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1.
Int J Mol Sci ; 25(10)2024 May 16.
Artigo em Inglês | MEDLINE | ID: mdl-38791451

RESUMO

Fluconazole (FZ) is a potential antifungal compound for treating superficial and systemic candidiasis. However, the use of conventional oral drug products has some limitations. The development of buccal film may be a potential alternative to oral formulations for FZ delivery. The present study involved the development of novel FZ-loaded solid lipid nanoparticles (FZ-SLNs) in pectin solutions and the investigation of their particle characteristics. The particle sizes of the obtained FZ-SLNs were in the nanoscale range. To produce pectin films with FZ-SLNs, four formulations were selected based on the small particle size of FZ-SLNs and their suitable polydispersity index. The mean particle sizes of all chosen FZ-SLNs formulations did not exceed 131.7 nm, and the mean polydispersity index of each formulation was less than 0.5. The properties of films containing FZ-SLNs were then assessed. The preparation of all FZ-SLN-loaded pectin films provided the mucoadhesive matrices. The evaluation of mechanical properties unveiled the influence of particle size variation in FZ-SLNs on the integrity of the film. The Fourier-transform infrared spectra indicated that hydrogen bonds could potentially form between the pectin-based matrix and the constituents of FZ-SLNs. The differential scanning calorimetry thermogram of each pectin film with FZ-SLNs revealed that the formulation was thermally stable and behaved in a solid state at 37 °C. According to a drug release study, a sustained drug release pattern with a burst in the initial stage for all films may be advantageous for reducing the lag period of drug release. All prepared films with FZ-SLNs provided a sustained release of FZ over 6 h. The films containing FZ-SLNs with a small particle size provided good permeability across the porcine mucosa. All film samples demonstrated antifungal properties. These results suggest the potential utility of pectin films incorporating FZ-SLNs for buccal administration.


Assuntos
Antifúngicos , Fluconazol , Nanopartículas , Tamanho da Partícula , Pectinas , Pectinas/química , Nanopartículas/química , Fluconazol/administração & dosagem , Fluconazol/química , Fluconazol/farmacocinética , Antifúngicos/administração & dosagem , Antifúngicos/química , Antifúngicos/farmacocinética , Administração Bucal , Lipídeos/química , Portadores de Fármacos/química , Liberação Controlada de Fármacos , Espectroscopia de Infravermelho com Transformada de Fourier , Sistemas de Liberação de Medicamentos/métodos , Mucosa Bucal/metabolismo , Mucosa Bucal/efeitos dos fármacos , Varredura Diferencial de Calorimetria , Animais , Lipossomos
2.
Saudi Pharm J ; 32(4): 102002, 2024 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-38439951

RESUMO

Pectin hydrogels have emerged as a highly promising medium for the controlled release of pharmaceuticals in the dynamic field of drug delivery. The present review sheds light on the broad range of applications and potential of pectin-based hydrogels in pharmaceutical formulations. Pectin, as a biopolymer, is a versatile candidate for various drug delivery systems because of its wide range of properties and characteristics. The information provided on formulation strategies and crosslinking techniques provides researchers with tools to improve drug entrapment and controlled release. Furthermore, this review provides a more in-depth understanding of the complex factors influencing drug release from pectin hydrogels, such as the impact of environmental conditions and drug-specific characteristics. Pectin hydrogels demonstrate adaptability across diverse domains, ranging from applications in oral and transdermal drug delivery to contributions in wound healing, tissue engineering, and ongoing clinical trials. While standardization and regulatory compliance remain significant challenges, the future of pectin hydrogels appears to be bright, opening up new possibilities for advanced drug delivery systems.

3.
Int J Cosmet Sci ; 45(6): 739-748, 2023 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-37402220

RESUMO

OBJECTIVE: The excessive use of plastic packaging, even though it is possible to recycle it, is one of the main causes of global warming. In this study, dissolvable shower gel tablets for multiple uses have been developed in order to reduce the use of fresh plastic packaging. METHODS: The appropriate ratio of two surfactants, cocoyl glutamic acid (CGA) and sodium coco sulphate (SCS), was optimized using design of experiments. Additionally, skin hydration of the emollient either omega oil or glycerine was taken into account when determining its concentration. After that, powdered shower gel formulations were made and tested for their properties, including cleaning power, and foamability. On 30 human volunteers, the effects of reconstituted shower gel on skin redness, cleaning effectiveness and overall satisfaction were evaluated. RESULTS: The study found that, when cleaning power and foam height were taken into account, the proper surfactant ratio was 7.5:0 (SCS:CGA). The 5% glycerine shower gel formula demonstrated significantly greater skin hydration than other formulas. The in vivo study's findings demonstrated that there was no statistically significant difference between selected formulas (5% glycerine and 2.5% omega oil) in terms of cleaning ability. Comparing both formulas to the control, neither showed any skin redness. Additionally, it was discovered that the developed products were much more effective at cleaning and easier to use when washing for the volunteers than regular liquid soap. Overall satisfaction and the moisturizing feel were not significantly different among all products. CONCLUSION: The formula with 7.5% SCS and 5% glycerine is said to be the best one for both cleaning ability and moisturizing effect. These findings suggest that dissolvable shower gel tablets with enhanced skin benefits could offer a promising innovation in the personal care industry.


OBJECTIF: L'utilisation excessive d'emballages en plastique, même s'il est possible de les recycler, est l'une des principales causes du réchauffement climatique. Dans cette étude, des pastilles de gel douche soluble à usages multiples ont été développées afin de réduire l'utilisation d'emballages plastiques. MÉTHODES: Le rapport approprié de deux tensioactifs, l'acide cocoyl glutamique (CGA) et le sulfate de coco sodique (SCS), a été optimisé à l'aide d'un plan d'expériences. De plus, l'hydratation de la peau par l'émollient, soit l'huile omega ou la glycérine, a été prise en compte lors de la détermination de sa concentration. Après cela, des formulations de gel douche en poudre ont été fabriquées et testées pour leurs propriétés, notamment leur pouvoir nettoyant et leur capacité à mousser. Sur 30 volontaires humains, les effets du gel douche reconstitué sur les rougeurs cutanées, l'efficacité nettoyante et la satisfaction globale ont été évalués. RÉSULTATS: L'étude a révélé que, lorsque la puissance de nettoyage et la hauteur de mousse étaient prises en compte, le rapport de surfactant approprié était de 7,5:0 (SCS:CGA). La formule du gel douche a 5 % de glycérine a démontré une hydratation de la peau nettement supérieure à celle des autres formules. Les résultats de l'étude in vivo ont démontré qu'il n'y avait pas de différence statistiquement significative entre les formules sélectionnées (5 % de glycérine et 2,5 % d'huile oméga) en termes de pouvoir nettoyant. En comparant les deux formules au contrôle, aucune n'a montré de rougeur cutanée. De plus, il a été découvert que les produits développés étaient beaucoup plus efficaces pour le nettoyage et plus faciles à utiliser lors du lavage pour les volontaires que le savon liquide ordinaire. La satisfaction globale et la sensation d'hydratation n'étaient pas significativement différentes entre tous les produits. CONCLUSION: La formule avec 7,5 % de SCS et 5 % de glycérine est considérée comme la meilleure pour la capacité de nettoyage et l'effet hydratant. Ces résultats suggèrent que les comprimés de gel douche solubles avec des bienfaits améliorés pour la peau pourraient offrir une innovation prometteuse dans l'industrie des soins personnels.


Assuntos
Glicerol , Pele , Humanos , Emolientes , Comprimidos
4.
Pharm Dev Technol ; 25(3): 340-350, 2020 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-31814494

RESUMO

Kaempferia parviflora, a medicinal herb, treats hypertension and promotes longevity with good health and well-being. Its bioactive component is poorly soluble in water, resulting in poor absorption. This study aimed to enhance the bioavailability of K. parviflora dichloromethane (KPD) extract using a self-nanoemulsifying drug delivery system (SNEDDS). KPD was dissolved in diethylene glycol monoethyl, polyoxyl-35 castor oil and caprylic/capric glyceride, and clear yellow SNEDDS solution was obtained. The methoxyflavone markers were used for content and dissolution analysis. Solid SNEDDS was prepared by stepwise mixing of KPD using a mortar and pestle (1:1 ratio) with five solid carriers: Aerosil® 200, Florite® RE, Neusilin® US2 (NEUS), Fujicalin®, and Neusilin® UFL2. The USP apparatus II with simulated gastric fluid USP (SGF without pepsin, pH 1.2) was used in order to perform the in vitro dissolution. The methoxyflavones dissolution at 60 min from KPD, SEDDS, and SNEDDS/NEUS were approximately 16, 92, and 73%, respectively. The pharmacokinetic profiles of methoxyflavones for oral administration were studied using Wistar rats; the areas under the curve of SNEDDS/NEUS (1.77-fold) and SNEDDS (5.38-fold) were significantly higher than that of KPD. The developed formulations showed good stability after storage for 6 months under accelerated and normal conditions.


Assuntos
Sistemas de Liberação de Medicamentos , Flavonas/administração & dosagem , Extratos Vegetais/administração & dosagem , Zingiberaceae/química , Administração Oral , Animais , Área Sob a Curva , Disponibilidade Biológica , Estabilidade de Medicamentos , Armazenamento de Medicamentos , Emulsões , Flavonas/isolamento & purificação , Flavonas/farmacocinética , Masculino , Extratos Vegetais/farmacocinética , Ratos , Ratos Wistar , Solubilidade , Água/química
5.
Chem Pharm Bull (Tokyo) ; 66(9): 859-865, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-30175742

RESUMO

We examined the effect of hot-melt extrusion condition on the physical stability of the solid dispersion prepared using partially hydrolyzed polyvinyl alcohol (PVOH). The hot-melt extrusion of indomethacin (IMC) and PVOH mixed at the weight ratio of 3 : 7, 5 : 5 and 7 : 3 was performed either at 170 or 190°C to prepare the IMC/PVOH hot-melt extrudate (HME). Differential scanning calorimetry represented that IMC was mixed with PVOH on a scale of several tens of nanometer in all the HMEs with different weight ratio. 13C solid-state NMR measurement revealed that an intermolecular interaction was formed between a carboxylic group of IMC and a hydroxy group of PVOH in the HMEs. The intermolecular interaction in the HMEs was stronger at the higher extrusion temperature. At the low IMC loading, the IMC molecules could be mixed with the amorphous PVOH at the molecular level, and the remained PVOH without interaction formed the crystal phase. On the other hand, at the high IMC loading, most PVOH could be amorphized by the interaction with IMC, and the excess IMC which did not interact with PVOH formed the IMC-rich domain. The IMC/PVOH HME at the weight ratio of 7 : 3 extruded at higher extrusion temperature showed higher physical stability of amorphous IMC compared with that extruded at lower extrusion temperature. The hot-melt extrusion process at higher temperature provided the rapid melting of PVOH crystal phase, resulted in the homogeneous mixing with IMC and the formation of stronger intermolecular interaction.


Assuntos
Portadores de Fármacos/química , Indometacina/química , Álcool de Polivinil/química , Cristalização , Composição de Medicamentos/métodos , Estabilidade de Medicamentos , Congelamento , Temperatura Alta , Hidrólise , Transição de Fase , Solubilidade
6.
AAPS PharmSciTech ; 20(1): 14, 2018 Dec 18.
Artigo em Inglês | MEDLINE | ID: mdl-30565000

RESUMO

In this study, the resveratrol spray-dried emulsions were developed using a quality-by-design approach. Further, the product and process factors that affected the quality of the spray-dried emulsions were analyzed and illustrated using an Ishikawa diagram. The product and process risks were prioritized using a risk-ranking system. The low methoxyl pectin (LMP) amount, caprylic/capric glyceride (CCG) amount, homogenization time, homogenization speed, inlet temperature, pump speed, drying airspeed, and de-blocking speed were observed to be the eight highest risk factors. Further, the criticality of these eight factors on the responses was determined using the Plackett-Burman design. Increasing the LMP amount increased the particle size, whereas increasing the CCG amount enhanced the drug-loading capacity and drug dissolution at 5-min intervals (Q5) and decreased the moisture content. Q5 was positively affected by the homogenization speed and pump speed; however, it was negatively affected by the LMP amount. The spraying efficiency was affected by the pump speed and the LMP amount. Further, the risk level of the homogenization time, inlet temperature, drying airspeed, and de-blocking speed were reduced. However, the LMP amount, CCG amount, homogenization speed, and pump speed were observed to remain at high risk and require further investigation. The risk assessment and Plackett-Burman design mitigated the risks and identified the critical factors that affected the quality of the resveratrol spray-dried emulsions and the spray-drying process.


Assuntos
Resveratrol/administração & dosagem , Medição de Risco , Emulsões , Humanos , Resveratrol/química , Tecnologia Farmacêutica , Temperatura
7.
Chem Pharm Bull (Tokyo) ; 65(3): 284-294, 2017 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-27980251

RESUMO

The objectives of this study were to prepare the hydroxypropyl methylcellulose (HPMC)/polycarbophil (PC) mucoadhesive blend film and to investigate the main and interaction effect of HPMC and PC mixtures on the physicochemical and mechanical properties of blend films using a simplex lattice mixture design approach. The cubic and quadratic models were selected to analyze mucoadhesive properties in terms of work of adhesion and maximum detachment force, respectively. It was shown that HPMC/PC blend film had higher mucoadhesive properties than pure HPMC film. The suitable models for analyzing swelling index of blend films at various times were assessed. The puncture strength, % elongation and hydrophilicity of films were also examined. The pure HPMC film displayed more homogeneous and smoother structures compared with the blend film, as observed by scanning electron microscope and atomic force microscopy. Intermolecular hydrogen bonding between HPMC and PC was detected using Fourier transform infrared and X-ray diffraction. Therefore, the blend film shows high potential for use as a buccal delivery system.


Assuntos
Resinas Acrílicas/química , Derivados da Hipromelose/química , Resinas Acrílicas/síntese química , Interações Hidrofóbicas e Hidrofílicas , Derivados da Hipromelose/síntese química
8.
Drug Dev Ind Pharm ; 43(12): 2064-2075, 2017 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-28836855

RESUMO

CONTEXT: Low bioavailability of oral manidipine (MDP) is due to its low water solubility. OBJECTIVE: The objective of this study was to increase the solubility and bioavailability of MDP by fabricating ternary solid dispersion (tSD) with d-α-tocopherol polyethyleneglycol-1000-succinate and copovidone. METHODS: In this study, solid ternary phase diagram was applied in order to check the homogeneity of tSD prepared by melting and solidifying with dry ice. The physicochemical properties of different formulations were determined by differential scanning calorimetry (DSC), powder X-ray diffraction (PXRD), Fourier transform infrared spectroscopy (FTIR) and hot stage microscopy. Their solubility, dissolution, stability and bioavailability were also investigated. RESULTS AND DISCUSSION: The results demonstrated that tSD obtained from ternary phase diagram divided into homogeneous and non-homogeneous regions. In the homogenous region, the transparent characteristics of tSD was observed and considered as a glass solution, which have a higher MDP solubility than that in non-homogenous region. The hot stage microscopy, DSC and PXRD confirmed that solid dispersion was formed in which MDP was molecularly dispersed in the carriers, especially in the homogenous region of phase diagram. FTIR analysis demonstrated strong hydrogen bonding between amine groups of MDP and carbonyl groups of copovidone, which supported a higher solubility and dissolution of tSD. The pharmacokinetic study in Wistar rats showed that the tSD had the greatest effect on oral bioavailability. Immediate hypotensive effect of tSD was also observed in vivo. CONCLUSIONS: The improvement of stability, dissolution and oral bioavailability of MDP could be achieved by using tSD technique.


Assuntos
Di-Hidropiridinas/química , Di-Hidropiridinas/farmacocinética , Polietilenoglicóis/química , Pirrolidinas/química , Succinatos/química , Compostos de Vinila/química , alfa-Tocoferol/química , alfa-Tocoferol/farmacocinética , Animais , Disponibilidade Biológica , Varredura Diferencial de Calorimetria , Nitrobenzenos , Piperazinas , Pós , Ratos , Ratos Wistar , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Difração de Raios X
9.
Drug Dev Ind Pharm ; 43(3): 483-491, 2017 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-27874293

RESUMO

CONTEXT: Manidipine (MDP) is generally used clinically as an antihypertensive agent; however, the bioavailability of orally administered MDP is limited due to their very low water solubility. OBJECTIVE: The objectives of this research were, therefore, to increase the solubility of MDP by the formation of ternary solid dispersions (tSD) with polyethylene glycol 4000 (PEG4000) and copovidone and to improve their stability. METHODS: Solid ternary phase diagram was constructed to find homogeneous solid dispersion region after melting and solidifying at low temperature with different quenching substances. The pulverized powder of solid dispersions was then determined, for their physicochemical properties, by differential scanning calorimetry, powder X-ray diffractometry, Fourier transform infrared (FTIR) spectroscopy and hot stage microscopy. The solubility and dissolution of MDP from the tSD were investigated. The physical stability of tSD was also determined under accelerated condition at 40 °C/75% relative humidity (RH) for 6 months. RESULTS AND DISCUSSION: The results showed that MDP was molecularly dispersed in PEG4000 and copovidone when the tSD was created from homogeneous region of solid ternary phase diagram. FTIR results confirmed that strong hydrogen bonding was presented between MDP and copovidone, leading to a significant increase in the solubility and dissolution of MDP. After storage at accelerated condition (40 °C/75%RH) for 6 months, the tSD still showed a good appearance and high solubility. CONCLUSION: The results of this study suggest that tSD prepared by melting has promising potential for oral administration and may be an efficacious approach for improving the therapeutic potential of MDP.


Assuntos
Química Farmacêutica/métodos , Di-Hidropiridinas/síntese química , Polietilenoglicóis/síntese química , Pirrolidinas/síntese química , Compostos de Vinila/síntese química , Varredura Diferencial de Calorimetria/métodos , Estabilidade de Medicamentos , Nitrobenzenos , Piperazinas , Espectroscopia de Infravermelho com Transformada de Fourier/métodos
10.
AAPS PharmSciTech ; 17(3): 693-9, 2016 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-26314245

RESUMO

The present study aims to develop floating drug delivery system by sublimation of ammonium carbonate (AMC). The core tablets contain a model drug, hydrochlorothiazide, and various levels (i.e., 0-50% w/w) of AMC. The tablets were then coated with different amounts of the polyacrylate polymers (i.e., Eudragit® RL100, Eudragit® RS100, and the mixture of Eudragit® RL100 and Eudragit® RS100 at 1:1 ratio). The coated tablets were kept at ambient temperature (25°C) or cured at 70°C for 12 h before further investigation. The floating and drug release behaviors of the tablets were performed in simulated gastric fluid USP without pepsin at 37°C. The results showed that high amount of AMC induced the floating of the tablets. The coated tablets containing 40 and 50% AMC floated longer than 8 h with a time-to-float of about 3 min. The sublimation of AMC from the core tablets decreased the density of system, causing floating of the tablets. The tablets coated with Eudragit® RL100 floated at a faster rate than those of Eudragit® RS100. Even the coating level of polymer did not influence the time-to-float and floating time of coated tablets containing the same amount of AMC, the drug release from the tablets coated with higher coating level of polymer showed slower drug release. The results suggested that the sublimation technique using AMC is promising for the development of floating drug delivery system.


Assuntos
Carbonatos/síntese química , Química Farmacêutica/métodos , Sistemas de Liberação de Medicamentos/métodos , Liberação Controlada de Fármacos , Carbonatos/farmacocinética , Comprimidos com Revestimento Entérico
11.
AAPS PharmSciTech ; 16(2): 435-43, 2015 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-25367002

RESUMO

Self-nanoemulsifying drug delivery system (SNEDDS) can be used to improve dissolution of poorly water-soluble drugs. The objective of this study was to prepare SNEDDS by using ternary phase diagram and investigate their spontaneous emulsifying property, dissolution of nifedipine (NDP), as well as the pharmacokinetic profile of selected SNEDDS formulation. The results showed that the composition of the SNEDDS was a great importance for the spontaneous emulsification. Based on ternary phase diagram, the region giving the SNEDDS with emulsion droplet size of less than 300 nm after diluting in aqueous medium was selected for further formulation. The small-angle X-ray scattering curves showed no sharp peak after dilution at different percentages of water, suggesting non-ordered structure. The system was found to be robust in different dilution volumes; the droplet size was in nanometer range. In vitro dissolution study showed remarkable increase in dissolution of NDP from SNEDDS formulations compared with NDP powders. The pharmacokinetic study of selected SNEDDS formulation in male Wistar rats revealed the improved maximum concentration and area under the curve. Our results proposed that the developed SNEDDS formations could be promising to improve the dissolution and oral bioavailability of NDP.


Assuntos
Emulsões/química , Nanopartículas/química , Nifedipino/química , Animais , Disponibilidade Biológica , Química Farmacêutica/métodos , Portadores de Fármacos/química , Sistemas de Liberação de Medicamentos/métodos , Masculino , Tamanho da Partícula , Ratos , Ratos Wistar , Solubilidade , Tensoativos/química
12.
AAPS PharmSciTech ; 15(2): 456-64, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24452500

RESUMO

A simple but novel mixed surfactant system was designed to fabricate a self-nanoemulsifying drug delivery system (SNEDDS) based on hydrophilic-lipophilic balance (HLB) value. The impacts of HLB and molecular structure of surfactants on the formation of SNEDDS were investigated. After screening various oils and surfactants, nifedipine (NDP)-loaded liquid SNEDDS was formulated with Imwitor(®) 742 as oil and Tween(®)/Span(®) or Cremophor(®)/Span(®) as mixed surfactant. Droplet size of the emulsions obtained after dispersing SNEDDS containing Tween(®)/Span(®) in aqueous medium was independent of the HLB of a mixed surfactant. The use of the Cremophor(®)/Span(®) blend gave nanosized emulsion at higher HLB. The structure of the surfactant was found to influence the emulsion droplet size. Solid SNEDDS was then prepared by adsorbing NDP-loaded liquid SNEDDS comprising Cremophor(®) RH40/Span(®) 80 onto Aerosil(®) 200 or Aerosil(®) R972 as inert solid carrier. Solid SNEDDS formulations using higher amounts (30-50% w/w) of Aerosil(®) 200 exhibited good flow properties with smooth surface and preserved the self-emulsifying properties of liquid SNEDDS. Differential scanning calorimetry and X-ray diffraction studies of solid SNEDDS revealed the transformation of the crystalline structure of NDP due to its molecular dispersion state. In vitro dissolution study demonstrated higher dissolution of NDP from solid SNEDDS compared with NDP powder.


Assuntos
Bloqueadores dos Canais de Cálcio/administração & dosagem , Sistemas de Liberação de Medicamentos , Nanotecnologia , Nifedipino/administração & dosagem , Tensoativos/química , Interações Hidrofóbicas e Hidrofílicas , Estrutura Molecular
13.
AAPS PharmSciTech ; 15(6): 1357-69, 2014 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-24927669

RESUMO

Tackiness caused by the gas-entrapped membrane (Eudragit(®)RL 30D) was usually observed during storage of the effervescent floating tablets, leading to failure in floatation and sustained release. In this work, common anti-tacking agents (glyceryl monostearate (GMS) and talc) were used to solve this tackiness problem. The impact of anti-tacking agent on the properties of free films and corresponding floating tablets was investigated. GMS was more effective than talc in reducing tackiness of the film. Addition and increasing amount of anti-tacking agents lowered the film mechanical strength, but the coating films were still strong and flexible enough to resist the generated gas pressure inside the floating tablet. Wettability and water vapor permeability of the film decreased with increasing level of anti-tacking agents as a result of their hydrophobicity. No interaction between anti-tacking agents and polymer was observed as confirmed by Fourier transform infrared spectroscopy, powder X-ray diffractometry, and differential scanning calorimetry studies. Increasing amount of anti-tacking agents decreased time to float and tended to retard drug release of the floating tablets. Floating properties and drug release were also influenced by type of anti-tacking agents. The obtained floating tablets still possessed good floating properties and controlled drug release even though anti-tacking agent had some effects. The results demonstrated that the tackiness problem of the floating tablets could be solved by incorporating anti-tacking agent into the gas-entrapped membrane.


Assuntos
Resinas Acrílicas/química , Excipientes/química , Glicerídeos/química , Membranas Artificiais , Talco/química , Adesividade , Varredura Diferencial de Calorimetria , Química Farmacêutica , Preparações de Ação Retardada , Gases , Interações Hidrofóbicas e Hidrofílicas , Cinética , Modelos Químicos , Permeabilidade , Pressão , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Comprimidos , Tecnologia Farmacêutica/métodos , Água/química , Difração de Raios X
14.
Pharm Nanotechnol ; 2024 Jan 08.
Artigo em Inglês | MEDLINE | ID: mdl-38192138

RESUMO

The primary goal of drug formulation is to improve a drug's bioavailability in the body. However, poorly water-soluble drugs present challenging issues related to their solubility and bioavailability factors. Emerging technologies, such as lipid-based drug delivery systems, including micro- or nanoemulsifying drug delivery systems, have become increasingly relevant to address the above challenges. This review presents a thorough overview of self-emulsifying drug delivery systems (SEDDS). It covers the properties, principles, self-emulsification mechanism, formulation strategies, and characterization methods of SEDDS. This review also addresses the delivery of antiviral agents through SEDDS. Moreover, it summarizes the marketed formulations of SEDDS consisting of antiviral agents. This review offers a comprehensive and valuable resource for future perspectives on SEDDS and their potential applications in antiviral drug delivery.

15.
Carbohydr Polym ; 339: 122266, 2024 Sep 01.
Artigo em Inglês | MEDLINE | ID: mdl-38823930

RESUMO

Konjac glucomannan (KG) is a dietary fiber hydrocolloid derived from Amorphophallus konjac tubers and is widely utilized as a food additive and dietary supplement. As a health-conscious choice, purified KG, along with konjac flour and KG-infused diets, have gained widespread acceptance in Asian and European markets. An overview of the chemical composition and structure of KG is given in this review, along with thorough explanations of the processes used in its extraction, production, and purification. KG has been shown to promote health by reducing glucose, cholesterol, triglyceride levels, and blood pressure, thereby offering significant weight loss advantages. Furthermore, this review delves into the extensive health benefits and pharmaceutical applications of KG and its derivatives, emphasizing its prebiotic, anti-inflammatory, and antitumor activities. This study highlights how these natural polysaccharides can positively influence health, underscoring their potential in various biomedical applications.


Assuntos
Amorphophallus , Mananas , Mananas/química , Mananas/isolamento & purificação , Humanos , Amorphophallus/química , Animais , Fibras na Dieta/análise , Anti-Inflamatórios/química , Anti-Inflamatórios/farmacologia , Anti-Inflamatórios/isolamento & purificação , Suplementos Nutricionais , Prebióticos , Antineoplásicos/química , Antineoplásicos/isolamento & purificação , Antineoplásicos/farmacologia
16.
Pharm Dev Technol ; 18(3): 686-93, 2013.
Artigo em Inglês | MEDLINE | ID: mdl-22568768

RESUMO

The potential of using two natural polymers (chitosan and shellac) for the formation of nanoparticles by the process of ionic cross-linking to encapsulate bovine serum albumin, a model protein was investigated. Depending on the concentrations of chitosan, shellac and bovine serum albumin, three physical states - nanoparticle, aggregation, and solution could be observed as a result of the electrostatic force. The formation of nanoparticles was due to the balance between the repulsion force and attractive force while the imbalance between both forces resulted in the formation of aggregation and solution. The Fourier transform infrared spectroscopy and differential scanning calorimetry were applied to prove the nanoparticle formation. The particle size was characterized by the light scattering technique and was found in the range between 100 and 300 nm. The morphology of the particles, detected by transmission electron microscopy was spherical shape. The result showed that the zeta potential of the nanoparticles possessed positive charges. The concentrations of chitosan, shellac and bovine serum albumin had an influence on the physicochemical properties of the nanoparticles such as the particle size, the zeta potential, the encapsulation, the loading efficiencies and the cumulative release. Therefore, chitosan and shellac could be used to form nanoparticles for protein delivery by the ionic cross-linking method.


Assuntos
Quitosana/síntese química , Sistemas de Liberação de Medicamentos/métodos , Nanopartículas/química , Resinas Vegetais/síntese química , Soroalbumina Bovina/administração & dosagem , Soroalbumina Bovina/síntese química , Animais , Bovinos , Quitosana/administração & dosagem , Quitosana/farmacocinética , Nanopartículas/administração & dosagem , Tamanho da Partícula , Resinas Vegetais/administração & dosagem , Resinas Vegetais/farmacocinética , Soroalbumina Bovina/farmacocinética
17.
Pharmaceutics ; 15(2)2023 Jan 31.
Artigo em Inglês | MEDLINE | ID: mdl-36839789

RESUMO

In this study, 3D-printed tablets with a constant surface area were designed and fabricated using polylactic acid (PLA) in the outer compartment and polyvinyl alcohol and felodipine (FDP) in the inner compartment. The influences of different surface geometries of the inner compartment, namely, round, hexagon, square, and triangle, on drug release from 3D-printed tablets were also studied. The morphology and porosity of the inner compartment were determined using scanning electron microscopy and synchrotron radiation X-ray tomographic microscopy, respectively. Additionally, drug content and drug release were also evaluated. The results revealed that the round-shaped geometry seemed to have the greatest total surface area of the inner compartment, followed by square-shaped, hexagon-shaped, and triangle-shaped geometries. FDP-loaded 3D-printed tablets with triangle and hexagon surface geometries had the slowest drug release (about 80% within 24 h). In the round-shaped and square-shaped 3D-printed tablets, complete drug release was observed within 12 h. Furthermore, the drug release from triangle-shaped 3D-printed tablets with double the volume of the inner compartment was faster than that of a smaller volume. This was due to the fact that a larger tablet volume increased the surface area contacting the medium, resulting in a faster drug release. The findings indicated that the surface geometry of 3D-printed tablets with a constant surface area affected drug release. This study suggests that 3D printing technology may be used to develop oral solid dosage forms suitable for customized therapeutic treatments.

18.
Pharmaceutics ; 15(7)2023 Jul 04.
Artigo em Inglês | MEDLINE | ID: mdl-37514063

RESUMO

Three-dimensional (3D) printing is an unrivaled technique that uses computer-aided design and programming to create 3D products by stacking materials on a substrate. Today, 3D printing technology is used in the whole drug development process, from preclinical research to clinical trials to frontline medical treatment. From 2009 to 2020, the number of research articles on 3D printing in healthcare applications surged from around 10 to 2000. Three-dimensional printing technology has been applied to several kinds of drug delivery systems, such as oral controlled release systems, micropills, microchips, implants, microneedles, rapid dissolving tablets, and multiphase release dosage forms. Compared with conventional manufacturing methods of pharmaceutical products, 3D printing has many advantages, including high production rates due to the flexible operating systems and high drug loading with the desired precision and accuracy for potent drugs administered in small doses. The cost of production via 3D printing can be decreased by reducing material wastage, and the process can be adapted to multiple classes of pharmaceutically active ingredients, including those with poor solubility. Although several studies have addressed the benefits of 3D printing technology, hospitals and pharmacies have only implemented this process for a small number of practical applications. This article discusses recent 3D printing applications in hospitals and pharmacies for medicinal preparation. The article also covers the potential future applications of 3D printing in pharmaceuticals.

19.
Nanomaterials (Basel) ; 13(19)2023 Sep 29.
Artigo em Inglês | MEDLINE | ID: mdl-37836320

RESUMO

Polyglycolic acid (PGA) nanoparticles show promise in biomedical applications due to their exceptional biocompatibility and biodegradability. These nanoparticles can be readily modified, facilitating targeted drug delivery and promoting specific interactions with diseased tissues or cells, including imaging agents and theranostic approaches. Their potential to advance precision medicine and personalized treatments is evident. However, conventional methods such as emulsification solvent evaporation via batch synthesis or tubular reactors via flow chemistry have limitations in terms of nanoparticle properties, productivity, and scalability. To overcome these limitations, this study focuses on the design and development of a 3D-printed vortex tube reactor for the continuous synthesis of PGA nanoparticles using flow chemistry. Computer-aided design (CAD) and the design of experiments (DoE) optimize the reactor design, and computational fluid dynamics simulations (CFD) evaluate the mixing index (MI) and Reynolds (Re) expression. The optimized reactor design was fabricated using fused deposition modeling (FDM) with polypropylene (PP) as the polymer. Dispersion experiments validate the optimization process and investigate the impact of input flow parameters. PGA nanoparticles were synthesized and characterized for size and polydispersity index (PDI). The results demonstrate the feasibility of using a 3D-printed vortex tube reactor for the continuous synthesis of PGA nanoparticles through flow chemistry and highlight the importance of reactor design in nanoparticle production. The CFD results of the optimized reactor design showed homogeneous mixing across a wide range of flow rates with increasing Reynolds expression. The residence time distribution (RTD) results confirmed that increasing the flow rate in the 3D-printed vortex tube reactor system reduced the dispersion variance in the tracer. Both experiments demonstrated improved mixing efficiency and productivity compared to traditional tubular reactors. The study also revealed that the total flow rate had a significant impact on the size and polydispersity index of the formulated PGA nanoparticle, with the optimal total flow rate at 104.46 mL/min, leading to smaller nanoparticles and a lower polydispersity index. Additionally, increasing the aqueous-to-organic volumetric ratio had a significant effect on the reduced particle size of the PGA nanoparticles. Overall, this study provides insights into the use of 3D-printed vortex tube reactors for the continuous synthesis of PGA nanoparticles and underscores the importance of reactor design and flow parameters in PGA nanoparticle formulation.

20.
Med Oncol ; 40(11): 314, 2023 Oct 03.
Artigo em Inglês | MEDLINE | ID: mdl-37787816

RESUMO

The fatal amplification of lung cancer across the globe and the limitations of current treatment strategies emphasize the necessity for substitute therapeutics. The incorporation of phyto-derived components in chemo treatment holds promise in addressing those challenges. Despite the significant progressions in lung cancer therapeutics, the complexities of molecular mechanism and pathways underlying this disease remain inadequately understood, necessitating novel biomarker targeting. The Himalayas, abundant in diverse plant varieties with established chemotherapeutic potential, presents a promising avenue for investigating potential cures for lung carcinoma. The vast diversity of phytocompounds herein can be explored for targeting the disease. This review delves into the multifaceted targets of lung cancer and explores the established phytochemicals with their specific molecular targets. It emphasizes comprehending the intricate pathways that govern effective therapeutic interventions for lung cancer. Through this exploration of Himalayan flora, this review seeks to illuminate potential breakthroughs in lung cancer management using natural compounds. The amalgamation of Himalayan plant-derived compounds with cautiously designed combined therapeutic approaches such as nanocarrier-mediated drug delivery and synergistic therapy offers an opportunity to redefine the boundaries of lung cancer treatment by reducing the drug resistance and side effects and enabling an effective targeted delivery of drugs. Furthermore, additional studies are obligatory to understand the possible derivation of natural compounds used in current lung cancer treatment from plant species within the Himalayan region.


Assuntos
Neoplasias Pulmonares , Humanos , Neoplasias Pulmonares/tratamento farmacológico , Plantas , Sistemas de Liberação de Medicamentos , Compostos Fitoquímicos/farmacologia , Compostos Fitoquímicos/uso terapêutico
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