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Fulltext Optimization of brush-like cationic copolymers for nonviral gene delivery

Wei H, Pahang JA, Pun SH

Biomacromolecules, 2013 Jan 14;14(1):275-84.
PMID: 23240866 DOI: 10.1021/bm301747r

Polyethylenimine (PEI) is one of the most broadly used polycations for gene delivery due to its high transfection efficiency and commercial availability but materials are cytotoxic and often polydisperse. The goal of current work is to develop an alternative family of polycations based on controlled living radical polymerization (CLRP) and to optimize the polymer structure for efficient gene delivery. In this study, well-defined poly(glycidyl methacrylate)(P(GMA)) homopolymers were synthesized using reversible addition-fragmentation chain transfer (RAFT) polymerization followed by decoration using three different types of oligoamines, i.e., tetraethylenepentamine (TEPA), pentaethylenehexamine (PEHA), and tris(2-aminoethyl)amine (TREN), respectively, to generate various P(GMA-oligoamine) homopolycations. The effect of P(GMA) backbone length and structure of oligoamine on gene transfer efficiency was then determined. The optimal polymer, P(GMA-TEPA)(50), provided comparable transfection efficiency but lower cytotoxicity than PEI. P(GMA-TEPA)(50) was then used as the cationic block in diblock copolymers containing hydrophilic N-(2-hydroxypropyl) methacrylamide (HPMA) and oligo(ethylene glycol) monomethyl ether methacrylate (OEGMA). Polyplexes of block copolymers were stable against aggregation in physiological salt condition and in Opti-MEM due to the shielding effect of P(HPMA) and P(OEGMA). However, the presence of the HPMA/OEGMA block significantly decreased the transfection efficacy of P(GMA-TEPA)(50) homopolycation. To compensate for reduced cell uptake caused by the hydrophilic shell of polyplex, the integrin-binding peptide, RGD, was conjugated to the hydrophilic chain end of P(OEGMA)(15)-b-P(GMA-TEPA)(50) copolymer by Michael-type addition reaction. At low polymer to DNA ratios, the RGD-functionalized polymer showed increased gene delivery efficiency to HeLa cells compared to analogous polymers lacking RGD.

Matched MeSH terms: Polymers/chemistry*
Structural and bone marrow stem cell biocompatibility studies of hydrogel synthesized via chemo-enzymatic route

Latfi ASA, Pramanik S, Poon CT, Gumel AM, Lai KW, Annuar MSM, et al.

J Biomater Appl, 2019 01;33(6):854-865.
PMID: 30458659 DOI: 10.1177/0885328218812490

Natural biopolymers have many attractive medical applications; however, complications due to fibrosis caused a reduction in diffusion and dispersal of nutrients and waste products. Consequently, severe immunocompatibility problems and poor mechanical and degradation properties in synthetic polymers ensue. Hence, the present study investigates a novel hydrogel material synthesized from caprolactone, ethylene glycol, ethylenediamine, polyethylene glycol, ammonium persulfate, and tetramethylethylenediamine via chemo-enzymatic route. Spectroscopic analyses indicated the formation of polyurea and polyhydroxyurethane as the primary building block of the hydrogel starting material. Biocompatibility studies showed positive observation in biosafety test using direct contact cytotoxicity assay in addition to active cellular growth on the hydrogel scaffold based on fluorescence observation. The synthesized hydrogel also exhibited (self)fluorescence properties under specific wavelength excitation. Hence, synthesized hydrogel could be a potential candidate for medical imaging as well as tissue engineering applications as a tissue expander, coating material, biosensor, and drug delivery system.

Matched MeSH terms: Polymers/chemistry*
Fulltext Antimicrobial Polymers: The Potential Replacement of Existing Antibiotics?

Kamaruzzaman NF, Tan LP, Hamdan RH, Choong SS, Wong WK, Gibson AJ, et al.

Int J Mol Sci, 2019 Jun 04;20(11).
PMID: 31167476 DOI: 10.3390/ijms20112747

Antimicrobial resistance is now considered a major global challenge; compromising medical advancements and our ability to treat infectious disease. Increased antimicrobial resistance has resulted in increased morbidity and mortality due to infectious diseases worldwide. The lack of discovery of novel compounds from natural products or new classes of antimicrobials, encouraged us to recycle discontinued antimicrobials that were previously removed from routine use due to their toxicity, e.g., colistin. Since the discovery of new classes of compounds is extremely expensive and has very little success, one strategy to overcome this issue could be the application of synthetic compounds that possess antimicrobial activities. Polymers with innate antimicrobial properties or that have the ability to be conjugated with other antimicrobial compounds create the possibility for replacement of antimicrobials either for the direct application as medicine or implanted on medical devices to control infection. Here, we provide the latest update on research related to antimicrobial polymers in the context of ESKAPE (Enterococcus faecium, Staphylococcus aureus, Klebsiella pneumoniae, Acinetobacter baumannii, Pseudomonas aeruginosa, and Enterobacter spp.) pathogens. We summarise polymer subgroups: compounds containing natural peptides, halogens, phosphor and sulfo derivatives and phenol and benzoic derivatives, organometalic polymers, metal nanoparticles incorporated into polymeric carriers, dendrimers and polymer-based guanidine. We intend to enhance understanding in the field and promote further work on the development of polymer based antimicrobial compounds.

Matched MeSH terms: Polymers/chemistry*
Synergetic effect of conductive polymer poly(3,4-ethylenedioxythiophene) with different structural configuration of anode for microbial fuel cell application

Kang YL, Ibrahim S, Pichiah S

Bioresour Technol, 2015;189:364-369.
PMID: 25913883 DOI: 10.1016/j.biortech.2015.04.044

PEDOT was synthesized by chemical polymerisation and characterised for its electrochemical insights. Three different anode configuration, namely graphite plate (GP), carbon cloth (CC) and graphite felt (GF) were then loaded with a fixed amount of PEDOT (2.5 mg/m(2)) denoted as GP-P, CC-P and GF-P respectively. The PEDOT coating improved the electrochemical characteristics and electron transfer capabilities of the anodes. They also contributed for enhanced MFC performances with maximum energy generation along with coulombic efficiency than the unmodified anodes. The morphological characteristics like higher surface area and open structure of felt material promoted both microbial formation and electrochemical active area. A maximum current density of 3.5A/m(2) was achieved for GF-P with CE and COD of 51% and 86% respectively. Thus, the GF-P anode excelled among the studied anodes with synergetic effect of PEDOT coating and structural configuration, making it as a potential optimum anode for MFC application.

Matched MeSH terms: Polymers/chemistry*
Fulltext Solubility of drugs in aqueous polymeric solution: effect of ovalbumin on microencapsulation process

Aziz HA, Tan YT, Peh KK

AAPS PharmSciTech, 2012 Mar;13(1):35-45.
PMID: 22101965 DOI: 10.1208/s12249-011-9707-x

Microencapsulation of water-soluble drugs using coacervation-phase separation method is very challenging, as these drugs partitioned into the aqueous polymeric solution, resulting in poor drug entrapment. For evaluating the effect of ovalbumin on the microencapsulation of drugs with different solubility, pseudoephedrine HCl, verapamil HCl, propranolol HCl, paracetamol, and curcuminoid were used. In addition, drug mixtures comprising of paracetamol and pseudoephedrine HCl were also studied. The morphology, encapsulation efficiency, particle size, and in vitro release profile were investigated. The results showed that the solubility of the drug determined the ratio of ovalbumin to be used for successful microencapsulation. The optimum ratios of drug, ovalbumin, and gelatin for water-soluble (pseudoephedrine HCl, verapamil HCl, and propranolol HCl), sparingly water-soluble (paracetamol), and water-insoluble (curcuminoid) drugs were found to be 1:1:2, 2:3:5, and 1:3:4. As for the drug mixture, the optimum ratio of drug, ovalbumin, and gelatin was 2:3:5. Encapsulated particles prepared at the optimum ratios showed high yield, drug loading, entrapment efficiency, and sustained release profiles. The solubility of drug affected the particle size of the encapsulated particle. Highly soluble drugs resulted in smaller particle size. In conclusion, addition of ovalbumin circumvented the partitioning effect, leading to the successful microencapsulation of water-soluble drugs.

Matched MeSH terms: Polymers/chemistry*
Formulation and evaluation of controlled release Eudragit buccal patches

Wong CF, Yuen KH, Peh KK

Int J Pharm, 1999 Feb 01;178(1):11-22.
PMID: 10205621

Controlled release buccal patches were fabricated using Eudragit NE40D and studied. Various bioadhesive polymers, namely hydroxypropylmethyl cellulose, sodium carboxymethyl cellulose and Carbopol of different grades, were incorporated into the patches, to modify their bioadhesive properties as well as the rate of drug release, using metoprolol tartrate as the model drug. The in-vitro drug release was determined using the USP 23 dissolution test apparatus 5 with slight modification, while the bioadhesive properties were evaluated using texture analyzer equipment with chicken pouch as the model tissue. The incorporation of hydrophilic polymers was found to affect the drug release as well as enhance the bioadhesiveness. Although high viscosity polymers can enhance the bioadhesiveness of the patches, they also tend to cause non-homogeneous distribution of the polymers and drug, resulting in non-predictable drug-release rates. Of the various bioadhesive polymers studied, Cekol 700 appeared to be most satisfactory in terms of modifying the drug release and enhancement of the bioadhesive properties.

Matched MeSH terms: Polymers/chemistry*
Investigation on the effect of polymer and starch on the tablet properties of lyophilized orally disintegrating tablet

Liew KB, Peh KK

Arch Pharm Res, 2021 Aug;44(8):1-10.
PMID: 25579848 DOI: 10.1007/s12272-014-0542-y

Orally disintegrating tablet (ODT) is a user friendly and convenient dosage form. The study aimed to investigate the effect of polymers and wheat starch on the tablet properties of lyophilized ODT, with dapoxetine as model drug. Three polymers (hydroxypropylmethyl cellulose, carbopol 934P and Eudragit® EPO) and wheat starch were used as matrix forming materials in preparation of lyophilized ODT. The polymeric dispersion was casted into a mould and kept in a freezer at -20 °C for 4 h before freeze dried for 12 h. It was found that increasing in HPMC and Carbopol 934P concentrations produced tablets with higher hardness and longer disintegration time. In contrast, Eudragit® EPO was unable to form tablet with sufficient hardness at various concentrations. Moreover, HPMC seems to have a stronger effect on tablet hardness compared to Carbopol 934P at the same concentration level. ODT of less friable was obtained. Wheat starch acted as binder which strengthen the hardness of ODTs and prolonged the disintegration time. ODT comprising of HPMC and wheat starch at ratio of 2:1 was found to be optimum based upon the tablet properties. The optimum formulation was palatable and 80 % of the drug was released within 30 min in the dissolution study.

Matched MeSH terms: Polymers/chemistry*
Diclofenac release from eudragit-containing matrices and effects of thermal treatment

Billa N, Yuen KH, Peh KK

Drug Dev Ind Pharm, 1998 Jan;24(1):45-50.
PMID: 15605596

Ethyl acrylate-methyl methacrylate copolymer (Eudragit NE40D) was evaluated as matrix material for preparing controlled-release tablets of diclofenac sodium. Drug release could be modified in a predictable manner by varying the Eudragit NE40D content, but was pH dependent, being markedly reduced at lower pH. This could be attributed to the low solubility of the drug at these pH values. Thermal treatment of the tablets at 60 degrees C was also found to affect the rate of drug release, which was found to decrease with an increase in the treatment duration, but could be stabilized after 96 hr of treatment. This was also associated with a corresponding increase in the tablet tensile strength. However, treatment of the granules for 5 hr prior to compaction into tablets could shorten the stabilizing time of the drug release to 48 hr and that of the tensile strength to 24 hr. The effect of thermal treatment may be ascribed to better coalescence of the Eudragit particles to form a fine network, resulting in matrix of higher tortuosity and lower porosity.

Matched MeSH terms: Polymers/chemistry*
Effect of polymer, plasticizer and filler on orally disintegrating film

Liew KB, Tan YT, Peh KK

Drug Dev Ind Pharm, 2014 Jan;40(1):110-9.
PMID: 23311593 DOI: 10.3109/03639045.2012.749889

Difficulty in swallowing tablets or capsules has been identified as one of the contributing factors to non-compliance of geriatric patients. Although orally disintegrating tablet was designed for fast disintegration in mouth, the fear of taking solid tablets and the risk of choking for certain patient populations still exist.

Matched MeSH terms: Polymers/chemistry*
Extrusion based rapid prototyping technique: an advanced platform for tissue engineering scaffold fabrication

Hoque ME, Chuan YL, Pashby I

Biopolymers, 2012 Feb;97(2):83-93.
PMID: 21830198 DOI: 10.1002/bip.21701

Advances in scaffold design and fabrication technology have brought the tissue engineering field stepping into a new era. Conventional techniques used to develop scaffolds inherit limitations, such as lack of control over the pore morphology and architecture as well as reproducibility. Rapid prototyping (RP) technology, a layer-by-layer additive approach offers a unique opportunity to build complex 3D architectures overcoming those limitations that could ultimately be tailored to cater for patient-specific applications. Using RP methods, researchers have been able to customize scaffolds to mimic the biomechanical properties (in terms of structural integrity, strength, and microenvironment) of the organ or tissue to be repaired/replaced quite closely. This article provides intensive description on various extrusion based scaffold fabrication techniques and review their potential utility for TE applications. The extrusion-based technique extrudes the molten polymer as a thin filament through a nozzle onto a platform layer-by-layer and thus building 3D scaffold. The technique allows full control over pore architecture and dimension in the x- and y- planes. However, the pore height in z-direction is predetermined by the extruding nozzle diameter rather than the technique itself. This review attempts to assess the current state and future prospects of this technology.

Matched MeSH terms: Polymers/chemistry
Fulltext Combating Intracellular Pathogens with Nanohybrid-Facilitated Antibiotic Delivery

Bose RJC, Tharmalingam N, Choi Y, Madheswaran T, Paulmurugan R, McCarthy JR, et al.

Int J Nanomedicine, 2020;15:8437-8449.
PMID: 33162754 DOI: 10.2147/IJN.S271850

BACKGROUND: Lipid polymer hybrid nanoparticles (LPHNPs) have been widely investigated in drug and gene delivery as well as in medical imaging. A knowledge of lipid-based surface engineering and its effects on how the physicochemical properties of LPHNPs affect the cell-nanoparticle interactions, and consequently how it influences the cytological response, is in high demand.
METHODS: Herein, we have engineered antibiotic-loaded (doxycycline or vancomycin) LPHNPs with cationic and zwitterionic lipids and examined the effects on their physicochemical characteristics (size and charge), antibiotic entrapment efficiency, and the in vitro intracellular bacterial killing efficiency against Mycobacterium smegmatis or Staphylococcus aureus infected macrophages.
RESULTS: The incorporation of cationic or zwitterionic lipids in the LPHNP formulation resulted in a size reduction in LPHNPs formulations and shifted the surface charge of bare NPs towards positive or neutral values. Also observed were influences on the drug incorporation efficiency and modulation of the drug release from the biodegradable polymeric core. The therapeutic efficacy of LPHNPs loaded with vancomycin was improved as its minimum inhibitory concentration (MIC) (2 µg/mL) versus free vancomycin (4 µg/mL). Importantly, our results show a direct relationship between the cationic surface nature of LPHNPs and its intracellular bacterial killing efficiency as the cationic doxycycline or vancomycin loaded LPHNPs reduced 4 or 3 log CFU respectively versus the untreated controls.
CONCLUSION: In our study, modulation of surface charge in the nanomaterial formulation increased macrophage uptake and intracellular bacterial killing efficiency of LPHNPs loaded with antibiotics, suggesting alternate way for optimizing their use in biomedical applications.

Matched MeSH terms: Polymers/chemistry
Permeability improvement of polyethersulfone-polietylene glycol (PEG-PES) flat sheet type membranes by tripolyphosphate-crosslinked chitosan (TPP-CS) coating

Lusiana RA, Sangkota VDA, Sasongko NA, Gunawan G, Wijaya AR, Santosa SJ, et al.

Int J Biol Macromol, 2020 Jun 01;152:633-644.
PMID: 32112845 DOI: 10.1016/j.ijbiomac.2020.02.290

In this study, improvement of urea and creatinine permeability of polyethersulfone (PES) membrane by coating with synthesized tripolyphosphate-crosslinked chitosan (TPP-CS) has been conducted. Original and modified membranes, e.g. pristine PES, polyethersulfone-polyethylene glycol (PES-PEG) and PES-PEG/TPP-CS membranes were characterized using FTIR, DTG, SEM, AFM, water uptake, contact angles, porosity measurement, tensile strength test and permeation tests against urea and creatinine. The results show that the PES modification by TPP-CS coating has been successfully carried out. The water uptake ability, hydrophilicity and porosity of the modified membranes increase significantly to a greater degree. All modified membranes have good thermal stability and tensile strength and their permeation ability towards urea and creatinine increase with the increasing concentration of TPP-CS. PES membrane has urea clearance ability of 7.36 mg/dL and creatinine of 0.014 mg/dL; membrane PES-PEG shows urea clearance of 11.87 mg/dL and creatinine of 0.32 mg/dL; while PES-PEG/TPP-CS membrane gives urea clearance of 20.87-36.40 mg/dL and creatinine in the range of 0.52-0.78 mg/dL. These results suggest that the PES-PEG membrane coated with TPP-CS is superior and can be used as potential material for hemodialysis membrane.

Matched MeSH terms: Polymers/chemistry*
Fulltext Role of morphological structure, doping, and coating of different materials in the sensing characteristics of humidity sensors

Tripathy A, Pramanik S, Cho J, Santhosh J, Osman NA

Sensors (Basel), 2014;14(9):16343-422.
PMID: 25256110 DOI: 10.3390/s140916343

The humidity sensing characteristics of different sensing materials are important properties in order to monitor different products or events in a wide range of industrial sectors, research and development laboratories as well as daily life. The primary aim of this study is to compare the sensing characteristics, including impedance or resistance, capacitance, hysteresis, recovery and response times, and stability with respect to relative humidity, frequency, and temperature, of different materials. Various materials, including ceramics, semiconductors, and polymers, used for sensing relative humidity have been reviewed. Correlations of the different electrical characteristics of different doped sensor materials as the most unique feature of a material have been noted. The electrical properties of different sensor materials are found to change significantly with the morphological changes, doping concentration of different materials and film thickness of the substrate. Various applications and scopes are pointed out in the review article. We extensively reviewed almost all main kinds of relative humidity sensors and how their electrical characteristics vary with different doping concentrations, film thickness and basic sensing materials. Based on statistical tests, the zinc oxide-based sensing material is best for humidity sensor design since it shows extremely low hysteresis loss, minimum response and recovery times and excellent stability.

Matched MeSH terms: Polymers/chemistry*
Synthesis, mechanical properties, and in vitro biocompatibility with osteoblasts of calcium silicate-reduced graphene oxide composites

Mehrali M, Moghaddam E, Shirazi SF, Baradaran S, Mehrali M, Latibari ST, et al.

ACS Appl Mater Interfaces, 2014 Mar 26;6(6):3947-62.
PMID: 24588873 DOI: 10.1021/am500845x

Calcium silicate (CaSiO3, CS) ceramics are promising bioactive materials for bone tissue engineering, particularly for bone repair. However, the low toughness of CS limits its application in load-bearing conditions. Recent findings indicating the promising biocompatibility of graphene imply that graphene can be used as an additive to improve the mechanical properties of composites. Here, we report a simple method for the synthesis of calcium silicate/reduced graphene oxide (CS/rGO) composites using a hydrothermal approach followed by hot isostatic pressing (HIP). Adding rGO to pure CS increased the hardness of the material by ∼40%, the elastic modulus by ∼52%, and the fracture toughness by ∼123%. Different toughening mechanisms were observed including crack bridging, crack branching, crack deflection, and rGO pull-out, thus increasing the resistance to crack propagation and leading to a considerable improvement in the fracture toughness of the composites. The formation of bone-like apatite on a range of CS/rGO composites with rGO weight percentages ranging from 0 to 1.5 has been investigated in simulated body fluid (SBF). The presence of a bone-like apatite layer on the composite surface after soaking in SBF was demonstrated by X-ray diffraction (XRD) and field emission scanning electron microscopy (FESEM). The biocompatibility of the CS/rGO composites was characterized using methyl thiazole tetrazolium (MTT) assays in vitro. The cell adhesion results showed that human osteoblast cells (hFOB) can adhere to and develop on the CS/rGO composites. In addition, the proliferation rate and alkaline phosphatase (ALP) activity of cells on the CS/rGO composites were improved compared with the pure CS ceramics. These results suggest that calcium silicate/reduced graphene oxide composites are promising materials for biomedical applications.

Matched MeSH terms: Polymers/chemistry
Fulltext Synergy of the flow behaviour and disperse phase of cellulose nanoparticles in enhancing oil recovery at reservoir condition

Agi A, Junin R, Arsad A, Abbas A, Gbadamosi A, Azli NB, et al.

PLoS One, 2019;14(9):e0220778.
PMID: 31560699 DOI: 10.1371/journal.pone.0220778

Ascorbic acid was used for the first time to synthesize cellulose nanoparticles (CNP) extracted from okra mucilage. The physical properties of the CNP including their size distribution, and crystalline structures were investigated. The rheological properties of the cellulose nanofluid (CNF) were compared with the bulk okra mucilage and commercial polymer xanthan. The interfacial properties of the CNF at the interface of oil-water (O/W) system were investigated at different concentrations and temperatures. The effects of the interaction between the electrolyte and ultrasonic were determined. Core flooding experiment was conducted at reservoir condition to justify the effect of the flow behaviour and disperse phase behaviour of CNF on additional oil recovery. The performance of the CNF was compared to conventional EOR chemical. The combined method of ultrasonic, weak-acid hydrolysis and nanoprecipitation were effective in producing spherical and polygonal nanoparticles with a mean diameter of 100 nm, increased yield of 51% and preserved crystallinity respectively. The zeta potential result shows that the CNF was stable, and the surface charge signifies long term stability of the fluid when injected into oil field reservoirs. The CNF, okra and xanthan exhibited shear-thinning and pseudoplastic behaviour. The IFT decreased with increase in concentration of CNF, electrolyte and temperature. The pressure drop data confirmed the stability of CNF at 120°C and the formation of oil bank was enough to increase the oil recovery by 20%. CNF was found to be very effective in mobilizing residual oil at high-temperature high-pressure (HTHP) reservoir condition. The energy and cost estimations have shown that investing in ultrasonic-assisted weak-acid hydrolysis is easier, cost-effective, and can reduce energy consumption making the method economically advantageous compared to conventional methods.

Matched MeSH terms: Polymers/chemistry
Aptamer-Mediated Polymeric Vehicles for Enhanced Cell-Targeted Drug Delivery

Tan KX, Danquah MK, Sidhu A, Yon LS, Ongkudon CM

Curr Drug Targets, 2018 02 08;19(3):248-258.
PMID: 27321771 DOI: 10.2174/1389450117666160617120926

BACKGROUND: The search for smart delivery systems for enhanced pre-clinical and clinical pharmaceutical delivery and cell targeting continues to be a major biomedical research endeavor owing to differences in the physicochemical characteristics and physiological effects of drug molecules, and this affects the delivery mechanisms to elicit maximum therapeutic effects. Targeted drug delivery is a smart evolution essential to address major challenges associated with conventional drug delivery systems. These challenges mostly result in poor pharmacokinetics due to the inability of the active pharmaceutical ingredients to specifically act on malignant cells thus, causing poor therapeutic index and toxicity to surrounding normal cells. Aptamers are oligonucleotides with engineered affinities to bind specifically to their cognate targets. Aptamers have gained significant interests as effective targeting elements for enhanced therapeutic delivery as they can be generated to specifically bind to wide range of targets including proteins, peptides, ions, cells and tissues. Notwithstanding, effective delivery of aptamers as therapeutic vehicles is challenged by cell membrane electrostatic repulsion, endonuclease degradation, low pH cleavage, and binding conformation stability.
OBJECTIVE: The application of molecularly engineered biodegradable and biocompatible polymeric particles with tunable features such as surface area and chemistry, particulate size distribution and toxicity creates opportunities to develop smart aptamer-mediated delivery systems for controlled drug release.
RESULTS: This article discusses opportunities for particulate aptamer-drug formulations to advance current drug delivery modalities by navigating active ingredients through cellular and biomolecular traffic to target sites for sustained and controlled release at effective therapeutic dosages while minimizing systemic cytotoxic effects.
CONCLUSION: A proposal for a novel drug-polymer-aptamer-polymer (DPAP) design of aptamer-drug formulation with stage-wise delivery mechanism is presented to illustrate the potential efficacy of aptamer- polymer cargos for enhanced cell targeting and drug delivery.

Matched MeSH terms: Polymers/chemistry
Two new polymorphs of 2,6-diaminopyrimidin-4(3H)-one monohydrate

Suleiman Gwaram N, Khaledi H, Ali HM, Olmstead MM

Acta Crystallogr C, 2011 Jan;67(Pt 1):o6-9.
PMID: 21206084 DOI: 10.1107/S0108270110046317

The title compound, C(4)H(6)N(4)O·H(2)O, crystallized simultaneously as a triclinic and a monoclinic polymorph from an aqueous solution of 2,4-diaminopyrimidin-6-ol. Previously, an orthorhombic polymorph was isolated under the same experimental conditions. The molecular geometric parameters in the two present polymorphs and the previously reported orthorhombic polymorph are similar, but the structures differ in the details of their crystal packing. In the triclinic system, the diaminopyrimidinone molecules are connected to one another via N-H···O and N-H···N hydrogen bonding to form infinite chains in the [011] direction. The chains are further hydrogen bonded to the water molecules, resulting in a three-dimensional network. In the monoclinic system, the diaminopyrimidinone molecules are hydrogen bonded together into two-dimensional networks parallel to the bc plane. The water molecules link the planes to form a three-dimensional polymeric structure.

Matched MeSH terms: Polymers/chemistry
Drug release property of chitosan-pectinate beads and its changes under the influence of microwave

Wong TW, Nurjaya S

Eur J Pharm Biopharm, 2008 May;69(1):176-88.
PMID: 17980563

The effects of microwave irradiation on the drug release property of pectinate beads loaded internally with chitosan (chitosan-pectinate beads) were investigated against the pectinate beads and beads coacervated with chitosan externally (pectinate-chitosonium beads). These beads were prepared by an extrusion method using sodium diclofenac as the model water-soluble drug. The beads were subjected to microwave irradiation at 80 W for 5, 10, 21 and 40 min. The profiles of drug dissolution, drug content, drug-polymer interaction and polymer-polymer interaction were determined by drug dissolution testing, drug content assay, drug adsorption study, differential scanning calorimetry (DSC) and Fourier transform infra-red spectroscopy (FTIR) techniques. Treatment of pectinate beads by microwave did not lead to a decrease, but an increase in the extent of drug released at 4h of dissolution owing to reduced pectin-pectin interaction via the CO moiety of polymer. In addition, the extent of drug released from the pectinate beads could not be reduced merely through the coacervation of pectinate matrix with chitosan. The reduction in the extent of drug released from the pectinate-chitosonium beads required the treatment of these beads by microwave, following an increase in drug-polymer and polymer-polymer interaction in the matrix. The extent of drug released from the pectinate beads was reduced through incorporating chitosan directly into the interior of pectinate matrix, owing to drug-chitosan adsorption. Nonetheless, the treatment of chitosan-pectinate matrix by microwave brought about an increase in the extent of drug released unlike those of pectinate-chitosonium beads. Apparently, the loading of chitosan into the interior of pectinate matrix could effectively retard the drug release without subjecting the beads to the treatment of microwave. The microwave was merely essential to reduce the release of drug from pectinate beads when the chitosan was introduced to the pectinate matrix by means of coacervation. Under the influences of microwave, the drug release property of beads made of pectin and chitosan was mainly modulated via the CH, OH and NH moieties of polymers and drug, with CH functional group purported to retard while OH and NH moieties purported to enhance the drug released from the matrix.

Matched MeSH terms: Polymers/chemistry
Fulltext Novel swellable polymer of orchidaceae family for gastroretentive drug delivery of famotidine

Razavi M, Nyamathulla S, Karimian H, Noordin MI

Drug Des Devel Ther, 2014;8:1315-29.
PMID: 25246773 DOI: 10.2147/DDDT.S68517

This study aimed to develop hydrophilic, gastroretentive matrix tablets of famotidine with good floating and swelling properties. A novel gastroretentive drug delivery formulation was designed using salep, also known as salepi, a flour obtained from grinding dried palmate tubers of Orchis morio var mascula (Orchidaceae family). The main polysaccharide content of salep is glucomannan, highly soluble in cold and hot water, which forms a viscous solution. Salep was characterized for physicochemical properties, thermal stability, chemical interaction, and surface morphology using X-ray diffraction analysis, differential scanning calorimetry, Fourier transform infrared spectroscopy, and scanning electron microscopy. Ten different formulations (S1-S10) were prepared using famotidine to salep ratios from 1:0.5 to 1:5. Results demonstrated that all formulations were able to sustain the drug release for more than 24 hours. The S5 formulation, with a famotidine to salep ratio of 1:2.5, had the shortest floating lag time of 35 seconds and 100% drug release within 24 hours. The dissolution data were fitted into popular mathematical models to assess the mechanism of drug release. S5 showed Zero order release (R=0.9746) with Higuchi diffusion (R=0.9428). We conclude that salep, a novel polymer, can be used in controlled release formulations to sustain release for 24 hours, due to inherent swelling and gelling properties.

Matched MeSH terms: Polymers/chemistry*
Fulltext Gamma scintigraphic evaluation of floating gastroretentive tablets of metformin HCl using a combination of three natural polymers in rabbits

Razavi M, Karimian H, Yeong CH, Chung LY, Nyamathulla S, Noordin MI

Drug Des Devel Ther, 2015;9:4373-86.
PMID: 26273196 DOI: 10.2147/DDDT.S86263

The present research was aimed at formulating a metformin HCl sustained-release formulation from a combination of polymers, using the wet granulation technique. A total of 16 formulations (F1-F16) were produced using different combinations of the gel-forming polymers: tamarind kernel powder, salep (palmate tubers of Orchis morio), and xanthan. Post-compression studies showed that there were no interactions between the active drug and the polymers. Results of in vitro drug-release studies indicated that the F10 formulation which contained 5 mg of tamarind kernel powder, 33.33 mg of xanthan, and 61.67 mg of salep could sustain a 95% release in 12 hours. The results also showed that F2 had a 55% similarity factor with the commercial formulation (C-ER), and the release kinetics were explained with zero order and Higuchi models. The in vivo study was performed in New Zealand White rabbits by gamma scintigraphy; the F10 formulation was radiolabeled using samarium (III) oxide ((153)Sm2O3) to trace transit of the tablets in the gastrointestinal tract. The in vivo data supported the retention of F10 formulation in the gastric region for 12 hours. In conclusion, the use of a combination of polymers in this study helped to develop an optimal gastroretentive drug-delivery system with improved bioavailability, swelling, and floating characteristics.

Matched MeSH terms: Polymers/chemistry*

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