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Article ; Online: Pegylated oleic acid: A promising amphiphilic polymer for nano-antibiotic delivery.

Omolo, Calvin A / Kalhapure, Rahul S / Jadhav, Mahantesh / Rambharose, Sanjeev / Mocktar, Chunderika / Ndesendo, Valence M K / Govender, Thirumala

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V

2017 Volume 112, Page(s) 96–108

Abstract: Vancomycin (VM), a last resort to control methicillin-resistant S. aureus (MRSA) infections, is on the verge of becoming ineffective. Novel nano delivery systems of VM have the potential to combat MRSA. The search for novel materials for nanoantibiotic ... ...

Abstract	Vancomycin (VM), a last resort to control methicillin-resistant S. aureus (MRSA) infections, is on the verge of becoming ineffective. Novel nano delivery systems of VM have the potential to combat MRSA. The search for novel materials for nanoantibiotic development is therefore an active research area. In this study, oleic acid (OA) was coupled with monomethoxy polyethylene glycol (mPEG) to obtain a novel bio-safe amphiphilic polymer, mPEG-OA. The critical micelle concentration of mPEG-OA, was found to be 4.5×10
MeSH term(s)	Animals ; Anti-Bacterial Agents/administration & dosage ; Anti-Bacterial Agents/pharmacology ; Calorimetry, Differential Scanning ; Cell Line, Tumor ; Drug Screening Assays, Antitumor ; Humans ; Methicillin-Resistant Staphylococcus aureus/drug effects ; Mice ; Microbial Sensitivity Tests ; Microscopy, Electron, Transmission ; Nanotechnology ; Oleic Acid/chemistry ; Polyethylene Glycols/chemistry ; Polymers/chemistry ; Vancomycin/administration & dosage ; Vancomycin/pharmacology
Chemical Substances	Anti-Bacterial Agents ; Polymers ; Oleic Acid (2UMI9U37CP) ; Polyethylene Glycols (30IQX730WE) ; Vancomycin (6Q205EH1VU)
Language	English
Publishing date	2017-03
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	1065368-5
ISSN	1873-3441 ; 0939-6411
ISSN (online)	1873-3441
ISSN	0939-6411
DOI	10.1016/j.ejpb.2016.11.022
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Article ; Online: Synthesis of an oleic acid based pH-responsive lipid and its application in nanodelivery of vancomycin.

Mhule, Danford / Kalhapure, Rahul S / Jadhav, Mahantesh / Omolo, Calvin A / Rambharose, Sanjeev / Mocktar, Chunderika / Singh, Sanil / Waddad, Ayman Y / Ndesendo, Valence M K / Govender, Thirumala

International journal of pharmaceutics

2018 Volume 550, Issue 1-2, Page(s) 149–159

Abstract: Stimuli-responsive nano-drug delivery systems can optimize antibiotic delivery to infection sites. Identifying novel lipids for pH responsive delivery to acidic conditions of infection sites will enhance the performance of nano-drug delivery systems. The ...

Abstract	Stimuli-responsive nano-drug delivery systems can optimize antibiotic delivery to infection sites. Identifying novel lipids for pH responsive delivery to acidic conditions of infection sites will enhance the performance of nano-drug delivery systems. The aim of the present investigation was to synthesize and characterize a biosafe novel pH-responsive lipid for vancomycin delivery to acidic conditions of infection sites. A pH-responsive solid lipid, N-(2-morpholinoethyl) oleamide (NMEO) was synthesized and used to prepare vancomycin (VCM)-loaded solid lipid nanoparticles (VCM_NMEO SLNs). The particle size (PS), polydispersity index (PDI), zeta potential (ZP) and entrapment efficiency (EE) of the formulation were 302.8 ± 0.12 nm, 0.23 ± 0.03, -6.27 ± 0.017 mV and 81.18 ± 0.57% respectively. The study revealed that drug release and antibacterial activity were significantly greater at pH 6.0 than at pH 7.4, while the in silico studies exposed the molecular mechanisms for improved stability and drug release. Moreover, the reduction of MRSA load was 4.14 times greater (p < 0.05) in the skin of VCM_NMEO SLNs treated mice than that of bare VCM treated specimens. Thus, this study confirmed that NMEO can successfully be used to formulate pH-responsive SLNs with potential to enhance the treatment of bacterial infections.
MeSH term(s)	Animals ; Anti-Bacterial Agents/administration & dosage ; Cell Line ; Drug Carriers ; Drug Liberation ; Humans ; Hydrogen-Ion Concentration ; Lipids ; Mice, Inbred BALB C ; Nanoparticles ; Oleic Acid ; Particle Size ; Skin/drug effects ; Vancomycin/administration & dosage
Chemical Substances	Anti-Bacterial Agents ; Drug Carriers ; Lipids ; Oleic Acid (2UMI9U37CP) ; Vancomycin (6Q205EH1VU)
Language	English
Publishing date	2018-08-17
Publishing country	Netherlands
Document type	Journal Article
ZDB-ID	428962-6
ISSN	1873-3476 ; 0378-5173
ISSN (online)	1873-3476
ISSN	0378-5173
DOI	10.1016/j.ijpharm.2018.08.025
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Zs.A 1409: Show issues

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Article ; Online: Diverse approaches for the enhancement of oral drug bioavailability.

Fasinu, Pius / Pillay, Viness / Ndesendo, Valence M K / du Toit, Lisa C / Choonara, Yahya E

Biopharmaceutics & drug disposition

2011 Volume 32, Issue 4, Page(s) 185–209

Abstract: In conscious and co-operating patients, oral drug delivery remains the preferable route of drug administration. However, not all drugs possess the desirable physicochemical and pharmacokinetic properties which favor oral administration mainly due to poor ...

Abstract	In conscious and co-operating patients, oral drug delivery remains the preferable route of drug administration. However, not all drugs possess the desirable physicochemical and pharmacokinetic properties which favor oral administration mainly due to poor bioavailability. This has in some cases led to the choice of other routes of administration, which may compromise the convenience and increase the risk of non-compliance. Poor bioavailability has necessitated the administration of higher than normally required oral doses which often leads to economic wastages, risk of toxicity, erratic and unpredictable responses. The challenge over the years has been to design techniques that will allow oral administration of most drugs, irrespective of their properties, to achieve a therapeutic systemic availability. This will be a worthy achievement since over 90% of therapeutic compounds are known to possess oral bioavailability limitations. In this review, an attempt has been made to explore various approaches that have been used in recent years to improve oral drug bioavailability, including physical and chemical means. This review strives to provide a comprehensive overview of advances made over the past 10 years (2000-2010) in the improvement of the oral bioavailability of drugs. Briefly, the design of prodrugs to bypass metabolism or to enhance solubility as well as modification of formulation techniques such as the use of additives, permeation enhancers, solubilizers, emulsifiers and non-aqueous vehicles have been discussed. Arising approaches, such as formulation modification techniques; novel drug delivery systems, which exploit the gastrointestinal regionality of drugs, and include the pharmaceutical application of nanotechnology as an emerging area in drug delivery; inhibition of efflux pumps; and inhibition of presystemic metabolism have been more extensively addressed. This critical review sought to assess each method aimed at enhancing the oral bioavailability of drugs in terms of the purpose, scientific basis, limitations, commercial application, as well as the areas in which current research efforts are being focused and should be focused in the future.
MeSH term(s)	Administration, Oral ; Biological Availability ; Drug Compounding/methods ; Drug Compounding/trends ; Drug Delivery Systems/methods ; Humans ; Pharmaceutical Preparations/administration & dosage ; Pharmaceutical Preparations/chemistry ; Prodrugs/administration & dosage ; Prodrugs/chemistry ; Prodrugs/pharmacokinetics ; Solubility
Chemical Substances	Pharmaceutical Preparations ; Prodrugs
Language	English
Publishing date	2011-05
Publishing country	England
Document type	Journal Article ; Review
ZDB-ID	603014-2
ISSN	1099-081X ; 0142-2782
ISSN (online)	1099-081X
ISSN	0142-2782
DOI	10.1002/bdd.750
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Article ; Online: A novel multilayered multidisk oral tablet for chronotherapeutic drug delivery.

Khan, Zaheeda / Choonara, Yahya E / Kumar, Pradeep / du Toit, Lisa C / Ndesendo, Valence M K / Pillay, Viness

BioMed research international

2013 Volume 2013, Page(s) 569470

Abstract: A Multilayered Multidisk Tablet (MLMDT) comprising two drug-loaded disks enveloped by three drug-free barrier layers was developed for use in chronotherapeutic disorders, employing two model drugs, theophylline and diltiazem HCl. The MLMDT was designed ... ...

Abstract	A Multilayered Multidisk Tablet (MLMDT) comprising two drug-loaded disks enveloped by three drug-free barrier layers was developed for use in chronotherapeutic disorders, employing two model drugs, theophylline and diltiazem HCl. The MLMDT was designed to achieve two pulses of drug release separated by a lag phase. The polymer disk comprised hydroxyethylcellulose (HEC) and ethylcellulose (EC) granulated using an aqueous dispersion of EC. The polymeric barrier layers constituted a combination of pectin/Avicel (PBL) (1st barrier layer) and hydroxypropylmethylcellulose (HPMC) (HBL1 and HBL2) as the 2nd and 3rd barrier layers, respectively. Sodium bicarbonate was incorporated into the diltiazem-containing formulation for delayed drug release. Erosion and swelling studies confirmed the manner in which the drug was released with theophylline formulations exhibiting a maximum swelling of 97% and diltiazem containing formulations with a maximum swelling of 119%. FTIR spectra displayed no interactions between drugs and polymers. Molecular mechanics simulations were undertaken to predict the possible orientation of the polymer morphologies most likely affecting the MLMDT performance. The MLMDT provided two pulses of drug release, separated by a lag phase, and additionally it displayed desirable friability, hardness, and uniformity of mass indicating a stable formulation that may be a desirable candidate for chronotherapeutic drug delivery.
MeSH term(s)	Cellulose/administration & dosage ; Cellulose/analogs & derivatives ; Cellulose/chemistry ; Diltiazem/administration & dosage ; Drug Chronotherapy ; Drug Delivery Systems ; Ethylene Glycols/administration & dosage ; Ethylene Glycols/chemistry ; Humans ; Hypromellose Derivatives ; Kinetics ; Methylcellulose/analogs & derivatives ; Methylcellulose/chemistry ; Pectins/chemistry ; Polymers/administration & dosage ; Polymers/chemistry ; Tablets/administration & dosage
Chemical Substances	Ethylene Glycols ; Polymers ; Tablets ; Hypromellose Derivatives (3NXW29V3WO) ; Pectins (89NA02M4RX) ; Cellulose (9004-34-6) ; hydroxyethylcellulose (9004-62-0) ; Methylcellulose (9004-67-5) ; Diltiazem (EE92BBP03H) ; 2-ethoxyethanol (IDK7C2HS09)
Language	English
Publishing date	2013-08-20
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2698540-8
ISSN	2314-6141 ; 2314-6133
ISSN (online)	2314-6141
ISSN	2314-6133
DOI	10.1155/2013/569470
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Article ; Online: A review of polymeric refabrication techniques to modify polymer properties for biomedical and drug delivery applications.

Pillay, Viness / Seedat, Ahmed / Choonara, Yahya E / du Toit, Lisa C / Kumar, Pradeep / Ndesendo, Valence M K

AAPS PharmSciTech

2013 Volume 14, Issue 2, Page(s) 692–711

Abstract: Polymers are extensively used in the pharmaceutical and medical field because of their unique and phenomenal properties that they display. They are capable of demonstrating drug delivery properties that are smart and novel, such properties that are not ... ...

Abstract	Polymers are extensively used in the pharmaceutical and medical field because of their unique and phenomenal properties that they display. They are capable of demonstrating drug delivery properties that are smart and novel, such properties that are not achievable by employing the conventional excipients. Appropriately, polymeric refabrication remains at the forefront of process technology development in an endeavor to produce more useful pharmaceutical and medical products because of the multitudes of smart properties that can be attained through the alteration of polymers. Small alterations to a polymer by either addition, subtraction, self-reaction, or cross reaction with other entities have the capability of generating polymers with properties that are at the level to enable the creation of novel pharmaceutical and medical products. Properties such as stimuli-responsiveness, site targeting, and chronotherapeutics are no longer figures of imaginations but have become a reality through utilizing processes of polymer refabrication. This article has sought to review the different techniques that have been employed in polymeric refabrication to produce superior products in the pharmaceutical and medical disciplines. Techniques such as grafting, blending, interpenetrating polymers networks, and synthesis of polymer complexes will be viewed from a pharmaceutical and medical perspective along with their synthetic process required to attain these products. In addition to this, each process will be evaluated according to its salient features, impeding features, and the role they play in improving current medical devices and procedures.
MeSH term(s)	Animals ; Biocompatible Materials ; Chemistry, Pharmaceutical ; Delayed-Action Preparations ; Drug Carriers ; Humans ; Molecular Structure ; Pharmaceutical Preparations/chemistry ; Polymers/chemistry ; Polymers/radiation effects ; Solubility ; Structure-Activity Relationship ; Technology, Pharmaceutical/methods ; Temperature ; Tissue Engineering/methods
Chemical Substances	Biocompatible Materials ; Delayed-Action Preparations ; Drug Carriers ; Pharmaceutical Preparations ; Polymers
Language	English
Publishing date	2013-03-30
Publishing country	United States
Document type	Journal Article ; Review
ZDB-ID	2052070-0
ISSN	1530-9932 ; 1530-9932
ISSN (online)	1530-9932
ISSN	1530-9932
DOI	10.1208/s12249-013-9955-z
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Article ; Online: Integration of biosensors and drug delivery technologies for early detection and chronic management of illness.

Ngoepe, Mpho / Choonara, Yahya E / Tyagi, Charu / Tomar, Lomas Kumar / du Toit, Lisa C / Kumar, Pradeep / Ndesendo, Valence M K / Pillay, Viness

Sensors (Basel, Switzerland)

2013 Volume 13, Issue 6, Page(s) 7680–7713

Abstract: Recent advances in biosensor design and sensing efficacy need to be amalgamated with research in responsive drug delivery systems for building superior health or illness regimes and ensuring good patient compliance. A variety of illnesses require ... ...

Abstract	Recent advances in biosensor design and sensing efficacy need to be amalgamated with research in responsive drug delivery systems for building superior health or illness regimes and ensuring good patient compliance. A variety of illnesses require continuous monitoring in order to have efficient illness intervention. Physicochemical changes in the body can signify the occurrence of an illness before it manifests. Even with the usage of sensors that allow diagnosis and prognosis of the illness, medical intervention still has its downfalls. Late detection of illness can reduce the efficacy of therapeutics. Furthermore, the conventional modes of treatment can cause side-effects such as tissue damage (chemotherapy and rhabdomyolysis) and induce other forms of illness (hepatotoxicity). The use of drug delivery systems enables the lowering of side-effects with subsequent improvement in patient compliance. Chronic illnesses require continuous monitoring and medical intervention for efficient treatment to be achieved. Therefore, designing a responsive system that will reciprocate to the physicochemical changes may offer superior therapeutic activity. In this respect, integration of biosensors and drug delivery is a proficient approach and requires designing an implantable system that has a closed loop system. This offers regulation of the changes by means of releasing a therapeutic agent whenever illness biomarkers prevail. Proper selection of biomarkers is vital as this is key for diagnosis and a stimulation factor for responsive drug delivery. By detecting an illness before it manifests by means of biomarkers levels, therapeutic dosing would relate to the severity of such changes. In this review various biosensors and drug delivery systems are discussed in order to assess the challenges and future perspectives of integrating biosensors and drug delivery systems for detection and management of chronic illness.
MeSH term(s)	Biomarkers/analysis ; Biomarkers/blood ; Biomarkers/urine ; Biosensing Techniques/instrumentation ; Biosensing Techniques/methods ; Blood Glucose/analysis ; Cardiovascular Diseases/diagnosis ; Cholesterol/blood ; Chronic Disease ; Diabetes Mellitus/diagnosis ; Drug Delivery Systems/instrumentation ; Drug Delivery Systems/methods ; Early Diagnosis ; Electrochemical Techniques/instrumentation ; Electrochemical Techniques/methods ; Humans
Chemical Substances	Biomarkers ; Blood Glucose ; Cholesterol (97C5T2UQ7J)
Language	English
Publishing date	2013-06-14
Publishing country	Switzerland
Document type	Journal Article ; Research Support, Non-U.S. Gov't ; Review
ZDB-ID	2052857-7
ISSN	1424-8220 ; 1424-8220
ISSN (online)	1424-8220
ISSN	1424-8220
DOI	10.3390/s130607680
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Article ; Online: Design of an interpolyelectrolyte gastroretentive matrix for the site-specific zero-order delivery of levodopa in Parkinson's disease.

Ngwuluka, Ndidi C / Choonara, Yahya E / Modi, Girish / du Toit, Lisa C / Kumar, Pradeep / Ndesendo, Valence M K / Pillay, Viness

AAPS PharmSciTech

2013 Volume 14, Issue 2, Page(s) 605–619

Abstract: This study focused on developing a gastroretentive drug delivery system employing a triple-mechanism interpolyelectrolyte complex (IPEC) matrix comprising high density, swelling, and bioadhesiveness for the enhanced site-specific zero-order delivery of ... ...

Abstract	This study focused on developing a gastroretentive drug delivery system employing a triple-mechanism interpolyelectrolyte complex (IPEC) matrix comprising high density, swelling, and bioadhesiveness for the enhanced site-specific zero-order delivery of levodopa in Parkinson's disease. An IPEC was synthesized and directly compressed into a levodopa-loaded matrix employing pharmaceutical technology and evaluated with respect to its physicochemical and physicomechanical properties and in vitro drug release. The IPEC-based matrix displayed superior mechanical properties in terms of matrix hardness (34-39 N/mm) and matrix resilience (44-47%) when different normality's of solvent and blending ratios were employed. Fourier transform infrared spectroscopy confirmed the formation of the IPEC. The formulations exhibited pH and density dependence with desirable gastro-adhesion with Peak Force of Adhesion ranging between 0.15 and 0.21 N/mm, densities from 1.43 to 1.54 g/cm(3) and swellability values of 177-234%. The IPEC-based gastroretentive matrix was capable of providing site-specific levodopa release with zero-order kinetics corroborated by detailed mathematical and molecular modeling studies. Overall, results from this study have shown that the IPEC-based matrix has the potential to improve the absorption and subsequent bioavailability of narrow absorption window drugs, such as levodopa with constant and sustained drug delivery.
MeSH term(s)	Adhesiveness ; Animals ; Antiparkinson Agents/chemistry ; Antiparkinson Agents/therapeutic use ; Carboxymethylcellulose Sodium/chemistry ; Chemistry, Pharmaceutical ; Delayed-Action Preparations ; Drug Carriers ; Galactans/chemistry ; Gastric Mucosa/metabolism ; Hardness ; Humans ; Hydrogen-Ion Concentration ; Kinetics ; Levodopa/chemistry ; Levodopa/therapeutic use ; Mannans/chemistry ; Methacrylates/chemistry ; Models, Chemical ; Models, Molecular ; Molecular Conformation ; Parkinson Disease/drug therapy ; Plant Gums/chemistry ; Polymers/chemistry ; Polymers/metabolism ; Solubility ; Solvents/chemistry ; Spectroscopy, Fourier Transform Infrared ; Swine ; Technology, Pharmaceutical/methods
Chemical Substances	Antiparkinson Agents ; Delayed-Action Preparations ; Drug Carriers ; Galactans ; Mannans ; Methacrylates ; Plant Gums ; Polymers ; Solvents ; Levodopa (46627O600J) ; Carboxymethylcellulose Sodium (K679OBS311) ; locust bean gum (V4716MY704)
Language	English
Publishing date	2013-03-15
Publishing country	United States
Document type	Journal Article
ZDB-ID	2052070-0
ISSN	1530-9932 ; 1530-9932
ISSN (online)	1530-9932
ISSN	1530-9932
DOI	10.1208/s12249-013-9945-1
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Article ; Online: A novel pH-dependant and double crosslinked polymethacrylate-based polysphere matrix for enteric delivery of isoniazid.

Cooppan, Shivaan / Choonara, Yahya E / du Toit, Lisa C / Ndesendo, Valence M K / Kumar, Pradeep / Pillay, Viness

Pharmaceutical development and technology

2013 Volume 18, Issue 5, Page(s) 1066–1077

Abstract: This study aimed at developing double crosslinked isoniazid (INH)-loaded polymethyl-methacrylate-ethylcellulose (PMMA-EC) polyspheres for rate-controlled enteric drug delivery. A PMMA solution was manipulated with the addition of EC to produce ... ...

Abstract	This study aimed at developing double crosslinked isoniazid (INH)-loaded polymethyl-methacrylate-ethylcellulose (PMMA-EC) polyspheres for rate-controlled enteric drug delivery. A PMMA solution was manipulated with the addition of EC to produce polyspheres by drop-wise extrusion into a primary crosslinking solution of AlCl3 (25% w/v), before adding a second crosslinking solution of either 30% w/v BaCl2 (polysphere Batch A) or 30% w/v MgCl2 (polysphere Batch B). The polyspheres were then subjected to FTIR spectroscopic analysis, in vitro drug release studies, drug entrapment efficiency (DEE) determination as well as surface area and porositometric investigations. Molecular Mechanics (MM) simulations elucidated the interaction between the cations and the PMMA-EC combination. FTIR spectra revealed an affinity of PMMA for Ba(2+), Mg(2+) and Al(3+). SEM showed smooth robust polyspheres ranging between 4-6 mm. Porositometric analysis established that polysphere Batch A had larger pores (315.314 Åabs) than Batch B (234.603 Åabs). Drug release profiles from polysphere Batch A displayed burst release with 50% INH released within 2 h (N = 3) that was attributable to the larger ionic radius of the second crosslinker Ba(2+) compared Mg(2+) which was employed for polysphere Batch B. The latter produced polyspheres with superior control in INH release (<25% within 2 h) (N = 3) and a higher DEE with minimal pore formation. The experimental findings were well corroborated by the MM simulations.
MeSH term(s)	Cellulose/analogs & derivatives ; Cellulose/chemistry ; Cross-Linking Reagents/chemistry ; Drug Delivery Systems/methods ; Hydrogen-Ion Concentration ; Isoniazid/chemistry ; Polymethacrylic Acids/chemistry ; Porosity ; Surface Properties
Chemical Substances	Cross-Linking Reagents ; Polymethacrylic Acids ; polymethacrylic acid (25087-26-7) ; ethyl cellulose (7Z8S9VYZ4B) ; Cellulose (9004-34-6) ; Isoniazid (V83O1VOZ8L)
Language	English
Publishing date	2013-09
Publishing country	England
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1331774-x
ISSN	1097-9867 ; 1083-7450
ISSN (online)	1097-9867
ISSN	1083-7450
DOI	10.3109/10837450.2012.685654
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Zs.A 5043: Show issues

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Article ; Online: Exploration of the biomacromolecular interactions of an interpenetrating proteo-saccharide hydrogel network at the mucosal interface.

Mashingaidze, Felix / Choonara, Yahya E / Kumar, Pradeep / du Toit, Lisa C / Maharaj, Vinesh / Buchmann, Eckhart / Ndesendo, Valence M K / Pillay, Viness

Journal of biomedical materials research. Part A

2013 Volume 101, Issue 12, Page(s) 3616–3629

Abstract: The relationship between mucin (MUC) and pectin (PEC) was explored in an attempt to understand the biomacromolecular interactions that occur at mucosal surfaces when mucus membranes are exposed to PEC-based materials. These interactions were explored ... ...

Abstract	The relationship between mucin (MUC) and pectin (PEC) was explored in an attempt to understand the biomacromolecular interactions that occur at mucosal surfaces when mucus membranes are exposed to PEC-based materials. These interactions were explored through techniques, such as attenuated total reflection Fourier transform infrared (ATR-FTIR) spectroscopy, SEM imagery of lyophilized MUC-PEC blends, thermodynamic analysis, rheology investigations, and in silico static lattice atomistic simulations using a molecular mechanics energy relationships (MMER) approach. Three types of PEC that had different degrees of esterification and degrees of amidation were investigated at different MUC-PEC mass ratios (1:0, 1:1, 1:4, 1:9, and 0:1). The effect PEG 400 and Ca(2 +) in the MUC-PEC interactions were also studied. ATR-FTIR spectroscopy revealed broadening and strengthening of FTIR peaks at 3363 cm(-1) and between 3000-3650 cm(-1) due to stretching vibrations of the -OH, -COOH groups on MUC and PEC as well as the -N-H group on MUC. This suggested significant intra- and inter-molecular H-bonding. Morphologically, MUC-rich scaffolds were porous, thin, and multidirectional compared with the smooth, rigid, and unidirectional PEC-rich scaffolds. The Flory-Huggins interaction parameter (χ12 ) for all MUC-PEC mass ratios was negative, thus confirming MUC-PEC miscibility and interactions. UV absorbance increased with increasing relative concentration of PEC in the aqueous MUC-PEC dispersions. Furthermore, rheology investigations demonstrated synergistic enhancement in viscosity (η) and dynamic moduli upon the addition of PEG 400 and Ca(2 +) . MMER analysis revealed several key MUC-PEC interactions that corroborated well with the experimental data. Notably, higher esterification and larger mass ratios of PEC yielded greater MUC-PEC interactions.
MeSH term(s)	Animals ; Calorimetry, Differential Scanning ; Carbohydrates/chemistry ; Cross-Linking Reagents/chemistry ; Elastic Modulus ; Freeze Drying ; Hydrogel, Polyethylene Glycol Dimethacrylate/metabolism ; Macromolecular Substances ; Mucins/metabolism ; Mucous Membrane/metabolism ; Pectins/metabolism ; Rheology ; Spectrophotometry, Ultraviolet ; Spectroscopy, Fourier Transform Infrared ; Sus scrofa ; Thermodynamics ; Viscosity
Chemical Substances	Carbohydrates ; Cross-Linking Reagents ; Macromolecular Substances ; Mucins ; Pectins ; Hydrogel, Polyethylene Glycol Dimethacrylate (25852-47-5) ; pectin (89NA02M4RX)
Language	English
Publishing date	2013-12
Publishing country	United States
Document type	Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	2099989-6
ISSN	1552-4965 ; 1549-3296 ; 0021-9304
ISSN (online)	1552-4965
ISSN	1549-3296 ; 0021-9304
DOI	10.1002/jbm.a.34664
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Zs.A 6195: Show issues

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Article ; Online: The influence of polyamide 6,10 synthesis variables on the physicochemical characteristics and drug release kinetics from a monolithic tablet matrix.

Kolawole, Oluwatoyin A / Pillay, Viness / Choonara, Yahya E / du Toit, Lisa C / Ndesendo, Valence M K

Pharmaceutical development and technology

2010 Volume 15, Issue 6, Page(s) 595–612

Abstract: This study investigated the influence of solute-solvent quotients on the physicochemical properties and release kinetics of two amitryptyline-loaded polyamide 6,10 (PA 6,10) monolithic matrices, Formulations A and B (FA and FB). The molecular mass, ... ...

Abstract	This study investigated the influence of solute-solvent quotients on the physicochemical properties and release kinetics of two amitryptyline-loaded polyamide 6,10 (PA 6,10) monolithic matrices, Formulations A and B (FA and FB). The molecular mass, crystallinity, structural elucidation and thermo-transitions were assessed using mass spectrophotometry, X-ray diffraction, FTIR and DSC. Surface morphologies of the matrices and physicomechanical strength were captured using SEM and textural analysis. Drug release, distension and matrix erosion were evaluated using mathematical modeling. FA and FB displayed overall drug release fractions of 0.58 and 0.92 with 55% and 30% of matrix remaining over 24 hours, respectively. The indentation diameters (FA = 1.51 mm; FB = 2.39 mm), deformation energies (FA = 0.02 J; FB = 0.03 J) and Brinell Hardness Numbers (FA = 17.88 N/mm²; FB = 14.45 N/mm²) were divergent. SEM revealed irregular matrix surfaces with varying pore distributions. Minimal shifts in the structural backbone of PA 6,10 and semi-crystallinity was noted. Multiple reversible and irreversible thermal transitions with molar masses of FA = 345.2 g/mol and FB = 307.2 g/mol were obtained. Drug release supported by in vivo studies provided sustained plasma levels of amitryptyline (T(max) = 24 ± 0.5 h and 12 ± 0.5 h; C(max) = 0.024 ± 0.003 μg/mL and 0.036 ± 0.002 μg/mL for FA and FB, respectively) compared to a conventional formulation, Trepiline® (T(max) = 4 ± 0.5 h and C(max) = 0.05 ± 0.002 μg/mL). The physicochemical properties of both formulations were reversibly influenced by differences in the PA 6,10 solute-solvent quotient employed during development.
MeSH term(s)	Amitriptyline/administration & dosage ; Animals ; Antidepressive Agents, Tricyclic/administration & dosage ; Crystallization ; Delayed-Action Preparations ; Kinetics ; Models, Theoretical ; Nylons/chemistry ; Solvents/chemistry ; Swine ; Tablets
Chemical Substances	Antidepressive Agents, Tricyclic ; Delayed-Action Preparations ; Nylons ; Solvents ; Tablets ; nylon 6-10 ; Amitriptyline (1806D8D52K)
Language	English
Publishing date	2010-12
Publishing country	England
Document type	Comparative Study ; Journal Article ; Research Support, Non-U.S. Gov't
ZDB-ID	1331774-x
ISSN	1097-9867 ; 1083-7450
ISSN (online)	1097-9867
ISSN	1083-7450
DOI	10.3109/10837450903397560
Database	MEDical Literature Analysis and Retrieval System OnLINE

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