- Feasibility of hydroxypropyl methylcellulose oleogel as an animal fat replacer for meat patties. [Journal Article]
- FRFood Res Int 2019; 122:566-572
- Canola oil was successfully structured with foam-structured hydroxypropyl methylcellulose (HPMC) into solid-like oleogels, and the feasibility of the HPMC oleogels as a replacement for animal fat (be…
Canola oil was successfully structured with foam-structured hydroxypropyl methylcellulose (HPMC) into solid-like oleogels, and the feasibility of the HPMC oleogels as a replacement for animal fat (beef tallow) was evaluated to reduce the level of saturated fat in meat patties. The textural properties (firmness and work of shear) of HPMC oleogels were higher than those of beef tallow and had a tendency to increase with increasing levels of HPMC in the oleogels. HPMC oleogels behaved rheologically like an elastic gel and also exhibited temperature-independent solid fat contents. They exhibited greater resistance against oxidation than the canola oil under the accelerated storage condition. When the beef tallow in the formulation of meat patties was replaced with HPMC oleogels at 50% and 100%, the cooking loss of the patties was significantly reduced, and their texture became much softer. Furthermore, the sensory evaluation indicated that the highest overall acceptability was attained at the 50% replacement level. The replacement of beef tallow with HPMC oleogels was significantly effective in reducing the ratio of saturated to unsaturated fat from 0.73 to 0.18, consequently producing meat patties with nutritional superiority.
- Impact of Surfactant and Surfactant-Polymer Interaction on Desupersaturation of Clotrimazole. [Journal Article]
- JPJ Pharm Sci 2019 Jun 14
- The impact of surfactants on supersaturation of clotrimazole solutions was systematically evaluated. Four clinically-relevant surfactants, sodium dodecyl sulfate (SDS), vitamin E TPGS, Tween 80 and d…
The impact of surfactants on supersaturation of clotrimazole solutions was systematically evaluated. Four clinically-relevant surfactants, sodium dodecyl sulfate (SDS), vitamin E TPGS, Tween 80 and docusate sodium were studied. The induction time for nucleation and rate of desupersaturation were determined at a supersaturation ratio of 90% amorphous solubility. Measurement was also performed in the presence of pre-dissolved hydroxypropyl methylcellulose acetate succinate (HPMCAS) to study the effect of surfactant-polymer interaction on desupersaturation. The four surfactants showed varied effects on desupersaturation. From supersaturation maintenance perspective, in the presence of HPMCAS, the rank order for the four surfactants was found to be: docusate sodium > vitamin E TPGS > SDS > Tween 80. Given the importance of maintaining supersaturation and varied effect of surfactants on nucleation kinetics and desupersaturation rate, a careful examination of API, polymer and surfactant interaction on an individual basis is recommended for selecting an appropriate surfactant for use in amorphous solid dispersion (ASD) formulation.
- Novel Hot Melt Extruded Matrices of Hydroxypropyl Cellulose and Amorphous Felodipine-Plasticized Hydroxypropyl Methylcellulose as Controlled Release Systems. [Journal Article]
- APAAPS PharmSciTech 2019 Jun 14; 20(6):219
- Hydroxypropyl methylcellulose (HPMC) is a hydrophilic retarding-release polymer with the limited application in hot melt extrusion (HME) due to its high glass transition temperature (Tg 181-191°C) an…
Hydroxypropyl methylcellulose (HPMC) is a hydrophilic retarding-release polymer with the limited application in hot melt extrusion (HME) due to its high glass transition temperature (Tg 181-191°C) and melt viscosity. The aim of this study is to develop hot melt extruded matrices using hydroxypropyl cellulose (HPC) and felodipine (FLDP) with HPMC for controlled release and explore the relations of their specialty, processability, and structure with the product properties. Results showed that FLDP/HPCEF/HPMC can be extruded at 160°C with torques not more than 0.5 N·m. The extruded matrices of FLDP/HPCEF/HPMCK15M (10:45:45 and 30:35:35) achieved the controlled release for 24 h. Rheological behaviors demonstrated that HPCEF and FLDP were miscible with HPMCK15M, attaining maximum 30% FLDP soluble in the molten mixtures. HPCEF and FLDP decreased the complex viscosity and plasticized HPMCK15M to improve the extrusion processing. DSC and FT-IR indicated that the molten soluble FLDP was amorphous in the extruded matrices by hydrogen bonding with HPCEF/HPMCK15M. SEM/energy-dispersive X-ray microanalysis illustrated that the microstructure of extrudates was surface dense and interior loose, and FLDP was homogenously dispersed. Three-point bending test revealed that the plasticizers of HPCEF and FLDP contributed differently to the mechanical properties. HPCEF decreased the flexural modulus of HPMCK15M while that of HPCEF/HPMCK15M was increased by FLDP. Besides controlled release, low moisture absorption and enhanced stability were also the correlated achievements. Therefore, HPCEF-combined poorly water-soluble drugs to plasticize HPMCK15M provide an alternative novel potential approach to realize the controlled-release delivery via HME.
- Fluoroquinolone Amorphous Polymeric Salts and Dispersions for Veterinary Uses. [Journal Article]
- PPharmaceutics 2019 Jun 09; 11(6)
- Enrofloxacin (ENRO) is a poorly soluble drug used in veterinary medicine. It differs from the more widely used fluoroquinolone ciprofloxacin (CIP) by the presence of an ethyl substituent on its piper…
Enrofloxacin (ENRO) is a poorly soluble drug used in veterinary medicine. It differs from the more widely used fluoroquinolone ciprofloxacin (CIP) by the presence of an ethyl substituent on its piperazine amino group. While a number of recent studies have examined amorphous composite formulations of CIP, little research has been conducted with ENRO in this area. Therefore, the main purpose of this work was to produce amorphous solid dispersions (ASDs) of ENRO. The solid-state properties of these samples were investigated and compared to those of the equivalent CIP ASDs, and their water uptake behavior, solubility, dissolution, and antibacterial activity were assessed. Like CIP, X-ray amorphous solid dispersions were obtained when ENRO was ball milled with acidic polymers, whereas the use of neutral polymers resulted in semi-crystalline products. Proton transfer from the carboxylic acids of the polymers to the tertiary amine of ENRO's piperazine group appears to occur in the ASDs, resulting in an ionic bond between the two components. Therefore, these ASDs can be referred to as amorphous polymeric salts (APSs). The glass transition temperatures of the APSs were significantly higher than that of ENRO, and they were also resistant to crystallization when exposed to high humidity levels. Greater concentrations were achieved with the APSs than the pure drug during solubility and dissolution studies, and this enhancement was sustained for the duration of the experiments. In addition, the antimicrobial activity of ENRO was not affected by APS formation, while the minimum inhibitory concentrations and minimum bactericidal concentrations obtained with the APS containing hydroxypropyl methylcellulose acetate succinate grade MG (HPMCAS-MG) were significantly lower than those of the pure drug. Therefore, APS formation is one method of improving the pharmaceutical properties of this drug.
- Effect of Riboflavin Solution With Hydroxypropyl Methylcellulose and Eyelid Speculum on Pachymetry Changes During Accelerated Collagen Crosslinking. [Journal Article]
- CCornea 2019; 38(7):864-867
- CONCLUSIONS: Closure of the eyelids further induces corneal swelling that may offer an advantage to improve safety of the procedure particularly in thin corneas.
- The Relationships between Process Parameters and Polymeric Nanofibers Fabricated Using a Modified Coaxial Electrospinning. [Journal Article]
- NNanomaterials (Basel) 2019 Jun 02; 9(6)
- The concrete relationship between the process parameters and nanoproduct properties is an important challenge for applying nanotechnology to produce functional nanomaterials. In this study, the relat…
The concrete relationship between the process parameters and nanoproduct properties is an important challenge for applying nanotechnology to produce functional nanomaterials. In this study, the relationships between series of process parameters and the medicated nanofibers' diameter were investigated. With an electrospinnable solution of hydroxypropyl methylcellulose (HPMC) and ketoprofen as the core fluid, four kinds of nanofibers were prepared with ethanol as a sheath fluid and under the variable applied voltages. Based on these nanofibers, a series of relationships between the process parameters and the nanofibers' diameters (D) were disclosed, such as with the height of the Taylor cone (H, D = 125 + 363H), with the angle of the Taylor cone (ɑ, D = 1576 - 19ɑ), with the length of the straight fluid jet (L, D = 285 + 209L), and with the spreading angle of the instable region (θ, D = 2342 - 43θ). In vitro dissolution tests verified that the smaller the diameters, the faster ketoprofen (KET) was released from the HPMC nanofibers. These concrete process-property relationships should provide a way to achieve new knowledge about the electrostatic energy-fluid interactions, and to meanwhile improve researchers' capability to optimize the coaxial process conditions to achieve the desired nanoproducts.
- Improving the lives of millions through new double fortification of salt technology. [Journal Article]
- MCMatern Child Nutr 2019; 15 Suppl 3:e12773
- Micronutrient deficiencies (including iodine and iron deficiency) is a global health problem affecting one third of the world's population. Salt is an ideal carrier for food fortification as it is un…
Micronutrient deficiencies (including iodine and iron deficiency) is a global health problem affecting one third of the world's population. Salt is an ideal carrier for food fortification as it is universally consumed at equal rates, independently of economic status, and it is industrially processed. Addressing iron and iodine deficiencies together is a challenge, due to interaction between iodine and iron, negating the effect of added iodine. This paper explains the development of an improved microencapsulation-based technology to produce iron premix, which, when added to iodized salt, is stable and organoleptically indistinguishable. Ferrous fumarate was extruded, followed by cutting, sieving to achieve a size of 300-710 μm (salt grain size). Agglomerated extrudates were microencapsulated (5% hydroxypropyl methylcellulose and 5% soy stearin) to form iron premix. Microencapsulation ensures that the added micronutrients are stable without interaction or degradation. Double Fortified Salt is formed by blending iron premix with iodized salt (1:200 ratio). This technology was transferred to India for industrial scale-up. The public distribution system was utilized to establish and monitor an efficient distribution network for DFS in a transparent manner. The scale-up process was initially demonstrated in the state of Uttar Pradesh, following its success two more Indian states have started distribution of DFS. At present, the DFS with iron and iodine is reaching 60 million people in India. This important health intervention technology through food fortification has the potential to be scaled globally to ensure a world free from iron deficiency anemia.
- Osmoprotectants in Hybrid Liposome/HPMC Systems as Potential Glaucoma Treatment. [Journal Article]
- PPolymers (Basel) 2019 May 28; 11(6)
- The combination of acetazolamide-loaded nano-liposomes and Hydroxypropyl methylcellulose (HPMC) with similar components to the preocular tear film in an osmoprotectant media (trehalose and erythritol…
The combination of acetazolamide-loaded nano-liposomes and Hydroxypropyl methylcellulose (HPMC) with similar components to the preocular tear film in an osmoprotectant media (trehalose and erythritol) is proposed as a novel strategy to increase the ocular bioavailability of poorly soluble drugs. Ophthalmic formulations based on acetazolamide-loaded liposomes, dispersed in the osmoprotectant solution (ACZ-LP) or in combination with HPMC (ACZ-LP-P) were characterized and in vivo evaluated. The pH and tonicity of both formulations resulted in physiological ranges. The inclusion of HPMC produced an increment in viscosity (from 0.9 to 4.7 mPa·s. 64.9 ± 2.6% of acetazolamide initially included in the formulation was retained in vesicles. In both formulations, a similar onset time (1 h) and effective time periods were observed (7 h) after a single instillation (25 μL) in normotensive rabbits' eyes. The AUC0-8h of the ACZ-LP-P was 1.5-fold higher than of ACZ-LP (p < 0.001) and the maximum hypotensive effect resulted in 1.4-fold higher (p < 0.001). In addition, the formulation of ACZ in the hybrid liposome/HPMC system produced a 30.25-folds total increment in ocular bioavailability, compared with the drug solution. Excellent tolerance in rabbits' eyes was confirmed during the study.
- Physical effects of dietary fibre on simulated luminal flow, studied by in vitro dynamic gastrointestinal digestion and fermentation. [Journal Article]
- FFFood Funct 2019 Jun 19; 10(6):3452-3465
- During the transit through the gastrointestinal tract, fibre undergoes physical changes not usually included in in vitro digestion studies even though they influence nutrient diffusion and might play…
During the transit through the gastrointestinal tract, fibre undergoes physical changes not usually included in in vitro digestion studies even though they influence nutrient diffusion and might play a role in gut microbiota growth. The aim of this study was to evaluate how physical fibre properties influence the physical properties of gastrointestinal fluids using a gastrointestinal model (stomach, small intestine, ascending colon, transverse colon, and descending colon) (simgi®). Analysis by rheological and particle size characterisation, microbiota composition and short-chain fatty acid (SCFA) determination allows the achievement of this goal. First, the water-holding capacity (WHC), microstructure, and viscosity of eight different fibres plus agar were tested. Based on the results, potato fibre, hydroxypropyl methylcellulose (HPMC), psyllium fibres, and agar (as a control) were selected for addition to a medium growth (GNMF) that was used to feed the stomach/small intestine and colon compartments in the simgi®. During gastrointestinal digestion, GNMF was collected at 5, 30 and 55 minutes of processing at the gastric stage and after the intestinal stage. Then, samples of GNMF with faecal slurry were collected at 0, 24 and 48 h of colonic fermentation. Results showed fibre-dependence on apparent viscosity. Although psyllium was partially broken down in the stomach (decrease in particle size), it was the most viscous at the colonic stage, opposite to the potato fibre, but both led to the highest total SFCA and acetic acid production profile. On a microbiological level, the most relevant increase of bacterial growth was observed in the faecal Lactobacillus species, especially for HPMC and potato fibre, that were not digested until reaching the colon. Besides fibre fermentability, viscosity also influenced microbial growth, and it is necessary to characterise these changes to understand fibre functionality.
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- Development and evaluation of performance characteristics of timolol-loaded composite ocular films as potential delivery platforms for treatment of glaucoma. [Journal Article]
- IJInt J Pharm 2019 May 23; 566:111-125
- Thin and erodible polymeric films were developed as potential ocular drug delivery systems to increase drug retention on the eye with the aim of improving bioavailability and achieving controlled dru…
Thin and erodible polymeric films were developed as potential ocular drug delivery systems to increase drug retention on the eye with the aim of improving bioavailability and achieving controlled drug release. Two biocompatible film forming polymers, hyaluronic acid (HA) and hydroxypropyl methylcellulose (HPMC), which are currently used as thickening agents in eye drops were employed. Two different films were prepared (i) as single polymer and (ii) as composite formulations by solvent casting method, incorporating glycerol (GLY) as plasticizer and timolol maleate (TM) as model glaucoma drug. After preliminary optimization of transparency and ease of handling, the formulations were further characterized for their physicochemical properties. No indication of significant drug-polymer or polymer-polymer (in composite films) interaction was observed from FTIR results while evaluation by IR mapping revealed uniform distribution of drug throughout the films. Amorphization of TM in the film matrix was confirmed by both DSC and XRD. Swelling studies illustrated remarkable swelling capacity of HA in comparison with HPMC which directly affected the drug release profiles, making HA a suitable polymer for controlled ocular drug delivery. Tensile and mucoadhesion properties confirmed higher elasticity and adhesiveness of HA while HPMC produced stronger films. The effect of sterilization by UV radiation on mechanical properties was also evaluated and showed no significant difference between the sterilized and non-sterilized films. The SEM results confirmed smoothness and homogeneity of film surfaces for all the formulations studied. The in vitro drug dissolution studies showed more extended release profiles of formulations containing HA. Cytotoxicity study (cell viability) using MTT assay on HeLa cells, confirmed that the single polymer and composite films are generally safe for ocular administration. The present work shows excellent film forming ability of HA and HPMC which can be used as single polymer or combined in composite formulations as potential topical ocular drug delivery platform to enhance drug retention on the ocular surface and therefore potential improved bioavailability.