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1.
Zhongguo Zhong Yao Za Zhi ; 46(15): 3764-3771, 2021 Aug.
Artigo em Chinês | MEDLINE | ID: mdl-34472248

RESUMO

The purpose of the present study was to investigate the relationship of the classification of traditional Chinese medicine(TCM) materials with the suitable binder concentration and dosage in the preparation of personalized water-paste pills and establish a model for predicting the binder concentration and dosage. Five representative TCM materials were selected, followed by mixture uniform design. The water-paste pills were prepared by extrusion and spheronization with hypromellose E5(HPMC E5) as the binder. The quality of intermediates and final products was evaluated, and the resulting data were subjected to multivariate statistical analysis. The prediction models for binder concentration and dosage were established as follows: binder concentration: Y_1=0.378 6 + 0.570 1X_A + 2.271 2X_B-0.894 5X_C-0.458 2X_D-1.145 4X_E(when Y_1 < 0, 10% HPMC E5 was required; when Y_1 > 0, 20% HPMC E5 was required), with the accuracy reaching up to 100%; binder dosage: Y_2=32.38 + 0.25X_A + 1.85X_B-0.013X_B~2-0.002 5X_C~2(R~2=0.932 6, P < 0.001). The results showed that the binder concentration and dosage were correlated positively with the proportion of fiber material but negatively with the proportions of sugar material and brittle material. Then the validation experiments were conducted with the prediction models and all the prescriptions could be successfully prepared at one time. These demonstrated that following the classification of TCM materials and the calculation of their proportions in the prescription, the established mathematical model could be adopted for predicting the binder concentration and dosage required in the preparation of personalized water-paste pills, which contributed to reducing the pre-formulation research and guiding the actual production of personalized water-paste pills.


Assuntos
Medicamentos de Ervas Chinesas , Medicina Tradicional Chinesa , Excipientes , Derivados da Hipromelose , Água
2.
Talanta ; 235: 122747, 2021 Dec 01.
Artigo em Inglês | MEDLINE | ID: mdl-34517615

RESUMO

Microchip capillary electrophoresis (MCE) is a powerful technique for rapid separation; however, its acceptance in routine laboratories is still limited. Compromises caused by the efforts for solving different problems, such as reducing its cost of fabrication and ensuring high separation efficiency, undermine the competitiveness of this technology compared to other separation techniques. Contrary to the conventional pursuit of narrow microchannels, this study investigated the suitability of microchips with channels at the sub-millimeter level, targeting the simplification of the overall operation, cost reduction, and robustness improvement. To this effect, we considered the influence of pressurized flow and Joule heating on the separation. The suppression of pressurized flow with viscous solutions was confirmed through a combination of simulations and experimental results, indicating that the buffer viscosity was enough for successful separation. We fabricated channels of 200 µm × 230 µm using computer numerical controlled (CNC) machining and obtained theoretical plate numbers of 4.8 × 105 m-1 and 5.3 × 105 m-1 for fluorescein isothiocyanate (FITC) labeled small molecules and DNA fragments, respectively, with a buffer viscosity of 168 mPa s (0.5 % hydroxypropyl methylcellulose, HPMC). These values are comparable with that of narrow-bore microchips. Furthermore, we did not observe any deleterious effects with low-conductivity buffers. We investigated the rapid and highly sensitive detection of mycoplasma contamination and the real samples of circulating cell-free DNA (cfDNA), which gave a limit of detection (LOD) as low as 2.3 ng mL-1. Owing to the significant reduction in cost, ease of operation, and fast separation capabilities demonstrated in this work, MCE can be a viable alternative to the usual slab gel electrophoresis running in most biological laboratories.


Assuntos
Eletroforese em Microchip , DNA , Eletroforese Capilar , Derivados da Hipromelose , Limite de Detecção
3.
J Refract Surg ; 37(9): 631-635, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34506235

RESUMO

PURPOSE: To evaluate corneal stiffening in porcine eyes induced by corneal cross-linking (CXL) using riboflavin dissolved in either aqueous dextran or hydroxypropyl methylcellulose (HPMC) solution. METHODS: Fifty-one porcine corneas were divided into three groups of 17 each. After deepithelialization, the first (Dresden) group was treated for 30 minutes with 0.1% riboflavin (riboflavin-5-monophosphate in 0.9% NaCl) dissolved in hypertonic 20% dextran and the second (HPMC) group for 30 minutes with isotonic solution containing 0.1% riboflavin and 1.1% HPMC. Thereafter, corneas of both groups were irradiated using 5.4 J/cm2 (irradiance of 9 mW/cm2 for 10 minutes; 10*9). After CXL, all corneas were kept in an isotonic 16% dextran bath for 2 hours to obtain an equal hydration state. The third group served as the control group. Stress-strain measurements were performed on 5-mm-wide strips. Corneal thickness was monitored throughout the entire course of the experiments. RESULTS: The required stress for a 10% strain was increased by 83% in the Dresden group and 35% in the HPMC group compared to the control group. Resultant Young's modulus (at 10% strain) was 2.53 ± 0.73, 1.87 ± 0.50, and 1.47 ± 0.44 Pa for the Dresden, HPMC, and control groups, respectively. The differences between the Dresden and HPMC groups (P = .006), the Dresden and control groups (P < .001), and the HPMC and control groups (P = .014) were statistically significant. Pachymetry measurements showed a significantly increased corneal thickness after application of HPMC compared with the Dresden group (P = .002) and control group (P = .041). CONCLUSIONS: The biomechanical stiffening of the cornea by CXL can be achieved using dextran- and HPMC-based riboflavin solutions in porcine corneas with an application time of 30 minutes. Dextran-based riboflavin solutions seem to induce a slightly stronger biomechanical response in this setting. HPMC solutions induce less thinning than dextran solutions. [J Refract Surg. 2021;37(9):631-635.].


Assuntos
Substância Própria , Dextranos , Animais , Fenômenos Biomecânicos , Colágeno , Córnea , Reagentes para Ligações Cruzadas , Derivados da Hipromelose , Fármacos Fotossensibilizantes , Riboflavina/farmacologia , Suínos , Raios Ultravioleta
4.
Mater Sci Eng C Mater Biol Appl ; 129: 110211, 2021 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-34579874

RESUMO

In part 1, we have investigated drug release by solid-solution single fibers comprising a sparingly water-soluble drug (ibuprofen) and a highly water-soluble dual excipient (low-molecular-weight hydroxypropyl methyl cellulose (HPMC) and polyoxyl stearate (POS)). In this part, fibrous dosage forms of the same formulation are prepared by 3D-micro-patterning, tested, and modeled. Upon immersion in a small volume of dissolution fluid, the dosage forms rapidly swelled and formed a low-viscosity medium, which subsequently dissolved. The dissolution time increased slightly with volume fraction of the fibers, φs, in the solid dosage form, but was less than 25 minutes even up to φs = 0.65. After dosage form dissolution, the fluid was supersaturated by a factor of two; the drug concentration then gradually decreased to solubility. The solubility was proportional to the concentration of POS, and was enhanced by a factor of six at φs = 0.65 (the most densely-packed dosage form). Theoretical models suggest that the dissolution fluid percolates the contiguous void space almost immediately, and the HPMC-POS fibers expand isotropically as water diffuses in. Because the void space remains contiguous in isotropic expansion, the dissolution fluid continues to percolate through and diffuse into the fibers. Thus, even the densely-packed dosage forms form a low-viscosity medium that deforms and dissolves rapidly. Consequently, the solid-solution fibrous dosage forms enable enhanced release rate, supersaturation, and solubility of sparingly-soluble drugs.


Assuntos
Preparações Farmacêuticas , Formas de Dosagem , Liberação Controlada de Fármacos , Excipientes , Derivados da Hipromelose , Solubilidade
5.
Int J Mol Sci ; 22(17)2021 Aug 30.
Artigo em Inglês | MEDLINE | ID: mdl-34502305

RESUMO

Oral delivery of curcumin (CUR) has limited effectiveness due to CUR's poor systemic bioavailability caused by its first-pass metabolism and low solubility. Buccal delivery of CUR nanoparticles can address the poor bioavailability issue by virtue of avoidance of first-pass metabolism and solubility enhancement afforded by CUR nanoparticles. Buccal film delivery of drug nanoparticles, nevertheless, has been limited to low drug payload. Herein, we evaluated the feasibilities of three mucoadhesive polysaccharides, i.e., hydroxypropyl methylcellulose (HPMC), starch, and hydroxypropyl starch as buccal films of amorphous CUR-chitosan nanoplex at high CUR payload. Both HPMC and starch films could accommodate high CUR payload without adverse effects on the films' characteristics. Starch films exhibited far superior CUR release profiles at high CUR payload as the faster disintegration time of starch films lowered the precipitation propensity of the highly supersaturated CUR concentration generated by the nanoplex. Compared to unmodified starch, hydroxypropyl starch films exhibited superior CUR release, with sustained release of nearly 100% of the CUR payload in 4 h. Hydroxypropyl starch films also exhibited good payload uniformity, minimal weight/thickness variations, high folding endurance, and good long-term storage stability. The present results established hydroxypropyl starch as the suitable mucoadhesive polysaccharide for high-payload buccal film applications.


Assuntos
Quitosana/química , Curcumina/química , Sistemas de Liberação de Medicamentos , Derivados da Hipromelose/química , Mucosa Bucal/química , Nanopartículas/química , Amido/química , Anti-Inflamatórios não Esteroides/química , Quelantes/química , Portadores de Fármacos/química , Humanos , Solubilidade
6.
Int J Pharm ; 607: 120984, 2021 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-34389423

RESUMO

Probucol (PBC)/hypromellose (HPMC)/sodium dodecyl sulfate (SDS) ternary solid dispersions (SDs) of various weight ratios were prepared and evaluated to unveil the effect of HPMC and SDS on the formation of amorphous PBC nanoparticles. The morphological variation of the PBC nanoparticles prepared using SDs of different compositions was determined using dynamic light scattering and cryogenic transmission electron microscopy (cryo-TEM). Statistical analysis of particle size versus roundness of PBC nanoparticles was carried out based on cryo-TEM images. A clear correlation was observed between the morphologies of the PBC nanoparticles and the amounts of HPMC and SDS, either admixed in SDs or pre-dissolved in an aqueous solution. The admixed HPMC in SDs was demonstrated to play the major role in determining the primary particle sizes of discrete amorphous PBC nanoparticles. Based on 13C solid-state NMR spectroscopy, this phenomenon should be due to the enlarged size of the PBC-rich domains in SDs, which depended on the decreasing amounts of admixed HPMC. Although the pre-dissolved part of HPMC had less impact on the primary particle sizes, it was found to inhibit the particle agglomeration and recrystallization of amorphous PBC nanoparticles. On the other hand, sufficient SDS admixed in SDs could suppress the size enhancement of the PBC-rich domains during water immersion and nanoparticle evolution (agglomeration and crystallization) after aqueous dispersion. The pre-dissolved SDS could restrain the agglomeration of amorphous PBC nanoparticles, ultimately forming hundreds of irregular nanometer-order structures. Since the increase in size during water immersion, their sizes were still slightly larger than those obtained with a high portion of admixed SDS. The findings of this study clarified the usefulness and necessity of adding polymers and surfactants to SDs to fabricate drug nanoparticle formulations.


Assuntos
Nanopartículas , Preparações Farmacêuticas , Derivados da Hipromelose , Tamanho da Partícula , Solubilidade , Água
7.
Int J Pharm ; 607: 121005, 2021 Sep 25.
Artigo em Inglês | MEDLINE | ID: mdl-34391855

RESUMO

Hydrophilic matrices are of utmost interest for oral prolonged release of drugs. However, they show decreasing release rate over time, mainly due to lengthening of the diffusional pathway across the gel formed upon glass-rubber transition of the polymer. Therefore, achievement of zero-order release kinetics, which could reflect in constant drug plasma levels, is still an open issue. With the aim of improving the release performance of hydroxypropyl methylcellulose (HPMC) systems, the use of cellulolytic enzymes was proposed to aid erosion of the swollen matrix, thereby counteracting the release rate decrease particularly toward the end of the process. The effectiveness of this strategy was evaluated by studying the mass loss and drug tracer release from tableted matrices consisting of high-viscosity HPMC (Methocel® K4M), Acetaminophen and increasing amounts (0.5-10% on HPMC) of a cellulolytic product (Sternzym® C13030). A faster erosion and progressive shift to linearity of the overall release profiles were observed as a function of the enzyme concentration. Release was markedly linear from matrices containing 5 and 10% Sternzym® C13030. In partially coated matrices with these cellulase concentrations, such results were in agreement with data of erosion and swelling front movement, which exhibited early and long-lasting synchronization.


Assuntos
Celulase , Excipientes , Química Farmacêutica , Preparações de Ação Retardada , Derivados da Hipromelose , Cinética , Metilcelulose , Solubilidade , Comprimidos
8.
J Pharm Biomed Anal ; 205: 114303, 2021 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-34391134

RESUMO

A new tioconazole (TCZ) mucoadhesive film, based on a biodegradable chitosan/ hydroxypropyl methylcellulose (CH/HPMC) blend, was developed for treatment of vaginal candidiasis. The formulation was optimized through an I-optimal design (minimizing the integral of the prediction variance across the factor space), where the impact of the proportion of the ingredients and processing variables on the quality of the final product was evaluated. Both, the thickness of the film and the swelling index, which affect patients' comfort and compliance, were considered. Mechanical testing, such as load at break, elongation at break, and mucoadhesive strength were also included as dependent variables. The optimal mucoadhesive film formulation, which should be obtained at a drying temperature of 30 °C, was found to include the combination of CH and HPMC (forming polymers) at 0.25:0.75 ratio, a mixture of polyethylene glycol 400 and propylene glycol as plasticizers (0.07:0.93, 5% w/w), and TCZ loaded at 15 % w/w. The optimal preparation was subjected to exhaustive characterization studies, which revealed that the drug was entrapped in the polymeric matrix in an amorphous state and that the film exhibited a smooth and uniform surface, demonstrating excellent component compatibility. In vitro tests showed that the formulation has an excellent time to kill value (3 min) and lacks cytotoxicity, suggesting that it should be highly effective and safe.


Assuntos
Imidazóis , Projetos de Pesquisa , Feminino , Humanos , Derivados da Hipromelose , Polímeros
9.
Arch Oral Biol ; 129: 105210, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34293645

RESUMO

OBJECTIVE: This study aimed to investigate the efficacy of double antibiotics, including ciprofloxacin and metronidazole, in a new vehicle, hydroxypropyl methylcellulose (HPMC), against Enterococcus faecalis and Streptococcus gordonii grown in biofilm. DESIGN: Human mandibular premolars were prepared and divided into four groups: (i) negative control, (ii) positive control, (iii) infected with E. faecalis and S. gordonii for 21 days and intracanally medicated with double antibiotics in HPMC, and (iv) infected with E. faecalis and S. gordonii for 21 days and intracanally medicated with calcium hydroxide (UltraCal™). The efficacy of medication for 14 or 28 days was determined by bacterial cultures and RT-qPCR for absolute quantities of E. faecalis and S. gordonii cDNA and for relative mRNA expressions of pbp5 and gtfG genes. RESULTS: There were significant decreases in the mean colony forming units and mean cDNA amounts of E. faecalis and S. gordonii in group (iii) on days 14 and 28 compared to those in group (ii) (p < 0.01). However, the mean cDNA amounts of E. faecalis and S. gordonii in group (iv) were found to be significantly increased on day 28 (p < 0.05). The mRNA expression of gtfG was significantly decreased in groups (iii) and (iv) on days 14 and 28, whereas that of pbp5 was significantly increased in group (iv) on days 14 and 28 (p < 0.01). CONCLUSION: Double antibiotics in HPMC gel showed an in vitro efficacy against E. faecalis and S. gordonii grown in biofilm, suggesting its clinical application as an intracanal medicament for both primary and persistent infections.


Assuntos
Enterococcus faecalis , Streptococcus gordonii , Antibacterianos/farmacologia , Biofilmes , Hidróxido de Cálcio , Cavidade Pulpar , Humanos , Derivados da Hipromelose , Irrigantes do Canal Radicular
10.
Int J Biol Macromol ; 184: 666-677, 2021 Aug 01.
Artigo em Inglês | MEDLINE | ID: mdl-34146561

RESUMO

The roselle anthocyanin extracts (RAE) were immobilized into polyvinyl alcohol (PVA)/hydroxypropyl methylcellulose (HPMC) film matrix, their interaction behavior and mechanism was fully understood for better shrimp freshness monitoring. Structural characterizations revealed RAE was firmly immobilized PVA/HPMC matrix by hydrogen bonds. With increasing RAE contents, dramatic increases of film thickness (from 15.90 ± 0.14 to 23.20 ± 3.35 µm), tensile strength (from 45.66 ± 1.07 to 56.98 ± 0.24 MPa), light barrier and active properties (increased by 83.18% for antioxidant and 146.91%, 59.18% for antibacterial activity against E. coli and S. aureus) were observed, while hydrophobic properties decreased significantly. Owing to great ammonia-sensitive ability, the PVA/HPMC/RAE (PHR) films were applied on shrimp freshness qualitative monitoring and greater visible color variations were identified with increasing RAE contents. Furthermore, mathematical models were established for quantitative monitoring. In conclusion, with the increasing RAE contents, the tighter interaction between RAE and PVA/HPMC matrix contributed to the better functional properties and freshness monitoring effects of PHR films.


Assuntos
Antocianinas/farmacologia , Antibacterianos/farmacologia , Antioxidantes/farmacologia , Hibiscus/química , Derivados da Hipromelose/química , Álcool de Polivinil/química , Antocianinas/química , Antibacterianos/química , Antioxidantes/química , Escherichia coli/efeitos dos fármacos , Embalagem de Alimentos , Ligação de Hidrogênio , Concentração de Íons de Hidrogênio , Testes de Sensibilidade Microbiana , Modelos Teóricos , Alimentos Marinhos/microbiologia , Staphylococcus aureus/efeitos dos fármacos , Resistência à Tração
11.
Int J Pharm ; 604: 120769, 2021 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-34089795

RESUMO

Cellulosic-based thickeners are commonly used in the preparation of hydro-alcoholic hand sanitisers. Yet, little is known about the behaviour of these polymeric dispersions in hydro-alcoholic mixtures. Here, we studied the dispersion ability and rheology of hydroxyethyl cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose and sodium carboxymethyl cellulose in water-ethanol mixtures. Hydroxypropyl cellulose formed transparent dispersions across the entire range of ethanol concentrations, while a critical ethanol concentration (CEC), above which dispersions became turbid, was found for all the other polymers. At and below the CEC, all the rheological parameters followed a bell-like shape profile as a function of ethanol concentration. Moreover, the molecular weight and degree of substitution of the polymers influenced the rheological properties. The CEC and rheological behaviour of the dispersions were both dependent on the ethanol/polymer and water/polymer interactions. As hand disinfectants should contain 60-95% ethanol, polymers of higher CEC, such as hydroxypropyl cellulose and hydroxypropyl methylcellulose, are recommended.


Assuntos
Higienizadores de Mão , Géis , Derivados da Hipromelose , Reologia , Viscosidade
12.
Int J Biol Macromol ; 183: 2314-2325, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34087300

RESUMO

Novel peppermint oil (PO)-loaded composite microcapsules (CM) with hydroxypropyl methyl cellulose (HPMC)/chitosan/silica shells were effectively fabricated by PO Pickering emulsion, which were stabilized with chitosan-decorated silica nanoparticles (CSN). The surface modification of chitosan could improve the hydrophobicity of silica nanoparticles and favor their adsorption at the oil-water interface of PO Pickering emulsions. The microcapsule composite shells were formed dependent on the electrostatic adsorption of HPMC and CSN, and further subjected to spray-drying. The peppermint oil-loaded composite microcapsules with 100% HPMC as wall material (PO-CM@100%HPMC) seemed to be optimum formulation based on the prolonged release, acceptable entrapment efficiency (89.1%) and drug loading (25.5%). The PO-CM@100%HPMC could remarkably prolong the stability of PO. Moreover, the PO-CM@100%HPMC had a long-term antimicrobial activity (85.4%) against S. aureus and E. coli even after storage for 60 days. Therefore, the Pickering emulsions based microcapsules seemed to be a promising strategy for antibacterial application for PO.


Assuntos
Antibacterianos/farmacologia , Quitosana/química , Portadores de Fármacos , Escherichia coli/efeitos dos fármacos , Nanopartículas , Óleos Vegetais/farmacologia , Dióxido de Silício/química , Staphylococcus aureus/efeitos dos fármacos , Adsorção , Antibacterianos/química , Cápsulas , Preparações de Ação Retardada , Composição de Medicamentos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Emulsões , Escherichia coli/crescimento & desenvolvimento , Interações Hidrofóbicas e Hidrofílicas , Derivados da Hipromelose/química , Óleos Vegetais/química , Staphylococcus aureus/crescimento & desenvolvimento , Fatores de Tempo
13.
AAPS PharmSciTech ; 22(5): 181, 2021 Jun 15.
Artigo em Inglês | MEDLINE | ID: mdl-34129154

RESUMO

In this study, two hydrophilic polymers hydroxypropyl methyl cellulose and beta-cyclodextrin (ß-CD) are used to synthesize highly responsive and spongy polymeric matrices. Porous and stimulus-responsive polymeric network was developed to improve the solubility of acyclovir (ACV) at significant level. Grafting was successfully carried out by free radical polymerization technique. Spongy matrices were characterized by percentage entrapment efficiency, drug loading, solubility studies, FTIR, powder X-ray diffraction, TGA, DSC, XRD, SEM, swelling studies, and in vitro studies. Acute oral toxicity studies were conducted to determine the safety of oral administration of prepared HPMC-ßCD-g-poly(AMPS) formulation. Porous and spongy structures were depicted in SEM images. Complex formation and thermal stability of constituents and drug (ACV) were analyzed by FTIR, TGA, and DSC spectra. XRD analysis revealed reduction in acyclovir crystallinity in spongy matrices. Particle size of optimized formulation was found in the range of 197 ± 2.55 nm. The momentous difference with reference product committed that drug solubility and release characteristics were markedly enhanced by the developed spongy matrices. Toxicity studies endorsed that developed spongy matrices were non-toxic and compatible to biological system. The efficient method of preparation, enhanced solubility, excellent physico-chemical characteristics, high dissolution, and non-toxic HPMC-ßCD-g-poly(AMPS) spongy matrices may be a promising approach for oral delivery of poorly soluble drugs.


Assuntos
Acrilamidas/síntese química , Aciclovir/síntese química , Alcanossulfonatos/síntese química , Derivados da Hipromelose/síntese química , Polimerização , beta-Ciclodextrinas/síntese química , Acrilamidas/administração & dosagem , Aciclovir/administração & dosagem , Administração Oral , Alcanossulfonatos/administração & dosagem , Animais , Antivirais/administração & dosagem , Antivirais/síntese química , Avaliação Pré-Clínica de Medicamentos/métodos , Derivados da Hipromelose/administração & dosagem , Masculino , Tamanho da Partícula , Polímeros/administração & dosagem , Polímeros/síntese química , Coelhos , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Difração de Raios X/métodos , beta-Ciclodextrinas/administração & dosagem
14.
Anticancer Res ; 41(6): 2759-2772, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34083266

RESUMO

The intestinal microbiota, which has gained a foothold in the field of research, represents a significant factor for human health because of its ability to form relationships with the organism through the modulation of pathophysiological processes. Dysbiosis, which is caused by non-specific intestinal inflammation and leads to a condition of persistent low-grade inflammation, may be caused by poor eating habits and an unhealthy lifestyle, as well as psycho-physical stress and a sedentary lifestyle. Diet, prebiotics and probiotics, and moderate and aerobic exercise can, in order to increase well-being and reduce the chance of recurrence, all be deemed effective methods of improving gut-microbiota pretreatment or mitigating diseases or dysbiosis. This study shows the ways in which good living habits, correct nutrients, and constant aerobic activity in chronic and immune conditions, can modify gut microbiota and microbiome characteristics, as well as the relationship between intestinal function and human health.


Assuntos
Dieta , Exercício Físico , Microbioma Gastrointestinal , Probióticos , Humanos , Derivados da Hipromelose
15.
Colloids Surf B Biointerfaces ; 205: 111877, 2021 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-34049001

RESUMO

In this investigation, we integrated the parent recurring sequence of the plastic-derived polypeptide, poly[0.8(AVGVP),0.2(AEGVP)] (A, V, G, P, and E represents Alanine, Valine, Glycine, Proline, and Glutamic acid respectively) followed by characterization with inverse transition temperature, 13C, and 1H-NMR spectroscopy. The miscibility attributes of poly[0.8(AVGVP),0.2(AEGVP)] with Hydroxypropylmethylcellulose was examined both in aqueous and solid-phase. The Huggins' co-efficient [KH], the intrinsic viscosity [η], the interaction parameters ΔB and µ suggested by Chee, ΔK and ß recommended by Jiang and Han, α by Sun, Δ[η]m by Garcia showed that the polypeptide was miscible with HPMC in all proportions. DSC studies revealed single Tg values, and TGA manifested the enhanced thermal stability for all the proportions compared with their individuals. Further, verified the results by SEM and XRD. The FTIR evidenced existence of intermolecular hydrogen bonding between the two constituent polymers that caused the miscible blend system.


Assuntos
Plásticos , Polímeros , Varredura Diferencial de Calorimetria , Humanos , Derivados da Hipromelose , Peptídeos , Espectroscopia de Infravermelho com Transformada de Fourier , Viscosidade
16.
Biochem Biophys Res Commun ; 560: 105-111, 2021 06 30.
Artigo em Inglês | MEDLINE | ID: mdl-33984767

RESUMO

Anti-prion effects of cellulose ether (CE) are reported in rodents, but the molecular mechanism is fully unknown. Here, we investigated the genetic background of CE effectiveness by proteomic and genetic analysis in mice. Proteomic analysis in the two mouse lines showing a dramatic difference in CE effectiveness revealed a distinct polymorphism in the glia maturation factor ß gene. This polymorphism was significantly associated with the CE effectiveness in various prion-infected mouse lines. Sequencing of this gene and its vicinity genes also revealed several other polymorphisms that were significantly related to the CE effectiveness. These polymorphisms are useful as genetic markers for finding more suitable mouse lines and exploring the genetic factors of CE effectiveness.


Assuntos
Fator de Maturação da Glia/genética , Derivados da Hipromelose/uso terapêutico , Doenças Priônicas/tratamento farmacológico , Animais , Encéfalo/metabolismo , Marcadores Genéticos , Genômica , Masculino , Camundongos , Polimorfismo Genético , Doenças Priônicas/genética , Doenças Priônicas/metabolismo , Proteômica
17.
Int J Biol Macromol ; 183: 1210-1221, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-33984383

RESUMO

Silk fibroin (SF) is a natural macromolecule material with good biocompatibility, which can be used to prepare a variety of biological materials. In this study, hydroxypropyl methylcellulose (HPMC) was applied to improve the properties of SF nanofibrous scaffolds (NFS) for skin tissue engineering applications. SF/HPMC NFS with varying weight ratios of SF: HPMC were prepared in batches by a modified free surface electrospinning. The effects of the varying weight ratio of SF: HPMC on the morphology, property and yield of SF/HPMC NFS were investigated. The results revealed that with the increase of HPMC contents, the hydrophilicity of SF/HPMC NFS would be improved, but the yield of that would decrease. Considering its effects on the morphology, property and yield of SF/HPMC NFS, the optimal weight ratio of SF: HPMC was 7:1. And SF/HPMC NFS with the weight ratio of 7:1 (SF/HPMC-7:1 NFS) had good mechanical property, hydrophilicity, porosity, swelling property and water vapor transmission rate (WVTR). In addition, the viability test results of human umbilical vein endothelial cells demonstrated that SF/HPMC-7:1 NFS maintained excellent biocompatibility for cell adhesion and proliferation.


Assuntos
Fibroínas/química , Derivados da Hipromelose/química , Tecidos Suporte/química , Adesão Celular , Proliferação de Células , Células Endoteliais da Veia Umbilical Humana , Humanos , Microscopia Confocal , Microscopia Eletrônica de Varredura , Nanofibras , Porosidade , Fenômenos Fisiológicos da Pele , Engenharia Tecidual , Molhabilidade
18.
Int J Pharm ; 605: 120726, 2021 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-34029664

RESUMO

In the design of abuse-deterrent formulations (ADFs), pharmaceutical strategies that do not modify the physical and chemical properties of opioid dosage forms should be investigated. Among these, four major drug abusing factors, including particle size by physical modification, swellability, dissolution rate, and solvent extraction, were mainly characterized for evaluating abuse deterrence of narcotics. Tramadol hydrochloride (TMD) was chosen as a model drug. In this study, the frequently used eight generally recognized as safe (GRAS)-listed pharmaceutical excipients, including polyvinyl alcohol (PVA), hydroxypropyl methylcellulose (HPMC 4,000, HPMC 100,000), xanthan gum (XG), cellulose acetate (CA), polyethylene oxide (PEO), carbomer 940 NF, and Compritol® 888 ATO, were selected as abuse deterring agents and used to prepare TMD-loaded tablet. A new abuse-deterrent index (ADI) for compressed TMD-loaded tablets was originally defined and considered as an index of drug abuse deterrence, based on the assumption that it was proportional to particle size and swellability but inversely proportional to dissolution and solvent extraction rates after assigning the categorized five scale scores (one to five) to the four experimental data. The resulting ADI of the selected eight abuse deterring agents in deionized water was given in decreasing order: HPMC 4000 > carbomer 940 > Compritol® 888 ATO > XG > PVA > HPMC 100,000 > PEO, and CA while in 40% hydro-alcoholic solution in the decreasing order: carbomer 940 > HPMC 4,000 ≒ XG > PVA > HPMC 100,000 > PEO > Compritol® 888 ATO > CA. Interestingly, the HPMC 4,000 and carbomer 940 showed the highest ADI and gave drug abuse deterrent potential. This study could provide a pharmaceutical strategy that utilizes a variety of abuse-deterring agents and resist to extraction solvents in designing drug abuse-deterrent formulations and establishing their standard guidelines for regulatory authorities.


Assuntos
Tramadol , Preparações de Ação Retardada , Composição de Medicamentos , Excipientes , Derivados da Hipromelose , Comprimidos
19.
Int J Biol Macromol ; 183: 1732-1742, 2021 Jul 31.
Artigo em Inglês | MEDLINE | ID: mdl-34051251

RESUMO

Oral montelukast (MTK) is prescribed to treat asthma or rhinitis, and is clinically investigated as new medication in the treatment of Alzheimer's dementia. Herein, in order to better patient's compliance, microsuspensions (MSs)-based oral liquid preparations of montelukast (MTK) were formulated with polymeric suspending agents including hypromellose (HPMC), and those drug-polymer interaction, physicochemical stability, dissolution, and in vivo pharmacokinetic profile was evaluated. When amorphous MTK particle was suspended in aqueous vehicle, it was readily converted into crystalline form and grown into aggregates, drastically lowering dissolution rate. However, the addition of HPMC polymer markedly suppressed the crystal growth, providing both improved drug stability and profound dissolution profile. Raman spectrometry denoted the inter-molecular hydrogen boding between MTK particle and HPMC polymer. The crystal growth or dissolution profile of MSs was markedly affected by pharmaceutical additives (sucrose or simethicone) in the preparations or storage temperature. The optimized HPMC-based MS exhibited over 80% higher bioavailability, compared to marketed granule (Singulair®) in rats. Therefore, novel MTK-loaded MS can be a promising liquid preparation, bettering oral absorption and patient's compliance.


Assuntos
Acetatos/administração & dosagem , Ciclopropanos/administração & dosagem , Derivados da Hipromelose/química , Quinolinas/administração & dosagem , Sulfetos/administração & dosagem , Acetatos/química , Acetatos/farmacocinética , Administração Oral , Animais , Cristalização , Ciclopropanos/química , Ciclopropanos/farmacocinética , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Ligação de Hidrogênio , Masculino , Quinolinas/química , Quinolinas/farmacocinética , Ratos , Solubilidade , Sulfetos/química , Sulfetos/farmacocinética , Suspensões
20.
Int J Pharm ; 604: 120718, 2021 Jul 15.
Artigo em Inglês | MEDLINE | ID: mdl-34048929

RESUMO

A commonly used approach to enhance the dissolution of drugs with pH-dependent solubility is the incorporation of pH modifiers. The aim of this study was to evaluate the duration and extent of pH modifying effect on the micro-environmental pH in HPMC matrix by applying two mechanistic approaches regarding hydrodynamic stress on the tested formulation (i.e. static dissolution apparatuses (USP2) and dynamic approaches including the Advanced gastric simulator (AGS) and the Intestinal model for simulation of peristaltic action (IMSPA)). Moreover, the aim of our research was also the preparation of sustained-release matrix systems with improved - enhanced drug dissolution. In our study, the occurrence of a pH gradient in the gel layer of the HPMC tablets was observed during simulation of their passage along different compartments of the GIT. The pH gradient was affected by the media composition and duration of tablet exposure to the surrounding media. Both dissolution methods were also used to evaluate the influence of the mechanical stress on the drug release kinetics. Micro-environmental pH (pHM) was evaluated, using two methods: the cryostatic method with a surface pH electrode, and with the incorporation of a pH sensitive dye (methyl orange) into the matrix tablets. Our study demonstrates a significantly higher dissolution rate due to mechanical stress during the bio-relevant simulation of GIT transit of the mechanically sensitive HPMC tablets with poorly soluble drugs. A considerably higher release rate was also observed from tablets with the weakly basic drugs dipyridamole and propranolol hydrochloride containing pH modifier in case of mechanically bio-relevant dissolution models compared to the USP2 apparatus. For the assessment of the pHM, the incorporation of a pH indicator dye in the HPMC tablet proved to be more suitable, while the cryostatic method was found to be useful only for a rough pHM estimation.


Assuntos
Trânsito Gastrointestinal , Metilcelulose , Preparações de Ação Retardada , Concentração de Íons de Hidrogênio , Derivados da Hipromelose , Lactose/análogos & derivados , Metilcelulose/análogos & derivados , Solubilidade , Comprimidos
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