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1.
Int J Pharm ; 643: 123243, 2023 Aug 25.
Artigo em Inglês | MEDLINE | ID: mdl-37463620

RESUMO

Complexation of nicotine (NCT) and magnesium aluminum silicate (MAS) has been formed in the dispersions that required multiple preparation steps. In this study, physical blending was used to produce NCT-MAS complexes. NCT, a free-base liquid state form, was adsorbed onto the MAS granules, where the diffusion and intercalation of NCT molecules into the MAS silicate layers occurred. These processes required a minimum of the 7-d-resting period to reach NCT complete distribution. FTIR, XRD, and 29Si NMR suggest that NCT could interact with MAS via hydrogen bonding, water bridging, and ionic electrostatic force. The 12 % NCT-MAS complexes enabled a sustained release of NCT, after a 2-min burst, in pH 6 phosphate buffer through a particle diffusion-controlled mechanism. Buccal discs formulated with NCT-MAS complexes and sodium alginate (SA) as drug carriers and matrix former could control NCT released through drug diffusion and swelling-controlled mechanisms. NCT release and membrane permeation increased with increasing NCT-MAS complexes or decreasing SA concentration. All NCT-MAS-containing buccal discs exhibited mucoadhesive properties related to the swelling characteristics of SA and MAS. Conclusively, NCT-MAS complexes can be produced through an uncomplicated single-step blending process, and the complexes obtained presented a potential to serve as drug carriers in buccal matrix formulations.


Assuntos
Portadores de Fármacos , Nicotina , Nicotina/química , Silicatos/química , Compostos de Magnésio/química , Compostos de Alumínio/química , Alginatos/química
2.
Pharmaceutics ; 15(1)2023 Jan 12.
Artigo em Inglês | MEDLINE | ID: mdl-36678892

RESUMO

Diarylheptanoids (DAs) characterized by a 1,7-diphenylheptane structural skeleton are considered a novel class of phytoestrogens. The DAs available in Curcuma comosa Roxb. (C. comosa) extract demonstrated significant estrogenic activities both in vitro and in vivo. This study aimed to develop and comprehensively evaluate a mucoadhesive vaginal gel for the sustained release of DAs. Different mucoadhesive polymers as gelling agents were investigated. C. comosa ethanolic crude extract was used as a source of DAs. All C. comosa gels were light brown homogeneous with pH within 4.4-4.6. Their flow behaviors were pseudoplastic with a flow behavior index of 0.18-0.38. The viscosity at a low shear rate varied from 6.2 to 335.4 Pa·s. Their mechanical and extrudability properties were associated well with rheological properties. Polycarbophil (PCP):hydroxypropyl methylcellulose (HPMC) blends had a higher mucoadhesiveness to porcine vaginal mucosa than those of PCP-based or HPMC-based gels. All C. comosa gels exhibited a sustained, zero-order DA release pattern over 72 h. Korsmeyer and Peppas equation fitting indicated a non-Fickian, case II transport release mechanism. C. comosa gels had good physical and chemical stability under low-temperature storage for up to 12 months. PCP:HPMC-based mucoadhesive gels could be a proper delivery system for vaginal administration of DAs.

3.
Gels ; 8(11)2022 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-36421561

RESUMO

The objective of this work was to examine the effect of quaternary polymethacrylate (QPM), a water-insoluble polymer with a positive charge, on the characteristics of the sodium alginate (SA) dispersions and the calcium alginate (CA) gel beads containing propranolol HCl (PPN). The SA-QPM composite dispersions presented the formation of flocculates with a negative charge due to the electrostatic interaction of both substances. The QPM addition did not affect the SA dispersions' Newtonian flow, but the composite dispersions' viscosity enhancement was found. The PPN-loaded CA-QPM gel beads had more spherical than the PPN-loaded CA gel beads. The incorporation of QPM caused a bigger particle size, higher drug entrapment efficiency, and greater particle strength of the gel beads. Despite the similar water uptake property, the PPN-loaded CA-QPM gel beads displayed lower burst release and slower drug release rate than the PPN-loaded CA gel beads. However, the drug release from the PPN-loaded CA-QPM gel beads involved drug diffusion and matrix swelling mechanisms. This study demonstrated that adding QPM into the SA dispersions leads to a viscosity synergism. The CA-QPM gel beads display a good potential for use as a bioactive compound delivery system.

4.
Pharmaceutics ; 14(11)2022 Nov 08.
Artigo em Inglês | MEDLINE | ID: mdl-36365225

RESUMO

This study demonstrated the implementation of a liquisolid technique to formulate directly compressible orally disintegrating tablets (ODTs). Cannabidiol (CBD), a hydrophobic cannabinoid, was prepared as a liquisolid powder using microcrystalline cellulose-colloidal silicon dioxide as a carrier-coating material. Different liquid vehicles differing in their volatility, hydrophilicity, and viscosity were investigated. Each of the CBD-ODTs comprised CBD liquisolid powder (10 mg CBD), superdisintegrant, flavors, lubricant, and filler. The physical mixture (PM) ODT was prepared as a control. Ethanol-based ODTs (CBD-EtOH-ODTs) had comparable tablet properties and stability to CBD-PM-ODTs. ODTs with nonvolatile-vehicle-based liquisolid powder had lower friability but longer disintegration times as compared with CBD-PM-ODTs and CBD-EtOH-ODTs. Compression pressure influenced the thickness, hardness, friability, and disintegration of the ODTs. With a suitable compression pressure to yield 31-N-hardness-ODTs and superdisintegrant (4-8%), CBD-ODTs passed the friability test and promptly disintegrated (≤25 s). Times to dissolve 50% of CBD-PM-ODTs, CBD-EtOH-ODTs, and nonvolatile-vehicle-based CBD-ODTs were 10.1 ± 0.7, 3.8 ± 0.2, and 4.2 ± 0.4-5.0 ± 0.1 min, respectively. CBD-EtOH-ODTs exhibited the highest dissolution efficiency of 93.5 ± 2.6%. Long-term and accelerated storage indicated excellent stability in terms of tablet properties and dissolution. Nonvolatile-vehicle-based CBD-ODTs exhibited a higher percentage of remaining CBD. This study provides useful basic information for the development of ODT formulations using a liquisolid technique application.

5.
Pharmaceutics ; 14(9)2022 Aug 26.
Artigo em Inglês | MEDLINE | ID: mdl-36145536

RESUMO

This work investigated the influence of liquid vehicles on the release, mucosal permeation and deposition of cannabidiol (CBD) from liquisolid systems. Various vehicles, including EtOH, nonvolatile low- and semi-polar solvents, and liquid surfactants, were investigated. The CBD solution was converted into free-flowing powder using carrier (microcrystalline cellulose) and coating materials (colloidal silica). A physical mixture of the CBD and carrier-coating materials was prepared as a control. The non-crystalline state of CBD in the liquisolid systems was confirmed using XRD, FTIR and SEM studies. The CBD liquisolid powder prepared with volatile and nonvolatile solvents had a better CBD release performance than the CBD formed as the surfactant-based and control powders. The liquisolid systems provided the CBD permeation flux through porcine esophageal mucosa ranging from 0.68 ± 0.11 to 13.68 ± 0.74 µg·cm-2·h-1, with the CBD deposition levels of 0.74 ± 0.04 to 2.62 ± 0.30 µg/mg for the dry mucosa. Diethylene glycol monoethyl ether showed significant CBD permeation enhancement (2.1 folds) without an increase in mucosal deposition, while the surfactants retarded the permeation (6.7-9.0 folds) and deposition (1.5-3.2 folds) significantly. In conclusion, besides the drug release, liquid vehicles significantly influence mucosal permeation and deposition, either enhanced or suppressed, in liquisolid systems. Special attention must be paid to the selection and screening of suitable liquid vehicles for liquisolid systems designed for transmucosal applications.

6.
Pharmaceutics ; 14(8)2022 Aug 13.
Artigo em Inglês | MEDLINE | ID: mdl-36015313

RESUMO

In this study, the mucosal permeation and deposition of cannabidiol (CBD) with neat and binary vehicles were investigated. Permeation experiments were performed using static diffusion cells coupled with fresh porcine esophageal mucosa. The CBD-vehicle solutions were applied at a fixed dose (~5 mg/cm2), and the corresponding permeation parameters were calculated. In neat vehicles, the permeation flux (Jss) ranged from 0.89 ± 0.15 to 179.81 ± 23.46 µg·cm-2·h-1, while the CBD deposition ranged from 11.5 ± 1.8 to 538.3 ± 105.3 µg·cm-2. Propylene glycol (PG) and diethylene glycol monoethyl ether (DEGEE) yielded the highest permeability (Ps) and CBD deposition, while medium-chain triglycerides (MCT) yielded the lowest Ps and deposition. This was due to the difference in apparent partition coefficient (K), which is related to the solubility of CBD in the vehicle. The PG:DEGEE binary vehicle boosted Jss (1.5-1.6 fold) and deposition (2.0-2.7 folds) significantly, compared to neat DEGEE. The combination of DEGEE with MCT dramatically enhanced Jss (11-44 fold) and deposition (1.6-4.7 fold). The addition of lipophilic enhancers, laurocapram, and oleic acid, to PG:DEGEE and DEGEE:MCT vehicles significantly reduced Jss (0.3-0.7 fold) and deposition (0.4-0.8 fold) while nerolidol had no effect. These permeation reductions were found to be related to modification of the K and/or diffusivity values. This study provides useful basic information for the development of CBD formulations intended for transmucosal delivery.

7.
Pharmaceutics ; 14(8)2022 Aug 18.
Artigo em Inglês | MEDLINE | ID: mdl-36015349

RESUMO

Denture stomatitis is induced by irritation or an inflammatory response when wearing a denture for a long time. Candida species are the leading cause of biofilm formation on the surfaces and fissures of dentures. Thus, this study aimed to formulate and evaluate fluconazole tablets for use in preparing a disinfectant mixture with anticandidal activity. For size enlargement of lactose, a tablet diluent, using polyvinylpyrrolidone (PVP) as an agglomerating agent, was developed to enhance the flowability and compactability of the tablet preparation using direct compression. Lactose agglomerates with 6% PVP were used as a diluent for the fluconazole tablets. Furthermore, other excipients were used, such as a buffering agent, disintegrant, surfactant, and lubricant. The fluconazole tablets obtained could be dispersed and dissolved within 10 min in distilled water to achieve a clear mixture, providing a neutral pH and 96% transmittance. Furthermore, the fluconazole mixtures displayed anticandidal efficiency against C. albicans with a similar effect to the standard fluconazole solution. These findings suggest that the fluconazole-loaded lactose agglomerate tablets show strong potential when prepared using direct compression. The fluconazole mixtures made by dispersing the tablets can be used as a disinfectant for Candida-associated dentures, particularly in patients with oral candidiasis.

8.
Pharmaceutics ; 14(6)2022 Jun 12.
Artigo em Inglês | MEDLINE | ID: mdl-35745817

RESUMO

Acid-modified tapioca starches (AMTSs) possessed good compressibility but showed poor particle flowability for preparing tablets by the direct compression method. The aims of this work were to prepare and characterize AMTS agglomerates using polyvinylpyrrolidone (PVP) as an agglomerating agent. The dilution potential and stability studies of the AMTS agglomerates were investigated. The results showed that particle enlargement of TS and AMTS could be achieved via agglomeration using PVP. The thermal behavior and molecular interaction of the agglomerates were revealed using DSC and FTIR spectroscopy, respectively. An increase in PVP concentrations resulted in greater particle strength of the TS agglomerates and a higher acid concentration for modification enhanced the strength of the AMTS agglomerates. All agglomerates presented good particle flowability. Moreover, the AMTS agglomerates provided higher compressibility hardness than the TS agglomerates. The addition of PVP could extend the disintegration time and slow drug dissolution from the agglomerate tablets. The humidity of the storage conditions influenced the thickness and hardness of the AMTS agglomerate tablets, and good physical and chemical stability of the tablets was obtained under ambient conditions and in the refrigerator. Furthermore, the AMTS agglomerates displayed good carrying capacity and possessed desirable characteristics for use in direct compression tablets.

9.
Carbohydr Polym ; 245: 116556, 2020 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-32718644

RESUMO

The fabrication and characterization of ball-milling modified glutinous rice starch (MGRS):chitosan (CS) composite films were demonstrated. Effect of CS ratios (2:1, 1:1, 1:2 MGRS:CS) on the film properties was investigated. Lidocaine hydrochloride was used as a model hydrophilic drug. ATR-FTIR confirmed hydrogen bond formation between MGRS and CS. XRD indicated an amorphous state of all fabricated films. The uniform and comparable thickness, weight, and drug contents of all fabricated films were obtained. The presence of CS did not affect the mucoadhesiveness of MGRS films. The increase in tensile strength and decreases in elongation and folding endurance were observed with 1:2 MGRS:CS films. The film swelling and drug release decreased with the CS ratio. Drug permeation across porcine mucosa indicated the enhancement effect of CS, whereby the permeation flux of 1:2 MGRS:CS composite increased by 3 folds. In conclusion, the MGRS:CS composite could be useful for buccal delivery of hydrophilic drug.


Assuntos
Anestésicos Locais/farmacologia , Quitosana/química , Portadores de Fármacos/química , Interações Hidrofóbicas e Hidrofílicas , Lidocaína/farmacologia , Oryza/química , Amido/química , Adesividade , Administração Bucal , Animais , Liberação Controlada de Fármacos , Mucosa Esofágica/efeitos dos fármacos , Mucosa Esofágica/metabolismo , Ligação de Hidrogênio , Permeabilidade/efeitos dos fármacos , Suínos , Resistência à Tração
10.
Carbohydr Polym ; 232: 115812, 2020 Mar 15.
Artigo em Inglês | MEDLINE | ID: mdl-31952609

RESUMO

This study aimed to investigate physicochemical properties and potential application as a mucoadhesive polymer of Thai glutinous rice starch modified by planetary ball milling. XRD and ATR-FTIR results indicated a reduction in crystallinity of starch after ball milling. Different ball milling times, ranging from 5 to 45 min, resulted in modified glutinous rice starch (MGRS) with different levels of crystallinity loss, and therefore varying degrees of cold water solubility, swelling capacity, and gelatinized dispersion viscosity. Investigation of mucoadhesive properties using Texture Analyzer with porcine mucosa demonstrated that MGRS tablets exhibited greater mucoadhesive abilities compared to hydroxypropyl methylcellulose tablets, but weaker than those of sodium carboxymethylcellulose tablets. Tablets made of 15-min-milled MGRS had comparable tableting, swelling and mucoadhesiveness, but lower erosion compared to 45-min-milled MGRS. Conclusively, ball milling treatment could successfully induce the mucoadhesive properties of Thai glutinous rice starch and expand its application as mucoadhesive polymer.

11.
Int J Biol Macromol ; 148: 1061-1071, 2020 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-31982519

RESUMO

Calcium alginate (CA) beads loaded with clotrimazole (CZ) were modified by adding poloxamer (PLX) in this study. Blends of PLX188 or PLX407 into sodium alginate (SA) dispersions caused a decrease in the SA zeta potential and led to viscosity synergism. SA with carboxyl and hydroxyl groups can interact with the hydroxyl groups of PLX via hydrogen bonding. A stronger interaction of SA with PLX407 was found when compared to the interaction between SA and PLX188. The PLX-CA beads gave a higher CZ entrapment efficiency than the CA beads. The highest PLX content used created an amorphous form of CZ in the beads because of the CZ solubilization by the PLX micelles. The addition of 0.5 or 1% w/v PLX can strengthen the CZ-loaded CA beads. Furthermore, the PLX-CA beads display a lower water uptake than the CA beads. PLX micellization can enhance CZ release and enhance the efficacy of CZ against Candida albicans. This study indicates that the molecular interaction of SA with PLX and the PLX micellization of CZ can improve the characteristics of CZ-loaded CA beads, which offer good potential for use as drug delivery systems or drug reservoirs in tablets for oral candidiasis.


Assuntos
Alginatos/química , Antifúngicos/química , Clotrimazol/química , Portadores de Fármacos/química , Poloxâmero/química , Tensoativos/química , Candida albicans/efeitos dos fármacos , Composição de Medicamentos , Liberação Controlada de Fármacos , Interações Hidrofóbicas e Hidrofílicas , Micelas , Microesferas , Solubilidade , Propriedades de Superfície , Viscosidade
12.
Eur J Pharm Biopharm ; 148: 126-133, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31982576

RESUMO

Polymeric film coatings based on quaternary polymethacrylates (QPMs, e.g. Eudragits®) are frequently used for controlled release applications. However, their considerable sticking tendency is a major drawback in practice. In this study, different amounts of magnesium aluminum silicate (MAS) were added to the film coatings in order to overcome this hurdle. MAS is negatively charged and can electrostatically interact with the positively charged QPM. Different types of tablet cores were coated with aqueous Eudragit® RL 30D dispersions, optionally containing varying amounts of MAS. Dynamic changes in the wet mass of the systems as well as drug release upon exposure to 0.1 M HCl and phosphate buffer pH 6.8 were monitored. Propranolol HCl, acetaminophen, and diclofenac sodium were used as cationic, nonionic and anionic model drugs. The tablets were optionally cured for 12 h at 45 or 60 °C. Importantly, the addition of MAS to aqueous Eudragit® RL 30D dispersion substantially reduced the films' stickiness and led to stable inner coating structures, even without curing. Desired drug release rates can be adjusted by varying the QPM:MAS ratio and coating level.


Assuntos
Compostos de Alumínio/química , Excipientes/química , Compostos de Magnésio/química , Polímeros/química , Silicatos/química , Acetaminofen/química , Química Farmacêutica , Preparações de Ação Retardada , Diclofenaco/química , Liberação Controlada de Fármacos , Propranolol/química , Comprimidos , Temperatura
13.
Mater Sci Eng C Mater Biol Appl ; 92: 827-839, 2018 Nov 01.
Artigo em Inglês | MEDLINE | ID: mdl-30184812

RESUMO

The aim of this study was to investigate the effect of clay, magnesium aluminum silicate (MAS), on the properties of sodium caseinate (SC) dispersions and films. Moreover, the SC-MAS dispersions were evaluated for film coating of modified-release tablets. The results showed that MAS addition led to particle flocculation and viscosity synergism in the SC-MAS dispersions. Exfoliated or intercalated nanocomposites of the SC-MAS films could be formed because of the molecular interaction of both components via hydrogen bonding. The puncture strength and elongation of the dry SC films decreased with increasing MAS ratios. However, MAS added enhanced the puncture strength of the wet films and reduced drug permeability and diffusivity across the films in acidic medium because of lower water uptake and denser matrix structure of the films. The SC-MAS dispersions showed strong potential for use as a film coating material with few defects in the coated acetaminophen (ACT) tablets. The ACT release of the coated tablets in acidic medium was modified by varying the MAS ratios and film coating levels. In addition, the SC-MAS coated tablets possessed sustained-release behavior for the drug under simulated gastrointestinal conditions. This finding indicates that the SC-MAS nanocomposite films can be applied as a tablet coating material to modify drug release.


Assuntos
Compostos de Alumínio/química , Caseínas/química , Compostos de Magnésio/química , Membranas Artificiais , Nanocompostos/química , Silicatos/química , Comprimidos/química , Liberação Controlada de Fármacos , Ligação de Hidrogênio
14.
Int J Biol Macromol ; 118(Pt A): 683-692, 2018 Oct 15.
Artigo em Inglês | MEDLINE | ID: mdl-29959011

RESUMO

Arrowroot (Tacca leontopetaloides L. Kuntze) starch in gelatinized and ungelatinized forms was used to modify the characteristics of calcium alginate (CA) beads containing diclofenac sodium (DS). Sodium alginate (SA) was able to molecularly interact with ungelatinized starch (UGS) granules and gelatinized starch (GS) gel via hydrogen bonding mechanisms in the dispersions, leading to viscosity synergism before cross-linking. The GS-CA beads provided a significantly higher DS entrapment efficiency than the UGS-CA beads. The added UGS retarded the water uptake of the CA beads, resulting in slower DS release profiles in purified water and a longer lag time of DS release in pH 6.8 phosphate buffer. On the other hand, GS enhanced water uptake and accelerated the DS release of the beads in both media. Moreover, the 1%GS-CA beads displayed slower DS release than the CA and 1%UGS-CA beads in pH 6.8 phosphate buffer when simulated gastro-intestinal (GI) condition was used. This study shows that UGS and GS obtained from Tacca leontopetaloides L. Kuntze have good potential to improve drug entrapment efficiency of the CA beads, and the DS-loaded GS-CA beads can be used as multiunit dosage forms for sustaining drug release in simulated GI condition.


Assuntos
Alginatos/química , Portadores de Fármacos/química , Gelatina/química , Marantaceae/química , Microesferas , Amido/química , Diclofenaco/química , Liberação Controlada de Fármacos , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Tamanho da Partícula , Água/química
15.
Int J Biol Macromol ; 115: 483-493, 2018 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-29679671

RESUMO

Polysaccharide-protein composites offer potential utility for the delivery of drugs. The objectives of this work were to investigate the molecular interactions between sodium alginate (SA) and sodium caseinate (SC) in dispersions and films and to characterize calcium alginate (CA) beads mixed with SC for the delivery of fluconazole (FZ) and clotrimazole (CZ). The results demonstrated that SA could interact with SC, which caused a viscosity synergism in the dispersions. Hydrogen bonding between the carboxyl or hydroxyl groups of SA and the amide groups of SC led to the formation of soluble complexes that could reinforce the CA beads prepared by calcium cross-linking. The SC-CA beads provided higher drug entrapment efficiency, lower water uptake and erosion, and slower drug release than for the CA beads. The loaded FZ was an amorphous form, but CZ crystals were embedded in the bead matrix due to the low water solubility of this drug. However, SC micellization could enhance the water solubility and efficacy of CZ against Candida albicans. This finding indicates that SA can interact with SC via hydrogen bonding to form complexes and that the anticandidal-loaded SC-CA beads can be used as drug delivery systems and drug reservoirs in tablets for oral candidiasis.


Assuntos
Alginatos/química , Antifúngicos/química , Candida albicans/efeitos dos fármacos , Caseínas/química , Portadores de Fármacos/química , Microesferas , Antifúngicos/farmacologia , Liberação Controlada de Fármacos , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Solubilidade , Água/química
16.
Int J Pharm ; 535(1-2): 410-419, 2018 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-29155229

RESUMO

Exfoliated nanocomposites of chitosan-magnesium aluminum silicate (CS-MAS) particles are characterized by good compressibility but poor flowability. Thus, the aims of this study were to investigate agglomerates of CS-MAS nanocomposites prepared using the agglomerating agents water, ethanol, or polyvinylpyrrolidone (PVP) for flowability enhancement and to evaluate the agglomerates obtained as direct compression fillers for tablets. The results showed that the addition of agglomerating agents did not affect crystallinity, but slightly influenced thermal behavior of the CS-MAS nanocomposites. The agglomerates prepared using water were larger than those prepared using 95% ethanol because high swelling of the layer of chitosonium acetate occurred, allowing formation of solid bridges and capillary force between particles, leading to higher flowability and particle strength. Incorporation of PVP resulted in larger agglomerates with good flowability and high strength due to the binder hardening mechanism. The tablets prepared from agglomerates using water showed lower hardness, shorter disintegration times and faster drug release than those using 95% ethanol. In contrast, greater hardness and more prolonged drug release were obtained from the tablets prepared from agglomerates using PVP. Additionally, the agglomerates of CS-MAS nanocomposites showed good carrying capacity and provided desirable characteristics of direct compression tablets.


Assuntos
Compostos de Alumínio/química , Quitosana/química , Compostos de Magnésio/química , Nanocompostos/química , Silicatos/química , Liberação Controlada de Fármacos , Etanol/química , Povidona/química , Comprimidos , Água/química
17.
Drug Dev Ind Pharm ; 43(3): 492-501, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-27900918

RESUMO

The aim of this study was to determine the potential of gellan gum (GG) and halloysite (HS) dispersions at different mixing ratios and to investigate the potential of GG-HS dispersions in film formation. To this end, the dispersions and films were characterized. The dispersions formed films with large particles ranging from 3 to 4 µm in size, with a zeta potential of ∼-35 mV. The GG-HS films were fabricated using a solvent-casting technique, which generated films with a white opaque appearance and rough surface. The GG-HS films were formed via hydrogen bonding and electrostatic interactions at the inner cavity and outer surface, as confirmed by ATR-FTIR spectroscopy and X-ray diffractometry. The %water uptake and erosion of the GG-HS film decreased with increasing HS content, whereas both puncture strength and elongation were increased in the GG-HS ratios of 1:0.4 and 1:1.2. Moreover, addition of HS into the GG films could possibly decrease drug permeability coefficient when using higher HS ratio in acidic and neutral media. These results suggested that HS modifies the characteristics of the GG used to coat modified-release tablets.


Assuntos
Silicatos de Alumínio/química , Silicatos de Alumínio/metabolismo , Fenômenos Químicos , Polissacarídeos Bacterianos/química , Polissacarídeos Bacterianos/metabolismo , Argila , Avaliação Pré-Clínica de Medicamentos/métodos , Liberação Controlada de Fármacos , Tamanho da Partícula , Permeabilidade
18.
Pharm Dev Technol ; 21(1): 86-97, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-25318551

RESUMO

The objective of this study was to apply fractional factorial and multi-response optimization designs using desirability function approach for developing topical microemulsions. Minoxidil (MX) was used as a model drug. Limonene was used as an oil phase. Based on solubility, Tween 20 and caprylocaproyl polyoxyl-8 glycerides were selected as surfactants, propylene glycol and ethanol were selected as co-solvent in aqueous phase. Experiments were performed according to a two-level fractional factorial design to evaluate the effects of independent variables: Tween 20 concentration in surfactant system (X1), surfactant concentration (X2), ethanol concentration in co-solvent system (X3), limonene concentration (X4) on MX solubility (Y1), permeation flux (Y2), lag time (Y3), deposition (Y4) of MX microemulsions. It was found that Y1 increased with increasing X3 and decreasing X2, X4; whereas Y2 increased with decreasing X1, X2 and increasing X3. While Y3 was not affected by these variables, Y4 increased with decreasing X1, X2. Three regression equations were obtained and calculated for predicted values of responses Y1, Y2 and Y4. The predicted values matched experimental values reasonably well with high determination coefficient. By using optimal desirability function, optimized microemulsion demonstrating the highest MX solubility, permeation flux and skin deposition was confirmed as low level of X1, X2 and X4 but high level of X3.


Assuntos
Química Farmacêutica/métodos , Emulsões/síntese química , Minoxidil/síntese química , Animais , Emulsões/administração & dosagem , Minoxidil/administração & dosagem , Técnicas de Cultura de Órgãos , Absorção Cutânea/efeitos dos fármacos , Absorção Cutânea/fisiologia , Solubilidade , Suínos
19.
Pharm Dev Technol ; 21(5): 590-9, 2016 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-25886079

RESUMO

By blending chitosan (CS) and gum arabic (GA), a powerful biomaterial complex might be obtained due to the unique properties of CS and the low viscosity and good emulsifying properties of GA. The objectives of this study were to prepare and examine the properties of dispersions and films of CS and GA as a function of the mixing weight ratio, pH value and molecular weight of CS. The dispersions were characterized by turbidity, zeta potential and cytotoxicity and then the dispersions were cast into films. Physicochemical properties of the film were performed. CS-GA dispersions exhibited higher turbidity and a lower zeta potential with an increase in the GA ratio. Continuous films of the CS-GA could be formed at all ratios. CS and GA could molecularly interact via electrostatic forces and intermolecular hydrogen bonding. The CS-GA (1:0.5) films exhibited relatively low water uptake, erosion, water vapor permeability and puncture strength compared to the CS films. Furthermore, the CS-GA films demonstrated good mucoadhesive properties, allowing for adhesion to the mucosal membrane. Based on these results, it could be advantageous to use CS-GA films as film formers for the formulation of coatings and drug delivery systems.


Assuntos
Adesivos/química , Quitosana/química , Portadores de Fármacos/química , Goma Arábica/química , Polieletrólitos/química , Adesivos/metabolismo , Fenômenos Biomecânicos , Células CACO-2 , Fenômenos Químicos , Quitosana/metabolismo , Portadores de Fármacos/metabolismo , Goma Arábica/metabolismo , Humanos , Polieletrólitos/metabolismo , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Propriedades de Superfície
20.
Pharm Dev Technol ; 21(4): 487-98, 2016.
Artigo em Inglês | MEDLINE | ID: mdl-25757646

RESUMO

The objectives in this study were to characterize quaternary polymethacrylate-sodium alginate (QPM-SA) films prepared using high G block or high M block SA (GSA or MSA, respectively), and to investigate the effects of QPM-SA ratios, film-coating levels and SA block structures on propranolol HCl (PPN) released from coated tablets. The results demonstrated that GSA and MSA shared a similar interaction mechanism with QPM. The QPM-GSA films had higher puncture strength than the QPM-MSA films in dry and wet states, whereas the % elongations were not different. The drug permeability of the QPM-GSA films was lower than that of the QPM-MSA films in both acidic and neutral media, but higher water uptake of the QPM-GSA films was found at neutral pH. Moreover, the QPM-MSA-coated tablets had a greater PPN release rate than the QPM-GSA-coated tablets, and drug release was dependent on the film-coating levels. In addition, the QPM-SA films at a ratio of 4:0.5 produced a stronger film and could sustain PPN release. These results indicate that the QPM-GSA films had greater film strength and lower drug permeability than the QPM-MSA films. Additionally, the QPM-SA films have a strong potential for use in sustained-release tablets.


Assuntos
Alginatos/química , Antiarrítmicos/administração & dosagem , Preparações de Ação Retardada/química , Ácidos Polimetacrílicos/química , Propranolol/administração & dosagem , Antiarrítmicos/química , Liberação Controlada de Fármacos , Ácido Glucurônico/química , Ácidos Hexurônicos/química , Permeabilidade , Propranolol/química , Comprimidos
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