scholarly journals Polycomplex Carrier for Buccal Mucoadhesion Delivery of Metronidazole

2020 ◽  
Vol 9 (2) ◽  
pp. 83-90
Author(s):  
R. I. Moustafine ◽  
V. V. Budnikov ◽  
S. G. Abdullina ◽  
Sh. F. Nasibullin ◽  
R. A. Saleev
Keyword(s):  
Periodontal Diseases ◽  
Pharmaceutical Research ◽  
Weight Ratio ◽  
Uv Spectrophotometry ◽  
Scanning Calorimetry ◽  
Interpolyelectrolyte Complex ◽  
Usp 4 ◽  
Buccal Drug Delivery ◽  
Long Time ◽  
Micro Systems

Introduction. One of the well-known requirements for buccal drug delivery systems is the demonstration of mucoadhesive properties of the carrier, ensuring retention on the mucosa for a long time with the gradual release of the included drug. It should be noted that one of the advantages of buccal systems compared with oral ones is the absence of the «first pass effect» through the liver.Aim. To carry out a physicochemical and pharmaceutical research of the interpolyelectrolyte complex (IPEC), obtained on the basis of pharmaceutically acceptable polymers – Eudragit® EPO and Noveon® AA-1, in comparison with the physical mixture and individual polymers, as a mucoadhesive delivery system of metronidazole for the treatment of periodontal diseases.Materials and methods. Obtained on the basis of a pair of pharmaceutical polymers (Eudragit® EPO and Noveon® AA-1), two IPEC samples were characterized by elemental analysis, FTIR spectroscopy, and modulated temperature differential scanning calorimetry (mDSC) in comparison with individual polymers and their physical mixtures. The study of swelling ability, bioadhesion and release was carried out in a medium simulating artificial salivary fluid (pH 7.0) at a temperature of 37 ± 0.1 °C. Mucoadhesion of polymer samples and IPEC was studied using a TA.XTplus texture analyzer (Stable Micro Systems, UK). The release of metronidazole (MD) from matrices based on the developed IPEC was studied on a CE 7Smart USP 4 apparatus (Sotax, Switzerland) using the Flow Trough Cell method at a speed a flow of 20 ml/min in an open cycle within 5 hours. The amount of released MD was estimated by UV spectrophotometry on a Lambda 25 instrument (PerkinElmer, USA) at a wavelength of 319 nm.Results and discussion. As a result of studies on the physicochemical and pharmaceutical properties, there was selected the optimal composition of a polycomplex carrier (IPEC 2) based on Eudragit® EPO and Noveon® AA-1, which is characterized by the required bioadhesive properties and the ability of providing controlled release of drug from the tablet matrix (with weight ratio MD/IPEC-2 1:0.5) in conditions mimicking oral cavity environment, which provides the necessary mode of buccal delivery of metronidazole in accordance with Fick's law of diffusion.Conclusion. IPEC 2 is a perspective for use as carrier for buccal controlled delivery of metronidazole.

scholarly journals Interpolymer Complexes Based on Carbopol® and Poly(2-ethyl-2-oxazoline) as Carriers for Buccal Delivery of Metformin

2021 ◽  
Vol 10 (1) ◽  
pp. 48-55
Author(s):  
A. S. Viktorova ◽  
E. S. Elizarova ◽  
R. S. Romanova ◽  
V. R. Timergalieva ◽  
V. V. Khutoryanskiy ◽  
...  
Keyword(s):  
Artificial Saliva ◽  
Weight Ratio ◽  
Polymer Matrices ◽  
Prolonged Release ◽  
Uv Spectrophotometry ◽  
Buccal Delivery ◽  
Interpolymer Complexes ◽  
Porcine Gastric Mucin ◽  
Buccal Drug Delivery ◽  
Swelling Capacity

Introduction. Buccal drug delivery has a number of advantages over oral administration: ease of application, good blood supply to the buccal mucosa, drug can enter the systemic circulation directly, avoiding the "first pass effect through the liver", and are not exposed to the acidic environment of the gastric juice and the destructive action of digestive enzymes. The use of interpolymer complexes (IPCs) makes it possible not only to ensure adhesion to the mucosal membranes of the oral cavity, but also to achieve a prolonged release of drugs.Aim. Development of carriers based on interpolymer complexes using Carbopol® 971 NF (C971) and poly(2-ethyl-2-oxazoline) (POZ) of different molecular weights for buccal delivery of metformin (MF).Materials and methods. The study of IPC adhesion was carried out using a TA.XTplus texture analyzer (Stable Micro Systems, UK); mucin compacts with a diameter of 13 mm were used as a substrate; these were prepared by compressing porcine gastric mucin powder using a manual hydraulic press for IR spectroscopy (PerkinElmer, USA) at a pressure of 2.45 MPa. The study of the swelling capacity was carried out by placing polymer matrices in an artificial saliva medium, with constant thermostating at a temperature of 37.0 ± 0.5 °C for 5 hours. The study of the release of MF from the matrices based on IPC was carried out using a DFZ II apparatus (Erweka, Germany) according to the Flow Through Cell method (USP IV) with cells for tablets (22.6 mm) and adaptors for ointments, creams and gels in a medium simulating saliva. The concentration of MF in the samples from the dissolution tests was determined with UV-spectrophotometry (Lambda, PerkinElmer, USA) at 232.8 nm.Results and discussion. In a comparative study of the mucoadhesive properties of polymer samples, IPC compacts showed a mucoadhesion capacity comparable to that of poly(2-ethyl-2-oxazoline); at the same time, compacts from physical mixtures (PM) and C971 are inferior in terms of the separation force to IPC samples, however, POZes dissolve in an artificial saliva medium, that is, they are not suitable as dosage forms for buccal delivery. For 5 hours of the experiment to assess the swelling capacity, the IPC matrices did not change significantly, which can ensure their comfortable use as carriers for buccal delivery. When evaluating the release of metformin from polymer matrices (with weight ratio MF/IPC 1: 0.5), the most complete release (more than 90 %) is observed from both IPC matrices compared to matrices of PM and individual polymers.Conclusion. Polycomplex matrix systems based on C971-POZ (50 kDa) and C971-POZ (500 kDa) are suitable for buccal delivery of metformin.

Thermal Behaviour of Candesartan Active substance and in pharmaceutical compounds

2017 ◽  
Vol 68 (8) ◽  
pp. 1895-1902
Author(s):  
Ioana Cristina Tita ◽  
Eleonora Marian ◽  
Bogdan Tita ◽  
Claudia Crina Toma ◽  
Laura Vicas
Keyword(s):  
Thermal Behaviour ◽  
Active Substance ◽  
Pharmaceutical Research ◽  
Pharmaceutical Product ◽  
Nitrogen Atmosphere ◽  
Pure Substance ◽  
Scanning Calorimetry ◽  
X Ray ◽  
Ft Ir

Thermal analysis is one of the most frequently used instrumental techniques in the pharmaceutical research, for the thermal characterization of different materials from solids to semi-solids, which are of pharmaceutical relevance. In this paper, simultaneous thermogravimetry/derivative thermogravimetry (TG/DTG) and differential scanning calorimetry (DSC) were used for characterization of the thermal behaviour of candesartan cilexetil � active substance (C-AS) under dynamic nitrogen atmosphere and nonisothermal conditions, in comparison with pharmaceutical product containing the corresponding active substance. It was observed that the commercial samples showed a different thermal profile than the standard sample, caused by the presence of excipients in the pharmaceutical product and to possible interaction of these with the active substance. The Fourier transformed infrared spectroscopy (FT-IR) and X-ray powder diffraction (XRPD) were used as complementary techniques adequately implement and assist in interpretation of the thermal results. The main conclusion of this comparative study was that the TG/DTG and DSC curves, together with the FT-IR spectra, respectively X-ray difractograms constitute believe data for the discrimination between the pure substance and pharmaceutical forms.

scholarly journals Physicochemical and Antifungal Properties of Clotrimazole in Combination with High-Molecular Weight Chitosan as a Multifunctional Excipient

Marine Drugs ◽  
2020 ◽  
Vol 18 (12) ◽  
pp. 591
Author(s):  
Bożena Grimling ◽  
Bożena Karolewicz ◽  
Urszula Nawrot ◽  
Katarzyna Włodarczyk ◽  
Agata Górniak
Keyword(s):  
Molecular Weight ◽  
High Molecular Weight ◽  
Weight Ratio ◽  
Scanning Calorimetry ◽  
Minimal Inhibitory Concentrations ◽  
Dissolution Tests ◽  
Effective Combination ◽  
The Impact ◽  
High Molecular Weight Chitosan

Chitosans represent a group of multifunctional drug excipients. Here, we aimed to estimate the impact of high-molecular weight chitosan on the physicochemical properties of clotrimazole–chitosan solid mixtures (CL–CH), prepared by grinding and kneading methods. We characterised these formulas by infrared spectroscopy, differential scanning calorimetry, and powder X-ray diffractometry, and performed in vitro clotrimazole dissolution tests. Additionally, we examined the antifungal activity of clotrimazole–chitosan mixtures against clinical Candida isolates under neutral and acid conditions. The synergistic effect of clotrimazole and chitosan S combinations was observed in tests carried out at pH 4 on Candida glabrata strains. The inhibition of C. glabrata growth reached at least 90%, regardless of the drug/excipient weight ratio, and even at half of the minimal inhibitory concentrations of clotrimazole. Our results demonstrate that clotrimazole and high-molecular weight chitosan could be an effective combination in a topical antifungal formulation, as chitosan acts synergistically with clotrimazole against non-albicans candida strains.

scholarly journals Improvement of dental health in professional athletes engaged in power sports

2017 ◽  
Vol 98 (2) ◽  
pp. 189-194
Author(s):  
F R Safaraliev ◽  
A M Safarov ◽  
F Yu Mamedov
Keyword(s):  
Oral Cavity ◽  
Periodontal Diseases ◽  
Dental Health ◽  
Dental Status ◽  
Professional Athletes ◽  
Before And After ◽  
Long Time ◽  
Dental Diseases ◽  
Anti Inflammatory ◽  
Intense Training

Aim. Evaluation of dental diseases prevalence in professional athletes engaged in power sports and of the influence of biologically neutral products based on propolis on the level of their dental health. Methods. The examination of organs and tissues of the oral cavity of professional athletes engaged for a long time in power sports was carried out. With the use of the developed specialized questionnaire dental status of the athletes was determined. Based on the analysis of the results of clinical and laboratory studies anti-inflammatory and anti-bacterial effectiveness of products based on propolis were evaluated. Results. The results of the survey showed that not all athletes are informed about the possibility of aggravation of pathological processes in soft and hard tissues of oral cavity during active training, mainly, in power sports. Lack of awareness of surveyed athletes about the need for timely individual oral hygiene procedures and regular dentist visits was revealed, especially during intense training before and after competitions. On evaluation of dental status of professional combat athletes high prevalence and intensity of inflammatory periodontal disease and caries were found. High anti-inflammatory efficiency of the product «Pomegranate Balm» for correction of dental status of professional athletes was proven. Conclusion. High incidence of inflammatory periodontal diseases of mild to moderate severity was revealed in athletes during prolonged and intense physical training; efficacy of biologically neutral products based on propolis was established.

Feasibility Study of Chemical Treatments on Sorghum Fibres for Compatibility Enhancement in Polypropylene Composites

2018 ◽  
Vol 929 ◽  
pp. 70-77 ◽  
Author(s):  
Ismojo ◽  
Rai Pratama ◽  
Ghiska Ramahdita ◽  
Anne Zulfia Syahrial ◽  
Mochamad Chalid
Keyword(s):  
Crystallinity Index ◽  
Ester Group ◽  
Hydroxyl Group ◽  
Compatibility Study ◽  
Scanning Calorimetry ◽  
Polypropylene Composites ◽  
Dsc Measurements ◽  
Long Time ◽  
Weak Compatibility ◽  
Pp Composites

Polypropylene (PP) is one of the biggest petro-polymers, which is used in very wide application nowadays. The environment problem due to materials such as plastics having very long time degradability, and critical petroleum sources have promoted some studies to empowerment of natural resources such as natural fibres for substituting or at least modifying petro-polymers. Because of biodegradability obtained from natural source, sorghum fibers are interesting to be used as filler in PP composites, despite of weak compatibility between them. Surface modification on the sorghum fibers through alkalinization prior to acetylation was aimed to improve the fiber compatibility to PP. The treatments were expected to substitute hydroxyl group in the sorghum fibers, into acetic ester group in order to increase their hydrophobicity as the fillers. Moreover, the treatments were able to unbundle single fibers into micro-fibrillated cellulose (MFC) fibres with increase in crystallinity index. Usage of this MFC fiber as filler in PP leads to improvement of the composite performances such as thermal properties. In this study, Fourier Transformation Infra-Red (FTIR) Spectroscopy, X-ray Diffraction (XRD), Differential Scanning Calorimetry (DSC) and Field-Emission Scanning Electron Microscope (FE-SEM) were used to evaluate the performances of the Sorghum fibers after the treatments and as the filler in the Sorghum fibers/PP composites. The experimental results showed the MFC fibers as the smallest sizes in 5.0 microns and the highest crystallinity index up to 79.1 %, obtained from alkalinization with 2.5 M NaOH prior to acetylation with 17.4 M CH3COOH and the glacial (CH3CO2)2. Compatibility study of the treated Sorghum fibers on PP shows an improvement indicated by a strong interaction between the fibers and PP on morphology observation, increase in melting point of PP from 163.4°C (using virgin Shorgum fibers) into 163.6°C (using treated Sorghum fibers) in DSC measurements.

Development and Characterization of the Neuroregenerative Xanthohumol C/Hydroxypropyl-β-cyclodextrin Complex Suitable for Parenteral Administration

Planta Medica ◽  
2019 ◽  
Vol 85 (16) ◽  
pp. 1233-1241
Author(s):  
Michael Kirchinger ◽  
Lara Bieler ◽  
Julia Tevini ◽  
Michael Vogl ◽  
Elisabeth Haschke-Becher ◽  
...  
Keyword(s):  
Water Solubility ◽  
Pharmaceutical Research ◽  
Water Soluble ◽  
Complexing Agents ◽  
Cyclodextrin Complex ◽  
Scanning Calorimetry ◽  
In Vivo Experiments ◽  
Strong Candidate

AbstractThe chroman-like chalcone Xanthohumol C, originally found in hops, was demonstrated to be a potent neuroregenerative and neuroprotective natural product and therefore constitutes a strong candidate for further pharmaceutical research. The bottleneck for in vivo experiments is the low water solubility of this chalcone. Consequently, we developed and validated a suitable formulation enabling in vivo administration. Cyclodextrins were used as water-soluble and nontoxic complexing agents, and the complex of Xanthohumol C and 2-hydroxypropyl-β-cyclodextrin was characterized using HPLC, HPLC-MS, NMR, and differential scanning calorimetry. The water solubility of Xanthohumol C increases with increasing concentrations of cyclodextrin. Using 50 mM 2-hydroxypropyl-β-cyclodextrin, solubility was increased 650-fold. Furthermore, in vitro bioactivity of Xanthohumol C in free and complexed form did not significantly differ, suggesting the release of Xanthohumol C from 2-hydroxypropyl-β-cyclodextrin. Finally, a small-scaled in vivo experiment in a rat model showed that after i. p. administration of the complex, Xanthohumol C can be detected in serum, the brain, and the cerebrospinal fluid at 1 and 6 h post-administration. Mean (± SD) Xanthohumol C serum concentrations after 1, 6, and 12 h were determined as 463.5 (± 120.9), 61.9 (± 13.4), and 9.3 (± 0.8) ng/mL upon i. v., and 294.3 (± 22.4), 45.5 (± 0.7), and 13 (± 1.0) ng/mL after i. p. application, respectively. Accordingly, the formulation of Xanthohumol C/2-hydroxypropyl-β-cyclodextrin is suitable for further in vivo experiments and further pharmaceutical research aiming for the determination of its neuroregenerative potential in animal disease models.

Magnetic Properties of Irradiated Nickel Ferrite Thermoplastic Natural Rubber Nanocomposite

2014 ◽  
Vol 879 ◽  
pp. 206-212 ◽  
Author(s):  
Sivanesan Appadu ◽  
Sahrim Hj. Ahmad ◽  
Chantara Thevy Ratnam ◽  
Meor Yahaya Razali ◽  
Moayad Husein Flaifel ◽  
...  
Keyword(s):  
Magnetic Properties ◽  
Thermal Properties ◽  
Natural Rubber ◽  
Weight Ratio ◽  
Xrd Analysis ◽  
Degree Of Crystallinity ◽  
Scanning Calorimetry ◽  
Magnetic Microstructure ◽  
Sem Image ◽  
Thermoplastic Natural Rubber

The effect of electron beam (EB) irradiation at different doses on the magnetic, microstructure, morphological and thermal properties of NiFe2O4/Thermoplastic Natural Rubber (TPNR) nanocomposite was investigated. The NiFe2O4/TPNR nanocomposite samples were prepared by using a Haake mixer in weight ratio of 12:88. The TPNR matrix consists of natural rubber (NR), liquid natural rubber (LNR) and high density polyethylene (HDPE) in weight ratio of 20:10:70. The samples were irradiated using a 2 MeV EB machine in doses from 0 - 200 kGy. Magnetic properties studied by using the vibrating sample magnetometer (VSM) at room temperature showed that the values of saturation magnetization (MS), remanence magnetization (MR) and the coercivity (HC) value increased with increasing doses of irradiation. The increase in MSand MRvalues is attributed to the increase in concentration of Fe3+ions at octahedral B-site and decrease of concentration at the tetrahedral A-site in the NiFe2O4cubic structure. X-ray diffraction (XRD) analysis of the samples showed that peak intensities decreased and the width of the peaks increased with increasing doses of irradiation. Scanning electron microscope (SEM) image of the nanocomposite cross section showed the presence of defects which is more visible with increasing doses of irradiation. In the case of thermal properties, differential scanning calorimetry (DSC) analysis showed that the crystallization temperature (Tc) and the degree of crystallinity (Xc) of the nanocomposite samples decreased with increasing doses of irradiation due to crosslinking of polymeric chains which hinders the growth of crystals.

Synthesis of Nanocrystalline CeO2 Using Mechanochemical Method: The Effect of Milling Time on the Particle Size

2006 ◽  
Vol 517 ◽  
pp. 105-110 ◽  
Author(s):  
Abdul Hadi ◽  
Iskandar Idris Yaacob ◽  
Cheah Seok Gaik
Keyword(s):  
Cerium Dioxide ◽  
Milling Time ◽  
Gas Adsorption ◽  
Weight Ratio ◽  
High Energy ◽  
Scanning Calorimetry ◽  
Characterization Methods ◽  
Energy Impact ◽  
Nanocrystalline Cerium Dioxide ◽  
Cerium Carbonate

Nanocrystalline cerium dioxide (CeO2) has been successfully synthesized by mechanochemical technique at 12, 24, 36, 48 and 60 hours milling times. The starting materials, hydrated cerium carbonate and sodium hydroxide, were mixed in a weight ratio of 4:1 and were milled in a planetary ball mill with ball to powder ratio of 10:1. The high energy impact forces provided by the milling media caused collision of starting materials and allowed the chemical reaction to occur thus produced nanocrystalline cerium dioxide. The products were characterized using a battery of characterization methods, including thermogravimetric analysis (TGA), differential scanning calorimetry (DSC), X-ray diffraction (XRD), and gas adsorption-desorption measurement. The nanocrystalline CeO2 with 6.7 nm of crystallite size and specific surface area of 66.66 m2/g was obtained when the sample was milled for 60 hrs and they annealed in air at 350 oC. The result showed that the crystallinity of nanocrystalline CeO2 decreased with increasing milling time.

Specific Heat Measurements of Ti6Al4V/Nano SiCp Composite

2017 ◽  
Vol 14 (1) ◽  
pp. 742-746
Author(s):  
S Krishnamohan ◽  
S Ramanathan ◽  
V Ramakrishnan
Keyword(s):  
Heat Capacity ◽  
Weight Ratio ◽  
Thermal Control ◽  
Ti6al4v Alloy ◽  
Thermal Design ◽  
Thermal Method ◽  
Scanning Calorimetry ◽  
Low Weight ◽  
Wide Range ◽  
Materials Used

The elevated strength, low weight ratio and excellent corrosion resistance intrinsic to titanium and its alloys has led to a wide range of successful applications which ensures high levels of unswerving performance in aerospace. The performance of the Thermal Control System extremely depends on the thermal behavior of the materials used in its elements. The measurements of the thermal properties of materials are necessary for better understanding of the thermal design. Differential scanning calorimetry (DSC) is the most extensively used thermal method for finding wealth of information about a material. The heat capacity (Cp) of a material was established quantitatively using DSC. The measurement was made by heating a very small quantity of the Ti6Al4V alloy and Ti6Al4V/Nano SiCp composites. Mechanical alloying (MA) and Powder metallurgy (P/M) techniques were used to fabricate the Ti6Al4V alloy and Ti6Al4V/ nano SiCp composites. The heat flow reaction was recorded as a function of definite sample temperature range from −100 °C to 375 °C. The measurements of the heat capacity of each sample in three runs were recorded by DSC. The heat capacity (Cp) of specimens is reported in this study.

Hydriding Behaviour of Mg-C Nanocomposites

2003 ◽  
Vol 801 ◽  
Author(s):  
A. Bassetti ◽  
E. Bonetti ◽  
A. L. Fiorini ◽  
J. Grbovic ◽  
A. Montone ◽  
...  
Keyword(s):  
Electron Microscopy ◽  
Scanning Electron Microscopy ◽  
Differential Scanning Calorimetry ◽  
Weight Ratio ◽  
Hydrogen Desorption ◽  
X Ray Diffraction ◽  
Scanning Calorimetry ◽  
Carbon Nanocomposites ◽  
X Ray ◽  
Scanning Electron

ABSTRACTMagnesium carbon nanocomposites for hydrogen storage have been synthesized by ball milling with different amount of benzene, acting as a lubricant. Their microstructure has been studied by X-ray diffraction and scanning electron microscopy, while the hydrogen desorption temperature has been tested by differential scanning calorimetry. Experimental results show that the microstructure after milling, the hydrogenation capabilities of the material and the reactivity with the air are related to the amount of additives. In particular the carbon to benzene ratio seems to play a major role. In fact, with an optimum value of carbon to benzene weight ratio of 1/6, the amount of carbon being 15 wt% of the milled mixture, a decomposition heat equal to 57% of pure MgH2 was measured, even after air manipulation of the sample.

Sign in / Sign up

Export Citation Format

Share Document