ABSTRACT
Dehydration is a well-known problem worldwide, and its assessment can be challenging due to confusing physical signs. The most effective way to assess hydration status is through the costly stable isotope methodology, but this approach has practical limitations. More commonly accepted and utilized indicators of hydration status are hematological and urinary parameters. However, hematological markers require invasive methods, and urinary markers have varying degrees of success in tracking hydration changes. While alterations in body weight can serve as a means of promptly evaluating hydration status, various factors such as food consumption, fluid intake, fecal losses, and urine production can impact these changes. Researchers have turned their attention to saliva as a potential marker and point-of-care (POC) testing to address the limitations of existing biomarkers. Saliva is appealing due to its easy collection process and similarities to extracellular fluid in terms of water and ion concentrations. Recent studies have shown that saliva flow rate, osmolarity/osmolality, and total protein concentration can effectively monitor changes in body mass during acute dehydration. Misdiagnosing dehydration can have severe clinical consequences, leading to morbidity and even mortality. This narrative review focuses on recognizing the significance of hydration assessment, monitoring, and the potential of salivary osmolarity (SOSM) as an assessment tool. Healthcare professionals can improve their practices and interventions to optimize hydration and promote overall wellness using such tools.
Subject(s)
Dehydration , Saliva , Humans , Saliva/chemistry , Osmolar Concentration , Dehydration/diagnosis , Biomarkers/analysis , Point-of-Care Systems , Organism Hydration Status/physiology , Point-of-Care TestingABSTRACT
UNLABELLED: Background. Starch is one of the most potential natural polymers used for various bio applications. Literature reports a num- ber of modification strategies such as physical, chemical, enzymatic and genetic to enhance the positive attributes and iron out the undesired features of neat starch. OBJECTIVES: To synthesize a crosslinked porous starch (CPS) as an efficient cargo for the delivery of calcium carbonate in an efficiently controlled manner for the treatment of hyperphosphatemia. MATERIAL AND METHODS: The CPS carrier was synthesized using a natural crosslinker, malic acid. The drug delivery system was formulated, followed by the in situ loading of calcium carbonate during the preparation of the CPS. The developed system was characterized with respect to FTIR, DSC, SEM, moisture content, zeta potential, encapsulation efficiency, phosphate binding efficiency and dissolution studies. RESULTS: The developed formulation was observed to deliver calcium carbonate in an enterically controlled manner. The binding of calcium to phosphate was established to be pH dependent and efficient at pH 7. The moisture content of CPS was in the range of 0.2-0.8%. The zeta potential of the colloidal system was noted to be sufficiently high, indicating the stability. The encapsulation efficiency of CPS particles for calcium was found to be 88-96%. CONCLUSIONS: An efficient, cost-effective, facile and commercially-viable formulation was demonstrated to deliver calcium carbonate for the treatment of hyperphosphatemia.
Subject(s)
Calcium Carbonate/administration & dosage , Cross-Linking Reagents/chemistry , Drug Carriers/chemistry , Starch/chemistry , Calcium/chemistry , Calcium Carbonate/chemistry , Chemistry, Pharmaceutical , Cross-Linking Reagents/chemical synthesis , Delayed-Action Preparations , Drug Carriers/chemical synthesis , Drug Delivery Systems/methods , Hydrogen-Ion Concentration , Malates/chemistry , Particle Size , Phosphates/chemistry , Porosity , Starch/chemical synthesis , Tablets, Enteric-CoatedABSTRACT
To circumvent the solubility-related issues associated with Biopharmaceutics Classification System class II drugs, a novel porous carrier has been developed. In the present study, a process for preparation of porous starch (PS) is demonstrated. The process briefly comprises of translucent gel preparation followed by solvent replacement, drying, and sizing. Carbamazepine (CBZ) was used as a drug candidate to exhibit solubility enhancement potential of PS. PS and CBZ-loaded PS (CBZ-PS) systems were characterized with respect to IR, DSC, XRD, SEM, and dissolution kinetic studies. PS-CBZ was found to follow a Fickian behavior during dissolution. In vivo studies conducted in mice displayed a superior performance of CBZ-PS as compared to neat CBZ.
Subject(s)
Anticonvulsants/chemistry , Carbamazepine/chemistry , Calorimetry, Differential Scanning , Kinetics , Microscopy, Electron, Scanning , Powder Diffraction , Solubility , Spectroscopy, Fourier Transform InfraredABSTRACT
BACKGROUND: A biodegradable porous starch (BPS) was developed in order to improve dissolution and oral bioavailability of Itraconazole as a poorly water-soluble antifungal drug. METHOD: BPS was developed by converting native starch from hydrogel to alcogel by solvent exchange method. The developed BPS carrier was characterized by SEM and nitrogen adsorption/desorption analysis to understand surface morphology and porosity distribution respectively. Itraconazole (ITR) was loaded on BPS by adsorption mediated solvent evaporation method, which provides a hydrophilic matrix powder. This causes drug distribution within hydrophilic matrix of porous starch. RESULTS: Solid-state characterization of optimized batch (ITR/BPS-3) was performed using DSC, PXRD, FTIR, SEM and FTIR chemical imaging. In vitro dissolution and in vivo pharmacokinetic studies were performed to evaluate therapeutic potential of ITR/BPS-3 system. In vitro studies of ITR: BPS-3 system revealed a burst effect in drug release (93%) compared to marketed product, which showed 90% drug release at the end of 60 min compared to 84% of marketed. Moreover, ITR/BPS-3 system showed improved oral bioavailability up to 3.93 fold and marketed product shows 3.12 fold compared to ITR. CONCLUSION: This effect is due to high surface area, improved wettability and reduced crystallinity of ITR due to its adsorption into BPS. A successful methodology was reported to prepare BPS from raw starch.
Subject(s)
Antifungal Agents/administration & dosage , Drug Carriers/administration & dosage , Itraconazole/administration & dosage , Starch/administration & dosage , Administration, Oral , Adsorption , Animals , Antifungal Agents/blood , Antifungal Agents/chemistry , Antifungal Agents/pharmacokinetics , Biological Availability , Calorimetry, Differential Scanning , Drug Carriers/chemistry , Drug Carriers/pharmacokinetics , Drug Liberation , Itraconazole/blood , Itraconazole/chemistry , Itraconazole/pharmacokinetics , Male , Microscopy, Electron, Scanning , Porosity , Powder Diffraction , Rats, Wistar , Spectroscopy, Fourier Transform Infrared , Starch/chemistry , Starch/pharmacokinetics , X-Ray DiffractionABSTRACT
This work studied artemether (ARTM) solid dispersion (SD) formulation using mixture of polymer excipient Soluplus, PEG 400, Lutrol F127, and Lutrol F68 melts at temperatures lower than the melting point of ARTM using a laboratory-size, single-screw rotating batch extruder. The effects of three surfactants PEG 400, Lutrol F127, and Lutrol F68 and parameters like mixing temperature, screw rotating speed, and residence time were systematically studied. SEM, XRD, and FT-IR were employed to investigate the evolution of ARTM's dissolution into the molten excipient. Differential scanning calorimetry (DSC) was used to quantitatively study the melting enthalpy evolution of the drug. The results showed that the dissolution rate increased with increasing the ratio of polymer and surfactant to that of drug. It was concluded that the dissolution of the drug in the polymer melt is a convective diffusion process and that laminar distributive mixing can significantly enhance the dissolution rate. The aqueous solubility and dissolution rate of prepared solid dispersion were significantly enhanced. In vitro antimalarial studies revealed marked improvement in IC50 values. Thus hot-melt extrusion (HME) is a promising technology for improving solubility and dissolution profile of ARTM.
ABSTRACT
In the present paper, preparation of mesoporous silica using hydroxy propyl-ß-cyclodextrin as a template and its use in solubility enhancement of carbamazepine (CBZ) is reported. The produced mesoporous silica (MS) displayed a large surface area 480.37 m(2)/g and pore volume 0.8041 cm(3)/g. CBZ was loaded on MS and then compressed into a tablet. Dissolution kinetics studies revealed rapid release profiles in comparison to neat crystalline CBZ. Solid-state characterization was done using IR, DSC, PXRD, SEM and TEM, and nitrogen sorption studies. CBZ was found to be in non-crystalline state due to geometric confinement in the nanopore.
ABSTRACT
Liquid antisolvent process was explored as a solubility modulating tool. Bicalutamide, a poorly water soluble drug, was used as a candidate. Low aqueous solubility and poor dissolution of bicalutamide results into poor and variable bioavailability. Therefore, the objective of the present work was to modify the solubility of bicalutamide using the liquid antisolvent precipitation process. HPMC E5 and Poloxamer 407 were shortlisted as a hydrophilic polymer and surfactant, respectively, for the process. Process optimization was done with respect to the hydrophilic polymer, surfactant and drug loading concentration. The resultant microcrystals were characterized with various instrumental techniques for material characterization such as IR, DSC, SEM, XRD, particle size, specific surface area and dissolution kinetics.