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1.
AAPS PharmSciTech ; 22(6): 205, 2021 Jul 20.
Artigo em Inglês | MEDLINE | ID: mdl-34286391

RESUMO

Drug-loaded electrospun fibers have attracted increasing attention as a promising wound dressing material due to their capability of preventing from infections and inflammation and maintaining an appropriate environment for wound healing. In this study, polylactic acid (PLA), which is widely used in wound management, was chosen as electrospinnable polymer. A triterpene extract (TE) from the outer bark of birch known for its anti-inflammatory, antiviral, antibacterial, and wound healing effects was chosen to produce TE-loaded PLA electrospun fibers for wound dressing. A binary solvent system of dichloromethane (DCM) and dimethyl sulfoxide (DMSO) was employed, and the ratio of the solvents was optimized for preparing smooth and uniform fibers. The morphology of TE-loaded PLA electrospun fibers was investigated by scanning electron microscopy (SEM). The entrapment of TE in PLA fibers was confirmed by confocal laser scanning microscopy (CLSM). Differential scanning calorimetry (DSC) and X-ray diffraction (XRD) were used to analyze the solid state of TE in PLA fibers. The release behavior of TE was assayed by a shaking flask method for a period of 96 h. The results revealed that TE-loaded electrospun PLA microfibers could be reliably prepared and are promising future candidates in wound therapy.


Assuntos
Bandagens , Betula/química , Nanofibras/química , Casca de Planta/química , Poliésteres/síntese química , Triterpenos/síntese química , Antibacterianos/análise , Antibacterianos/síntese química , Química Farmacêutica/métodos , Nanofibras/análise , Extratos Vegetais/análise , Extratos Vegetais/síntese química , Poliésteres/análise , Triterpenos/análise
2.
Int J Pharm ; 605: 120843, 2021 Aug 10.
Artigo em Inglês | MEDLINE | ID: mdl-34216765

RESUMO

Alkanediols are frequently used as alternative antimicrobial preservatives for dermal formulations. However, these substances can also have an influence on the biopharmaceutical properties of the applied preparations. Therefore, the influence 2-methyl-2,4-pentanediol, 1,2-pentanediol, 1,2-hexanediol and 1,2-octanediol on the release of triamcinolone acetonide (TAA) from four different commonly used semi-solid vehicles was investigated. In addition, the solubility of TAA in aqueous alkanediol solutions was evaluated. It was observed that its solubility increases as a function of chain length of the alkanediol, with exception of 1,2-octanediol. This can be related to the corresponding solubility parameters. Despite alkanediols increase the aqueous solubility of TAA, polarization microscopic images revealed that a significant amount of the drug is present in the suspended state in all formulations. Therefore, TAA release was proportional to the square root of time, indicating Higuchi kinetic. Alkanediols modify the release of TAA depending on the used base. The addition of alkanediols to the hydrogel formulation result in a slightly augmented release rate of the drug with increasing chain length of the added alkanediol. In contrast, alkanediols having longer chain lengths diminish the TAA release rate from all tested creams. Consequently, TAA release revealed to be partially inequivalent upon the addition of alkanediols.


Assuntos
Anti-Infecciosos , Triancinolona Acetonida , Excipientes , Hidrogéis , Solubilidade
3.
Pharmacy (Basel) ; 9(1)2021 Mar 08.
Artigo em Inglês | MEDLINE | ID: mdl-33800450

RESUMO

Despite the steadily improving medical care situation in pediatrics, some drugs are still not available in a suitable dose or dosage form and thus need to be prepared extemporaneously. Capsules can be easily compounded at the hospital and public pharmacies, offering an alternative to liquid formulations. This study aims at testing a mass-based approach for the extemporaneous preparation of low-dose pediatric capsules and investigating systematically the API loss during this procedure. A total of 54 capsule batches were prepared with baclofen and spironolactone as pediatric-relevant drugs. The hard capsules were prepared using three different bulking agents consisting of either mannitol, lactose-monohydrate and microcrystalline cellulose mixed with 0.5% colloidal silica. Capsules were tested according to Ph. Eur. method "2.9.40 Content Uniformity" as well as for occurring powder loss and mass uniformity. The results reveal that the mass-based approach, in general, allows the preparation of low-dose pediatric capsules of appropriate quality. However, absolute quality is highly dependent on the homogeneity of the powder mixture and the use of defined parameters for capsule preparation.

4.
Pharmaceutics ; 12(11)2020 Nov 20.
Artigo em Inglês | MEDLINE | ID: mdl-33233527

RESUMO

Alkanediols are often used as alternative antimicrobial preservatives for dermal formulations, e.g., hydrophilic creams. These substances show an antimicrobial effect due to their amphiphilic structure. At the same time, their amphiphilic behavior enables various interactions with the cream base itself. Therefore, the effect of four different alkanediols, namely 1,2-pentanediol, 2-methyl-2,4-pentanediol (hexylene glycol), 1,2-hexanediol, and 1,2-octanediol on the physical stability of a nonionic hydrophilic cream was investigated. Further, the incorporation of the alkanediols into lamellar structures of the cream was evaluated using differential scanning calorimetry (DSC) and small-angle X-ray scattering (SAXS) measurements. The interaction with the mixed crystals of the cream was found to increase with raising alkyl chain length of the added alkanediol. As a result, consistency and stability of the cream are slightly impaired. A test for efficacy of antimicrobial preservation according to the European Pharmacopoeia (Ph.Eur.) revealed that the antimicrobial activity is directly linked to the length of the alkyl chain of the alkanediols. 2-Methyl-2,4-pentanediol differs from both findings. This compound has non-vicinal hydroxy groups which result in a reduced amphiphilicity compared to the others. Consequently, it has a smaller impact on the colloidal structure of the cream and shows a comparatively low antimicrobial activity.

5.
Drug Dev Ind Pharm ; 46(11): 1753-1762, 2020 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-33006298

RESUMO

OBJECTIVE: Probiotic bacteria, such as different lactobacilli strains, have successfully been used to treat gingivitis and periodontitis or caries. By formulating probiotics as orodispersible tablet (ODT), the benefits of this dosage form could be utilized. Without any further measures, the probiotic bacteria will be eliminated too fast from the intended site of action, the oral mucosa. The use of mucoadhesive granules, composed of mucoadhesive polymer and probiotics, is a promising strategy to prolong the contact time between lactobacilli and oral mucosa without delaying disintegration. METHODS: Three common mucoadhesive polymers, anionic Carbopol 971P NF, nonionic Metolose 65SH50 and cationic chitosan were included into tablets either by direct compression (DC) or after granulation with the probiotics. Disintegration, mucoadhesion of the tablets, and storage stability of the probiotics were characterized. RESULTS: By incorporating a sufficient amount of polymer superior probiotic mucoadhesion could be achieved. All formulations based on granulated probiotics and mucoadhesive polymer fulfilled the Food and Drug Administration (FDA) acceptance level for disintegration of orodispersible tablets. These formulations exhibited excellent storage stability under refrigerated conditions over 30 months. Interestingly, ODTs including Carbopol 971P NF still proved superior mucoadhesion after long-term storage, whereas the mucoadhesive effect of Metolose 65SH50 and chitosan declined markedly. CONCLUSIONS: The results of this study suggest that Carbopol 971P NF was the most appropriate polymer for a probiotic mucoadhesive ODT.


Assuntos
Polímeros/química , Probióticos , Adesividade , Administração Bucal , Mucosa Bucal/efeitos dos fármacos , Comprimidos
6.
Molecules ; 25(20)2020 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-33086645

RESUMO

Triterpenes from the outer bark of birch (TE) are known for various pharmacological effects including enhanced wound healing. Apart from an already authorized oleogel, electrospun nanofiber mats containing these triterpenes in a polyvinyl alcohol (PVA) matrix appear to be an advantageous application form. The effects of PVA molecular weight and concentration on the fiber morphology have been investigated. Three different molecular weights of PVA ranging from 67 to 186 kDa were used. The concentration of PVA was varied from 5 to 20 wt%. Polymer solutions were blended with colloidal dispersions of birch bark extract at a weight ratio of 60:40 (wt.%). The estimated viscosity of polymer solutions was directly linked to their concentration and molecular weight. In addition, both pure and blended solutions showed viscoelastic properties with a dominant viscous response in the bulk. Fiber morphology was confirmed using scanning electron microscopy (SEM). Both polymer concentration and molecular weight were found to be significant factors affecting the diameter of the fibers. Fiber diameter increased with a higher molecular weight and polymer concentration as more uniform fibers were obtained using PVA of higher molecular weight (146-186 kDa). In vitro drug release and ex vivo permeation studies indicated a faster drug release of betulin from electrospun scaffolds with lower PVA molecular weight. Our research suggests that the fabricated TE-loaded PVA electrospun dressings represent potential delivery systems of TE for wound care applications.


Assuntos
Betula/química , Nanofibras/química , Triterpenos/farmacologia , Cicatrização/efeitos dos fármacos , Sistemas de Liberação de Medicamentos , Humanos , Peso Molecular , Compostos Orgânicos/química , Compostos Orgânicos/farmacologia , Casca de Planta/química , Álcool de Polivinil/química , Triterpenos/química
7.
Pharmaceutics ; 12(10)2020 Oct 19.
Artigo em Inglês | MEDLINE | ID: mdl-33086775

RESUMO

The authors wish to make the following correction to this paper [...].

8.
Pharmaceutics ; 12(9)2020 Aug 31.
Artigo em Inglês | MEDLINE | ID: mdl-32878213

RESUMO

This study investigated the formulation and processing of aqueous colloidal dispersions containing a birch bark dry extract (TE) as the active substance and hydrogenated phospholipids (Phospholipon 90H) as stabilizer, which can be used in the preparation of electrospun wound dressings. Colloidal dispersions manufactured using a two-stage homogenization process had a bimodal particle size distribution, which was most significantly (p < 0.0001) affected by the phospholipid content. The size of the single particles decreased from an average particle size of about 4 µm to a particle size of approximately 400 nm. Dynamic interfacial tension studies performed using a profile analysis tensiometer (PAT) showed that the phospholipids strongly declined the interfacial tension, whereas a further decrease was observed when phospholipids were combined with birch bark extract. Interfacial viscoelasticity properties analyzed using the oscillating drop technique resulted in an increase of both interfacial elasticity and viscosity values. These results indicated that the phospholipids are preferentially located at the lipophilic/water interface and a stable film is formed. Furthermore, the results point to a synergistic interaction between phospholipids and TE. Confocal Raman microscopy (CRM) suggested that the TE is predominantly located in the oil phase and the phospholipids at the interface.

9.
Pharmaceutics ; 12(8)2020 Aug 14.
Artigo em Inglês | MEDLINE | ID: mdl-32823875

RESUMO

Novel birch bark dry extract (TE)-loaded polyvinyl alcohol (PVA) fiber mats intended for wound therapy were developed through an electrospinning process. Colloidal dispersions containing TE as the active substance were prepared by the high-pressure homogenization (HPH) technique using hydrogenated phospholipids as stabilizer. Subsequently, the colloidal dispersions were blended with aqueous PVA solutions in the ratio of 60:40 (wt.%) and electrospun to form the nanofiber mats. Fiber morphology examined using scanning electron microscopy (SEM) indicated that fibers were uniform and achieved diameters in the size range of 300-1586 nm. Confocal Raman spectral imaging gave good evidence that triterpenes were encapsulated within the electrospun mats. In vitro drug release and ex vivo permeation studies indicated that the electrospun nanofibers showed a sustained release of betulin, the main component of birch bark dry extract, making the examined dressings highly applicable for several wound care applications. Ex vivo wound healing studies proved that electrospun fiber mats containing TE accelerated wound healing significantly more than TE oleogel, which was comparable to an authorized product that consists of TE and sunflower oil and has proved to enhance wound healing. Therefore, our results conclude that the developed TE-PVA-based dressings show promising potential for wound therapy, an area where effective remedy is needed.

10.
Mol Imaging Biol ; 22(5): 1324-1332, 2020 10.
Artigo em Inglês | MEDLINE | ID: mdl-32514887

RESUMO

PURPOSE: Inflammation is involved in many disease processes. However, accurate imaging tools permitting diagnosis and characterization of inflammation are still missing. As inflamed tissues exhibit a high rate of glycolysis, pyruvate metabolism may offer a unique approach to follow the inflammatory response and disease progression. Therefore, the aim of the study was to follow metabolic changes and recruitment of inflammatory cells after onset of inflammation in arthritic ankles using hyperpolarized 1-13C-pyruvate magnetic resonance spectroscopy (MRS) and 19F magnetic resonance imaging (MRI), respectively. PROCEDURE: Experimental rheumatoid arthritis (RA) was induced by intraperitoneal injection of glucose-6-phosphate-isomerase-specific antibodies (GPI) containing serum. To monitor pyruvate metabolism, the transformation of hyperpolarized 1-13C-pyruvate into hyperpolarized 1-13C-lactate was followed using MRS. To track phagocytic immune cell homing, we intravenously injected a perfluorocarbon emulsion 48 h before imaging. The animals were scanned at days 1, 3, or 6 after GPI-serum injection to examine the different stages of arthritic inflammation. Finally, to confirm the pyruvate metabolic activity and the link to inflammatory cell recruitment, we conducted hematoxylin-eosin histopathology and monocarboxylase transporter (MCT-1) immune histochemistry (IHC) of inflamed ankles. RESULTS: Hyperpolarized 1-13C-pyruvate MRS revealed a high rate of lactate production immediately at day 1 after GPI-serum transfer, which remained elevated during the progression of the disease, while 19F-MRI exhibited a gradual recruitment of phagocytic immune cells in arthritic ankles, which correlated well with the course of ankle swelling. Histopathology and IHC revealed that MCT-1 was expressed in regions with inflammatory cell recruitment, confirming the metabolic shift identified in arthritic ankles. CONCLUSIONS: Our study demonstrated the presence of a very early metabolic shift in arthritic joints independent of phagocytic immune cell recruitment. Thus, hyperpolarized 1-13C-pyruvate represents a promising tracer to monitor acute arthritic joint inflammation, even with minor ankle swelling. Furthermore, translated to the clinics, these methods add a detailed characterization of disease status and could substantially support patient stratification and therapy monitoring.

11.
Drug Dev Ind Pharm ; 46(7): 1185-1198, 2020 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-32536225

RESUMO

Objective: The development of medicinal plants for clinical use represents an important direction in biomedical research, despite the technological difficulties.Significance: The aim of this study was to compare pharmaceutical characteristics and in vitro release of Classical and Pickering emulsions containing crude or fractionated extracts of Libidibia ferrea.Methods: After evaluating the extract's solubility in formulation, a dispersion of hydroxypropyl methylcellulose (HPMC) was prepared in water. For Pickering emulsions, the aqueous phase was HPMC and the oil phase was Miglyol® 812; for Classical emulsions, water with Tween® 20 and Miglyol® 812 with Span® 80 were used for aqueous and oil phases, respectively. Crude or fractionated extracts were added to the aqueous phase (5% w/v). Both phases were heated (40 °C); then, the oil phase was poured into the aqueous phase and homogenized using an Ultra-Turrax. Emulsions were characterized for 90 days by pH, polyphenol content, phytomarker content, macroscopic characteristics, droplet size, and zeta potential.Results: These formulations displayed satisfactory stability for 90 days when stored at 25 °C. Regarding the investigation of rheological properties, Pickering emulsions displayed higher viscosity with lesser deformation than Classical emulsions. Moreover, the emulsions displayed similar in vitro release behavior.Conclusion: Based on the results of present study, the Pickering emulsions were obtainable and displayed higher stability than Classical emulsions. Additionally, maintenance of system integrity points to promising systems for delivery of active pharmaceutical ingredients in the internal phase, despite the complex chemical mixture added to the external phase.


Assuntos
Extratos Vegetais , Água , Emulsões , Tamanho da Partícula , Reologia
12.
Pharmaceutics ; 12(4)2020 Apr 01.
Artigo em Inglês | MEDLINE | ID: mdl-32244827

RESUMO

Already in ancient times, semisolid preparations for cutaneous application, popularly known as ointments, played an important role in human society [...].

13.
Pharmaceutics ; 12(2)2020 Feb 21.
Artigo em Inglês | MEDLINE | ID: mdl-32098195

RESUMO

Triterpenes from the outer bark of birch have many beneficial biological and pharmacological activities. In particular, its wound healing efficacy is of paramount importance. Apart from that, particles of a birch bark dry extract aggregate into a three dimensional network when they are dispersed in lipids yielding a semi-solid oleogel. However, gel formation requires high amounts of the extract, which then acts at once as the active ingredient and the gelling agent. Infrared spectra of the respective mixtures proved that hydrogen bonds play a crucial role in the formation of the gel network. Dicarboxylic acids had almost no effect on gel strength. Monoalcohols increased the firmness of the oleogel with a decreasing effect from methanol > ethanol > butanol > octanol. All tested terminal diols increased the gel strength whereas vicinal diols affected the gel strength negatively. The effect was highly dependent on their concentration. The different effects of the diols are linked to their structure and polarity. The most pronounced enhancement of gelation was found for 1,6-hexanediol, which reduced the amount of triterpene extract (TE), which is necessary for the formation of an oleogel by a factor of 10.

14.
Eur J Pharm Sci ; 142: 105109, 2020 Jan 15.
Artigo em Inglês | MEDLINE | ID: mdl-31770662

RESUMO

Ongoing demand in sustainable and biocompatible drug dosage forms is reflected in the search for novel pharmaceutical excipients with equal properties. A group of microbial exopolysaccharides offers a variety of biopolymers with many alleged uses and effects. This study aims to assess applicative properties of levan obtained from Bacillus licheniformis NS032, focusing on its potential co-stabilizing and drug release-controlling functions in pertaining emulsion systems. Despite its high molecular weight and partial existence in globular nanometric structures (180-190 nm), levan was successfully incorporated into both tested colloidal systems: those stabilized with synthetic/anionic or natural-origin/non-ionic emulsifiers. In the tested levan concentrations range (0.2-3.0% w/w) the monitored flow and thermal parameters failed to show linear concentration dependence, which prompted us to revisit certain colloidal fundamentals of this biopolymer. Being a part of the external phase of the investigated emulsion systems, levan contributed to formation of a matrix-like environment, offering additional stabilization of the microstructure and rheology modifying properties (hysteresis loop elevation as high as 4167±98 to 20792±3166 Pa•s-1), especially in case of the samples where lamellar liquid crystalline formation occurred. Apart from its good water solubility and considerable conformational flexibility, the investigated homofructan easily saturated the external phase of the samples stabilized with a conventional anionic emulsifier, leading to similar properties of 0.2% and 3.0% levan-containing samples. After closer consideration of thermal and release behavior, this was considered as a favorable property for a novel excipient, offering tailored formulation characteristics even with lower levan concentrations, consequently not compromising the potential cost of the final drug dosage form.


Assuntos
Bacillus licheniformis/química , Biopolímeros/química , Preparações de Ação Retardada/química , Frutanos/química , Administração Tópica , Formas de Dosagem , Liberação Controlada de Fármacos/efeitos dos fármacos , Emulsificantes/química , Emulsões/química , Excipientes/química , Reologia/métodos , Solubilidade/efeitos dos fármacos
15.
Eur J Pharm Biopharm ; 139: 240-245, 2019 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-30946916

RESUMO

Orodispersible tablets (ODTs) are a convenient dosage form and a recent trend in formulation development. The fast disintegration is accompanied by rapid removal of the active principle and the excipients from the mouth due to saliva flow and swallowing. Probiotic bacteria are a promising strategy to fight disease with bacterial aetiology in the mouth, but a certain residence time in the oral cavity is inevitable to exert their positive effects. The addition of a mucoadhesive polymer, like hydroxypropyl methylcellulose (HPMC), is an auspicious strategy to prolong this residence time. Nevertheless, the disintegration time of the tablets should still meet the acceptance level from the FDA (<30 s). To reach intimate contact of bacteria and mucoadhesive polymer on the one hand and to support fast disintegration on the other hand, granulation of probiotic bacteria and mucoadhesive HPMC with a methacrylic acid copolymer was performed first. Moreover, high mucoadhesion could be obtained because bacteria and mucoadhesive polymer could interact more strongly with the mucosa after the ODT disintegrated and the methacrylic acid copolymer dissolved in the pH neutral saliva.


Assuntos
Excipientes/química , Derivados da Hipromelose/química , Mucosa Bucal/metabolismo , Probióticos/administração & dosagem , Saliva/metabolismo , Adesividade , Administração Bucal , Animais , Disponibilidade Biológica , Química Farmacêutica , Composição de Medicamentos/métodos , Lactobacillus paracasei , Lactobacillus plantarum , Ácidos Polimetacrílicos/química , Probióticos/farmacocinética , Solubilidade , Suínos , Comprimidos , Fatores de Tempo
16.
Klin Monbl Augenheilkd ; 236(1): 69-73, 2019 Jan.
Artigo em Alemão | MEDLINE | ID: mdl-28514816

RESUMO

Silicone oil endotamponades need to be injected and removed in a reasonable time and under moderate pressure conditions. However, due to ever-decreasing sizes of incisions and trocars, injection and removal of highly viscous silicone oils is very time-consuming. To address resulting problems like longer treatment times or hypotony, thixotropic silicone oils were developed. These oils are characterized by a diminished viscosity under constant mechanical stress; whilst there is pressure or vacuum acting on it, the oils will become more fluid and, therefore, much easier to be applied. Once the force is being removed from the oil, it will automatically return to its initial viscosity after a short time.


Assuntos
Tamponamento Interno , Descolamento Retiniano , Óleos de Silicone , Humanos , Descolamento Retiniano/terapia , Viscosidade , Vitrectomia
17.
Int J Pharm ; 551(1-2): 141-147, 2018 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-30194013

RESUMO

Oromucosal drug delivery is necessary when a local effect in the oral cavity is required. Bioadhesive formulations should be advantageous because a larger fraction of the active principal is retained at the site of action allowing for an enhanced and prolonged effect. Despite a variety of mucoadhesion test systems being described in literature, none of these in-vitro tests does relate to physiological conditions in the oral cavity and suites for the testing of complete dosage forms, e.g. tablets. The novel mucoadhesion test is based on porcine buccal mucosa. Constituents, osmolality and pH of the used artificial saliva was as close as possible to physiologic conditions and the flushing rate was equivalent to the physiological secretion rate of saliva. Suitability of the novel test was evaluated with ODTs with live probiotic bacteria as the active principle. With the novel test system, it was shown that in the presence of mucoadhesive polymers (Carbopol®, Metolose® and chitosan) up to 36 % of the probiotic bacteria adhered to the mucosa corresponding to a two- or threefold increase compared to tablets without such polymers. Furthermore, the influence of the tablet size (contact area) on the mucoadhesive properties could be resolved.


Assuntos
Resinas Acrílicas/administração & dosagem , Quitosana/administração & dosagem , Derivados da Hipromelose/administração & dosagem , Mucosa Bucal/química , Probióticos/administração & dosagem , Adesividade , Administração Bucal , Animais , Suínos , Comprimidos
18.
Int J Pharm ; 550(1-2): 333-346, 2018 Oct 25.
Artigo em Inglês | MEDLINE | ID: mdl-30179702

RESUMO

The objective of this work was to investigate and profoundly characterize low-energy nanoemulsions as multifunctional carriers, with slight reference to dermal administration. An evidence-based approach was offered for deepening the knowledge on their formation via spontaneous emulsification. Curcumin, a compound of natural origin, potentially powerful therapeutic, was chosen as a model API. Due to curcumin's demanding properties (instability, poor solubility, low permeability), its potentials remain unreached. Low-energy nanoemulsions were considered carriers capable of overcoming imposed obstacles. Formulation consisting of Polysorbate 80 and soybean lecithin as stabilizers (9:1, 10%), medium-chain triglycerides as the oil phase (10%) and ultrapure water was selected for curcumin incorporation in 3 different concentrations (1, 2 and 3 mg/mL). Physicochemical stability was demonstrated during 3 months of monitoring (mean droplet size: 111.3-146.8 nm; PDI < 0.2; pH: 4.73-5.73). Curcumin's release from developed vehicles followed Higuchi's kinetics. DPPH (IC50 = 0.1187 mg/mL) and FRAP (1.19 ±â€¯0.02 mmol/g) assays confirmed that curcumin acts as a potent antioxidant through different mechanisms, with no alterations after incorporation in the formulation. High biocompatibility in line with antigenotoxic activity of curcumin-loaded formulations (protective and reparative) was estimated through Comet assay. A multidisciplinary approach is needed to fully characterize developed systems, directing them to more concrete application possibilities.


Assuntos
Antioxidantes , Curcumina , Nanopartículas , Adulto , Antioxidantes/administração & dosagem , Antioxidantes/química , Compostos de Bifenilo/química , Ensaio Cometa , Curcumina/administração & dosagem , Curcumina/química , Vias de Administração de Medicamentos , Liberação Controlada de Fármacos , Emulsões , Feminino , Humanos , Nanopartículas/administração & dosagem , Nanopartículas/química , Picratos/química
19.
Eur J Pharm Biopharm ; 131: 1-7, 2018 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-30048744

RESUMO

Topical formulations are the most common therapeutic agents in the treatment of skin diseases. They contain one or more active pharmaceutical ingredients (API) which need to penetrate or permeate the skin in order to exert their effect. However, after application a part of the formulation is removed from the skin due to contact with the environment. Therefore, a part of the active is then not available for penetration and thus, a loss in therapeutic effect will result. To achieve the desired therapeutic outcome a sufficient fraction of the formulation must remain on the skin. The extent to which the loss of preparation affects penetration and permeation is less investigated. This work presents a method to examine the influence of mechanical stress and formulation loss on skin permeation. A movable punch with a defined weight simulated contact between clothing or skin and the applied formulation. Weight of the tool, number of contacts and speed settings were variable and were investigated. Ex vivo permeation experiments were performed in Franz diffusion cells using porcine skin. Three preparations with nonivamide as active ingredient were chosen as model formulations: A semisolid cream, an oil-in-oil emulsion and a film-forming formulation. The last two show sustained permeation profiles. The method uses skin-to-formulation and clothing-to-formulation contact to simulate the removal of the formulations from the skin.


Assuntos
Fármacos Dermatológicos/farmacocinética , Absorção Cutânea , Administração Cutânea , Administração Tópica , Animais , Capsaicina/administração & dosagem , Capsaicina/análogos & derivados , Capsaicina/farmacocinética , Vestuário , Fármacos Dermatológicos/administração & dosagem , Fármacos Dermatológicos/química , Cultura em Câmaras de Difusão , Composição de Medicamentos , Sistemas de Liberação de Medicamentos , Emulsões , Inibidores Enzimáticos/administração & dosagem , Inibidores Enzimáticos/farmacocinética , Técnicas In Vitro , Pomadas , Pele/metabolismo , Suínos
20.
Int J Pharm ; 528(1-2): 253-267, 2017 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-28602800

RESUMO

This work aimed to prove the ability of "ready-to-use" topical vehicles based on alkyl polyglucoside-mixed emulsifier (with/without co-solvent modifications) to replace the conventionally used pharmacopoeial bases (e.g., non-ionic hydrophilic cream) in compounding practice. For this purpose, considering the regulatory efforts to establish alternative, scientifically valid methods for evaluating therapeutic equivalence of topical semisolids, we performed a comparative assessment of microstructure, selected critical quality attributes (CQAs) and in vitro/in vivo product performances, by utilizing aceclofenac as a model drug. The differences in composition between investigated samples have imposed remarkable variances in monitored CQAs (particularly in the amount of aceclofenac dissolved, rheological properties and water distribution mode), reflecting the distinct differences in microstructure formed, as partially observed by polarization microscopy and confocal Raman spectral imaging. Although not fully indicative of the in vivo performances, in vitro release data (vertical diffusion vs. immersion cells) proved the microstructure peculiarities, asserting the rheological properties as decisive factor for obtained liberation profiles. Contrary, in vitro permeation results obtained using pig ear epidermis correlated well with in vivo dermatopharmacokinetic data and distinguished unequivocally between tested formulations, emphasizing the importance of skin/vehicle interactions. In summary, suggested multi-faceted approach can provide adequate proof on topical semisolids therapeutic equivalence or lack thereof.


Assuntos
Portadores de Fármacos/química , Emulsificantes/química , Absorção Cutânea , Adulto , Animais , Liberação Controlada de Fármacos , Feminino , Humanos , Masculino , Pele , Fita Cirúrgica , Suínos
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