral Delivery of Peptide Drugs Henrik L. Luessen, J. Coos Verhoef, A. (Bert) G. de Boer, H. E. Junginger, Bas J. de Leeuw, Gerrit Borchard, and Claus-Michael Lehr Chitosan and Chitosan Derivatives as Absorption Enhancers for Peptide Drugs Across Mucosal Epithelia A. F. Kotze, Henrik L. Luessen, M. Thanou, J. Coos Verhoef, A. (Bert) G. de Boer, H. E. Junginger, and Claus-Michael Lehr Plant Lectins for Oral Drug Delivery to Different Parts of the Gastrointestinal Tract Arpad Pusztai, Susan Bardocz, and Stanley W. B. Ewen Bacterial Invasion Factors and Lectins as Second-Generation Bioadhesives James H. Easson, Eleonore Haltner, Claus-Michael Lehr, and Dieter Jahn Novel PEG-Containing Acrylate Copolymers with Improved Mucoadhesive Properties Amir H. Shojaei and Xiaoling Li Bioadhesive, Bioerodible Polymers for Increased Intestinal Uptake Gerardo P. Carino, Jules S. Jacob, C. James Chen, Camilla A. Santos, Benjamin A. Hertzog, and Edith Mathiowitz Development Issues of Bioadhesive Drug Delivery Systems: Products and Clinical Trials Novel Formulation Approaches to Oral Mucoadhesive Drug Delivery Systems Yohko Akiyama and Naoki Nagahara Bioadhesive Formulations for Nasal Peptide Delivery Lisbeth Illum Development of Bioadhesive Buccal Patches Jian-Hwa Guo and Karsten Cremer Vaginal Delivery of Calcitonin by Hyaluronic Acid Formulations Julie L. Richardson and Trevor I. Armstrong Ocular Bioadhesive Drug Delivery Systems Marco Fabrizio Saettone, Susi Burgalassi, and Patrizia Chetoni Bioadhesive Preparations as Topical Dosage Forms Yoshiharu Machida and Tsuneji Nagai
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Bioadhesive drug delivery systems fundamentals novel approaches and development
1999Co-Authors: Edith Mathiowitz, Donald E. Chickering, Claus-michael LehrAbstract:Fundamentals of Bioadhesion Definitions, Mechanisms, and Theories of Bioadhesion Donald E. Chickering III and Edith Mathiowitz The Role of Water Movement and Polymer Hydration in Mucoadhesion John D. Smart A Rheological Approach to Explain the Mucoadhesive Behavior of Polymer Hydrogels Carla Marcella Caramella, Silvia Rossi, and Maria Cristina Bonferoni Functional Histology of Epithelia Relevant for Drug Delivery: Respiratory Tract, Digestive Tract, Eye, Skin, and Vagina Udo Schumacher and Dietlind Schumacher Biochemical and Functional Aspects of Mucus and Mucin-Type Glycoproteins Barry James Campbell Methods of Evaluating Bioadhesive Interactions Adaptation of a Microbalance to Measure Bioadhesive Properties of Microspheres Donald E. Chickering III, Camilla A. Santos, and Edith Mathiowitz Novel Magnetic Technique to Measure Bioadhesion Benjamin A. Hertzog and Edith Mathiowitz Principles of Skin Adhesion and Methods for Measuring Adhesion of Transdermal Systems Michael Horstmann, Walter Muller, and Bodo Asmussen Force Microscopy of Cells to Measure Bioadhesion E. zur Muhlen, P. Koschinski, S. Gehring, Robert Ros, Louis Tiefenhauer, Eleonore Haltner, Claus-Michael Lehr, Uwe Hartmann, Falk Schwesinger, and A. Pluckthun Direct Measurement of Molecular-Level Forces and Adhesion in Biological Systems James Schneider and Matthew Tirrell A Centrifugation Method for Measurement of Two-Dimensional Binding Characteristics of Receptor-Ligand Interaction Cheng Zhu, James W. Piper, and Robert A. Swerlick Novel Concepts and Strategies for Bioadhesive Drug Delivery Systems Multifunctional Polymers for the Peroral Delivery of Peptide Drugs Henrik L. Luessen, J. Coos Verhoef, A. (Bert) G. de Boer, H. E. Junginger, Bas J. de Leeuw, Gerrit Borchard, and Claus-Michael Lehr Chitosan and Chitosan Derivatives as Absorption Enhancers for Peptide Drugs Across Mucosal Epithelia A. F. Kotze, Henrik L. Luessen, M. Thanou, J. Coos Verhoef, A. (Bert) G. de Boer, H. E. Junginger, and Claus-Michael Lehr Plant Lectins for Oral Drug Delivery to Different Parts of the Gastrointestinal Tract Arpad Pusztai, Susan Bardocz, and Stanley W. B. Ewen Bacterial Invasion Factors and Lectins as Second-Generation Bioadhesives James H. Easson, Eleonore Haltner, Claus-Michael Lehr, and Dieter Jahn Novel PEG-Containing Acrylate Copolymers with Improved Mucoadhesive Properties Amir H. Shojaei and Xiaoling Li Bioadhesive, Bioerodible Polymers for Increased Intestinal Uptake Gerardo P. Carino, Jules S. Jacob, C. James Chen, Camilla A. Santos, Benjamin A. Hertzog, and Edith Mathiowitz Development Issues of Bioadhesive Drug Delivery Systems: Products and Clinical Trials Novel Formulation Approaches to Oral Mucoadhesive Drug Delivery Systems Yohko Akiyama and Naoki Nagahara Bioadhesive Formulations for Nasal Peptide Delivery Lisbeth Illum Development of Bioadhesive Buccal Patches Jian-Hwa Guo and Karsten Cremer Vaginal Delivery of Calcitonin by Hyaluronic Acid Formulations Julie L. Richardson and Trevor I. Armstrong Ocular Bioadhesive Drug Delivery Systems Marco Fabrizio Saettone, Susi Burgalassi, and Patrizia Chetoni Bioadhesive Preparations as Topical Dosage Forms Yoshiharu Machida and Tsuneji Nagai
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A microtensiometer for the analysis of Bioadhesive microspheres
Biomedical Instrumentation & Technology, 1995Co-Authors: Donald E. Chickering, W. P. Harris, Edith MathiowitzAbstract:: Bioadhesive polymer microspheres are potential vehicles for the delivery of bioactive agents to mucosal tissues. Bioadhesive delivery devices could improve drug absorption, enhance bioavailability, and increase patient compliance by minimizing dosing regimens. Identification of Bioadhesive materials is the first phase in developing Bioadhesive drug delivery systems. Additionally, quantification and analysis of the Bioadhesive event are essential to successful development of a new generation of adhesive delivery systems. A unique, microbalance-based instrument was developed to analyze Bioadhesive forces between polymer microspheres and mucosal tissue segments. A contact angle analyzer, with a custom-made physiologic tissue chamber, was linked to a computer via the serial port. Software was used to modify the microbalance operation to behave as a microtensiometer with a sensitivity of 0.1 microN. After mounting a microsphere and tissue segment in the balance and adjusting the experimental settings, the instrument performs a tensile experiment and automatically determines the following parameters: compressive deformation, peak compressive load, compressive work, yield point, deformation to yield, returned work, peak tensile load, deformation to peak tensile load, fracture strength, deformation to failure, and tensile work. Using this device the authors identified several Bioadhesive materials ideally suited for orally-delivered, controlled-release systems. GI-transit studies in rats showed strong correlation between increased GI-residence time and strong Bioadhesive interactions.
Hangon Choi - One of the best experts on this subject based on the ideXlab platform.
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effect of sodium chloride on the gelation temperature gel strength and Bioadhesive force of poloxamer gels containing diclofenac sodium
International Journal of Pharmaceutics, 2001Co-Authors: Chul Soon Yong, Jin Suck Choi, Qizhe Quan, Jongdal Rhee, Philsoo Oh, Hangon ChoiAbstract:Liquid suppository systems composed of poloxamers and Bioadhesive polymers were easy to administer to the anus and mucoadhesive to the rectal tissues without leakage after the dose. However, a liquid suppository system containing diclofenac sodium could not be developed using Bioadhesive polymers, since the drug was precipitated in this preparation. To develop a liquid suppository system using sodium chloride instead of Bioadhesive polymers, the physicochemical properties such as gelation temperature, gel strength and Bioadhesive force of various formulations composed of diclofenac sodium, poloxamers and sodium chloride were investigated. The mixtures of P 407 (15%) and P 188 (15-20%) existed as a liquid at room temperature, but gelled at physiological temperature. Diclofenac sodium significantly increased the gelation temperature and weakened the gel strength and Bioadhesive force, while sodium chloride did the opposite. Furthermore, the poloxamer gels with less than 1.0% of sodium chloride, in which the drug was not precipitated, were inserted into the rectum of rabbits without difficulty and leakage, and retained in the rectum of rats for at least 6 h. Our results suggested that a thermosensitive liquid suppository system with sodium chloride and poloxamers was a more physically stable and convenient rectal dosage form for diclofenac sodium.
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Physicochemical characterization and evaluation of buccal adhesive tablets containing omeprazole.
Drug Development and Industrial Pharmacy, 2001Co-Authors: Chul Soon Yong, Jongdal Rhee, Chong-kook Kim, Jae-hee Jung, Hangon ChoiAbstract:The objective of this study was to develop an effective omeprazole buccal adhesive tablet with excellent Bioadhesive force and good drug stability in human saliva. The omeprazole buccal adhesive tablets were prepared with various Bioadhesive polymers, alkali materials, and croscarmellose sodium. Their physicochemical properties, such as Bioadhesive force and drug stability in human saliva, were investigated. The release and bioavailability of omeprazole delivered by the buccal adhesive tablets were studied. As Bioadhesive additives for the omeprazole tablet, a mixture of sodium alginate and hydroxypropylmethylcellulose (HPMC) was selected. The omeprazole tablets prepared with Bioadhesive polymers alone had Bioadhesive forces suitable for a buccal adhesive tablet, but the stability of omeprazole in human saliva was not satisfactory. Among alkali materials, only magnesium oxide could be an alkali stabilizer for omeprazole buccal adhesive tablets due to its strong waterproofing effect. Croscarmellose sodium ...
Fabiana Volpe Zanutto - One of the best experts on this subject based on the ideXlab platform.
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semisynthetic derivative of artemisia annua loaded transdermal Bioadhesive for the treatment of uncomplicated malaria caused by plasmodium falciparum in children
Journal of Pharmaceutical Sciences, 2019Co-Authors: Uno Fonsecasantos, Fabiana Volpe Zanutto, Emma Mcaliste, Marcelo Marucci Pereira Tangerina, Tais Helena Costa Salles, Ilza Maria Oliveira Souza, Andi Isibe, Wagne Vilegas, Marlus ChorilliAbstract:Abstract According to the most recent World Health Organization statistics, malaria infected approximately 219 million people in 2017, with an estimate of 435,000 deaths (World Health Organization, 2018). Communities isolated from cities are the most deprived of access to the necessary hospital facilities. Herein we report the development of a transdermal Bioadhesive containing artemether (ART), an alternative, potentially lifesaving, treatment regimen for malaria in low-resource settings. Bioadhesives were prepared from an aqueous blend of hydroxyethylcellulose (4.5% w/w), ART, propoxylated-ethoxylated-cetyl-alcohol, polysorbate 80, propyleneglycol, glycerine, mineral oil, and oleic acid. In this study, the average pore size of Bioadhesive 5.5b was 52.6 ± 15.31 μm. Differential scanning calorimetry and thermogravimetric analyses confirm the thermal stability of ART Bioadhesives at room temperature. Tensile tests indicated good mechanical properties for Bioadhesive 5.5b, when compared to 5.5a, where 5.5b showed elastic modulus 0.19 MPa, elongation at break 204%, tensile stress 0.31 MPa, tensile strength at break 0.23 MPa. Bioadhesion assays suggested that formulations containing surfactants had higher detachment forces. Permeation studies demonstrated that the best outcome was achieved with a Bioadhesive containing 25 mg ART (5.5b) that after 24 h released 6971 ± 125 μg, which represents approximately 28% of drug permeation. Data reported presents a promising candidate for a new antimalarial transdermal formulation.
Jian Yang - One of the best experts on this subject based on the ideXlab platform.
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development of tannin inspired antimicrobial Bioadhesives
Acta Biomaterialia, 2018Co-Authors: Xili Lu, Juange Cheng, Qiyao Li, Guoying Qian, Oliver Mrowczynski, Elias Rizk, Jian YangAbstract:Abstract Tissue adhesives play an important role in surgery to close wounds, seal tissues, and stop bleeding, but existing adhesives are costly, cytotoxic, or bond weakly to tissue. Inspired by the water-resistant adhesion of plant-derived tannins, we herein report a new family of Bioadhesives derived from a facile, one-step Michael addition of tannic acid and gelatin under oxidizing conditions and crosslinked by silver nitrate. The oxidized polyphenol groups of tannic acid enable wet tissue adhesion through catecholamine-like chemistry, while both tannic acid and silver nanoparticles reduced from silver nitrate provide antimicrobial sources inherent within the polymeric network. These tannin-inspired gelatin Bioadhesives are low-cost and readily scalable and eliminate the concerns of potential neurological effect brought by mussel-inspired strategy due to the inclusion of dopamine; variations in gelatin source (fish, bovine, or porcine) and tannic acid feeding ratios resulted in tunable gelation times (36 s–8 min), controllable degradation (up to 100% degradation within a month), considerable wet tissue adhesion strengths (up to 3.7 times to that of fibrin glue), excellent cytocompatibility, as well as antibacterial and antifungal properties. The innate properties of tannic acid as a natural phenolic crosslinker, molecular glue, and antimicrobial agent warrant a unique and significant approach to Bioadhesive design. Statement of Significance This manuscript describes the development of a new family of tannin-inspired antimicrobial Bioadhesives derived from a facile, one-step Michael addition of tannic acid and gelatin under oxidizing conditions and crosslinked by silver nitrate. Our strategy is new and can be easily extended to other polymer systems, low-cost and readily scalable, and eliminate the concerns of potential neurological effect brought by mussel-inspired strategy due to the inclusion of dopamine. The tannin-inspired gelatin Bioadhesives hold great promise for a number of applications in wound closure, tissue sealant, hemostasis, antimicrobial and cell/drug delivery, and would be interested to the readers from biomaterials, tissue engineering, and drug delivery area.
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synthesis and characterization of anti bacterial and anti fungal citrate based mussel inspired Bioadhesives
Biomaterials, 2016Co-Authors: Jianqing Hu, Ethan Gerhard, Merisa Nisic, Guoying Qian, Siyang Zheng, Dingying Shan, Jian YangAbstract:Bacterial and fungal infections in the use of surgical devices and medical implants remain a major concern. Traditional Bioadhesives fail to incorporate anti-microbial properties, necessitating additional anti-microbial drug injection. Herein, by the introduction of the clinically used and inexpensive anti-fungal agent, 10-undecylenic acid (UA), into our recently developed injectable citrate-based mussel-inspired Bioadhesives (iCMBAs), a new family of anti-bacterial and anti-fungal iCMBAs (AbAf iCs) was developed. AbAf iCs not only showed strong wet tissue adhesion strength, but also exhibited excellent in vitro cyto-compatibility, fast degradation, and strong initial and considerable long-term anti-bacterial and anti-fungal ability. For the first time, the biocompatibility and anti-microbial ability of sodium metaperiodate (PI), an oxidant used as a cross-linking initiator in the AbAf iCs system, was also thoroughly investigated. Our results suggest that the PI-based Bioadhesives showed better anti-microbial properties compared to the unstable silver-based Bioadhesive materials. In conclusion, AbAf iCs family can serve as excellent anti-bacterial and anti-fungal Bioadhesive candidates for tissue/wound closure, wound dressing, and bone regeneration, especially when bacterial or fungal infections are a major concern.
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design strategies and applications of tissue Bioadhesives
Macromolecular Bioscience, 2013Co-Authors: Mohammad Reza Mehdizadeh, Jian YangAbstract:In the past two decades tissue adhesives and sealants have revolutionized bleeding control and wound healing. This paper focuses on existing tissue adhesive design, their structure, functioning mechanism, and their pros and cons in wound management. It also includes the latest advances in the development of new tissue adhesives as well as the emerging applications in regenerative medicine. We expect that this paper will provide insightful discussion on tissue Bioadhesive design and lead to innovations for the development of the next generation of tissue Bioadhesives and their related biomedical applications.