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1.
Pharmaceutics ; 15(12)2023 Nov 27.
Artigo em Inglês | MEDLINE | ID: mdl-38140026

RESUMO

The impairment of skin integrity derived from derangement of the orthorhombic lateral organization is mainly caused by dysregulation of ceramide amounts in the skin barrier. Ceramides, fatty acids, and cholesterol-containing nano-based formulations have been used to impair the skin barrier. However, there is still a challenge to formulate novel formulations consisting of ceramides due to their chemical structure, poor aqueous solubility, and high molecular weight. In this study, the design and optimization of Ceramide 3 (CER-NP)-loaded liposomes are implemented based on response surface methodology (RSM). The optimum CER-NP-loaded liposome was selected based on its particle size (PS) and polydispersity index (PDI). The optimum CER-NP-loaded liposome was imagined by observing the encapsulation by using a confocal laser scanning microscope (CLSM) within fluorescently labeled CER-NP. The characteristic liquid crystalline phase and lipid chain conformation of CER-NP-loaded liposomes were determined using attenuated total reflectance infrared spectroscopy (ATR-IR). The CER-NP-loaded liposomes were imagined using a field emission scanning electron microscope (FE-SEM). Finally, the in vitro release of CER-NP from liposomes was examined using modified Franz Cells. The experimental and predicted results were well correlated. The CLSM images of optimized liposomes were conformable with the other studies, and the encapsulation efficiency of CER-NP was 93.84 ± 0.87%. ATR-IR analysis supported the characteristics of the CER-NP-loaded liposome. In addition, the lipid chain conformation shows similarity with skin barrier lipid organization. The release pattern of CER-NP liposomes was fitted with the Korsmeyer-Peppas model. The cytotoxicity studies carried out on HaCaT keratinocytes supported the idea that the liposomes for topical administration of CER-NP could be considered relatively safe. In conclusion, the optimized CER-NP-loaded liposomes could have the potential to restore the skin barrier function.

2.
Bioengineering (Basel) ; 10(8)2023 Aug 04.
Artigo em Inglês | MEDLINE | ID: mdl-37627812

RESUMO

One of the crucial approaches to managing the low solubility and weak bioavailability of drugs is via nanocrystal technology. Through this technology, drug particles have an increased solubility and a faster dissolution rate due to high surface free energy, which requires an appropriate stabilizer(s) to prevent instabilities during the manufacturing process and storage of the nanosuspension. This study aimed to establish a scientific predictive system for properly selecting stabilizers or to reduce the attempts on a trial-and-error basis in the wet-milling method. In total, 42 experiments were performed to examine the effect of critical material attributes on the wettability of the drug, the saturation solubility in the stabilizer solutions or combinations thereof and the dynamic viscosity of stabilizer solutions. All data were evaluated by Minitab 19® and an optimization study was performed. The optimized formulation at a certain concentration of stabilizer combination was ground by Dyno Mill® with 0.3 mm beads for one hour. The optimized nanosuspension with a particle size of 204.5 nm was obtained in short milling time and offered 3.05- and 3.51 times better dissolution rates than the marketed drug product (Invokana® 100 mg) in pH 4.5 and pH 6.8 as non-sink conditions, respectively. The formulation was monitored for three months at room temperature and 4 °C. The parameters were 261.30 nm, 0.163, -14.1 mV and 261.50 nm, 0.216 and -17.8 mV, respectively. It was concluded that this approach might indicate the appropriate selection of stabilizers for the wet-milling process.

3.
Pharmaceutics ; 15(6)2023 Jun 02.
Artigo em Inglês | MEDLINE | ID: mdl-37376092

RESUMO

Due to their increased surface area, extent of swelling and active substance-loading capacity and flexibility, nanogels made from natural and synthetic polymers have gained significant interest in scientific and industrial areas. In particular, the customized design and implementation of nontoxic, biocompatible, and biodegradable micro/nano carriers makes their usage very feasible for a range of biomedical applications, including drug delivery, tissue engineering, and bioimaging. The design and application methodologies of nanogels are outlined in this review. Additionally, the most recent advancements in nanogel biomedical applications are discussed, with particular emphasis on applications for the delivery of drugs and biomolecules.

4.
Pharmaceutics ; 15(4)2023 Mar 25.
Artigo em Inglês | MEDLINE | ID: mdl-37111550

RESUMO

Nanofibers are frequently encountered in daily life as a modern material with a wide range of applications. The important advantages of production techniques, such as being easy, cost effective, and industrially applicable are important factors in the preference for nanofibers. Nanofibers, which have a broad scope of use in the field of health, are preferred both in drug delivery systems and tissue engineering. Due to the biocompatible materials used in their construction, they are also frequently preferred in ocular applications. The fact that they have a long drug release time as a drug delivery system and have been used in corneal tissue studies, which have been successfully developed in tissue engineering, stand out as important advantages of nanofibers. This review examines nanofibers, their production techniques and general information, nanofiber-based ocular drug delivery systems, and tissue engineering concepts in detail.

5.
Pharmaceutics ; 14(3)2022 Feb 27.
Artigo em Inglês | MEDLINE | ID: mdl-35335902

RESUMO

BACKGROUND: Fungal ocular infections can cause serious consequences, despite their low incidence. It has been reported that Posaconazole (PSC) is used in the treatment of fungal infections in different ocular tissues by diluting the oral suspension, and successful results were obtained despite low ocular permeation. Therefore, we optimized PSC-loaded ocular micelles and demonstrated that the permeation/penetration of PSC in ocular tissues was enhanced. METHODS: The micellar-based in situ gels based on the QbD approach to increase the ocular bioavailability of PSC were developed. Different ratios of Poloxamer 407 and Poloxamer 188 were chosen as CMAs. Tsol/gel, gelling capacity and rheological behavior were chosen as CQA parameters. The data were evaluated by Minitab 18, and the formulations were optimized with the QbD approach. The in vitro release study, ocular toxicity, and anti-fungal activity of the optimized formulation were performed. RESULTS: Optimized in situ gel shows viscoelastic property and becomes gel form at physiological temperatures even when diluted with the tear film. In addition, it has been shown that the formulation had high anti-fungal activity and did not have any ocular toxicity. CONCLUSIONS: In our previous studies, PSC-loaded ocular micelles were developed and optimized for the first time in the literature. With this study, the in situ gels of PSC for ocular application were developed and optimized for the first time. The optimized micellar-based in situ gel is a promising drug delivery system that may increase the ocular permeation and bioavailability of PSC.

6.
Drug Deliv Transl Res ; 12(3): 662-675, 2022 03.
Artigo em Inglês | MEDLINE | ID: mdl-33830458

RESUMO

Posaconazole (PSC) is a triazole group anti-fungal agent with the widest spectrum. Although there is no commercially available ocular dosage form, its diluted oral suspension preparation (Noxafil®) is used as off-label in topical treatment of severe keratitis and sclerokeratitis in the clinic. However, ocular bioavailability of PSC suspension form is extremely low due to its highly lipophilic character. Thus, there is a clinical need to improve its ocular bioavailability and to develop novel delivery system for the treatment of ocular fungal infections. Herein, we studied ex vivo permeation, penetration, anti-fungal activity, and Hen's Egg Test-Chorioallantoic Membrane (HET-CAM) toxicity tests in order to assess ocular targeting of PSC micelles, which were optimized in our previous study. The results indicated that micellar carrier system increased the permeability of PSC to eye tissues. Micelles showed higher affinity to ocular tissues than that of commercial oral suspension of PSC (Noxafil®). In vitro anti-fungal activity data also confirmed the efficacy of PSC loaded micellar formulations against Candida. albicans strains. The relative safety of the optimized micelles on the ocular tissue was shown with the HET-CAM toxicity test. In conclusion, micellar systems could be a promising strategy for the effective and safe delivery of PSC in the treatment of ocular fungal infections.


Assuntos
Infecções Oculares Fúngicas , Ceratite , Animais , Antifúngicos/toxicidade , Galinhas , Infecções Oculares Fúngicas/tratamento farmacológico , Feminino , Ceratite/tratamento farmacológico , Micelas , Suspensões , Triazóis/farmacologia
7.
Drug Deliv Transl Res ; 11(2): 626-646, 2021 04.
Artigo em Inglês | MEDLINE | ID: mdl-33666878

RESUMO

Acne is a chronic dermatological disease of pilosebaceous units existing in the form of hair follicles (HFs) and accompanying sebaceous glands. In topical acne treatment, localisation of drug substance at the target site, in pilosebaceous units, especially in HFs is essential. The aims of this study were to develop and optimise adapalene (ADA)-loaded PAMAM dendrimer-based nanocarriers for topical acne treatment and to prepare gel formulations of the selected nanocarriers and to characterise their rheological properties and spreadability. ADA accumulation in HFs and in the skin from PAMAM dendrimers' aqueous colloidal formulations and their gel formulations were quantitatively determined using punch biopsy technique. Follicular targeting efficiency from PAMAM dendrimers and their gel formulation was compared with the commercial gel product, Differin® Gel. The localisation of fluorescently labelled PAMAM dendrimers was visualised using a confocal microscope, which confirmed a successful delivery of the carrier system to the HFs. It was also quantified that PAMAM dendrimers improved follicular localisation and skin deposition of ADA. PAMAM dendrimers' gel formulation including lower ADA doses compared with the commercial product exhibited efficient performance in terms of drug accumulation in HFs. In vitro cell viability studies showed the relative safety of G2-PAMAM dendrimers which could be considered to possibly be well tolerated by the skin. Overall, PAMAM dendrimers' potential to selectively target drugs to the site of action, reduce dose administrated, therefore minimise side effects and provide efficiency in topical treatment of dermatological diseases such as acne was shown.


Assuntos
Dendrímeros , Adapaleno , Portadores de Fármacos/metabolismo , Pele/metabolismo , Absorção Cutânea
8.
Eur J Pharm Sci ; 158: 105638, 2021 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-33176190

RESUMO

The cutaneous drug delivery represents an attractive option for the management of skin diseases. However, the skin has a very complex morphological structure, although the skin barrier is disrupted in some of dermatological diseases. Therefore, to safely overcome the skin barrier and to deliver drugs across the skin efficiently is still remain as a challenge in the management of dermatological diseases. The nanocarrier mediated cutaneous delivery appears to offer a hope to provide targeting potential of the drugs into specific sites of the skin with minimizing side effects. This review highlights the human structure and diseased skin barrier, and possible therapeutic outcomes of nanocarrier based drug delivery in the treatment of skin diseases due to their skin transport and follicular targeting mechanisms, and summarizes recent studies in which polymer, lipid and surfactant based nanocarriers of drugs used in the skin diseases.


Assuntos
Portadores de Fármacos , Nanopartículas , Administração Cutânea , Portadores de Fármacos/metabolismo , Sistemas de Liberação de Medicamentos , Humanos , Pele/metabolismo , Absorção Cutânea
9.
Recent Pat Drug Deliv Formul ; 14(3): 191-200, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32819264

RESUMO

Atopic dermatitis is a chronic inflammatory disease of the skin, which is characterized by itching, erythema, and eczematous lacerations. It affects about 10 % of adults and approximately 15-20 % of children worldwide. As a result of genetic, immunologic, and environmental factors, the disease manifests itself with the impaired stratum corneum barrier and then immunological responses. Topical administration of corticosteroids and calcineurin inhibitors are currently used as the first strategy in the management of the disease. However, they have low skin bioavailability and some side effects. The nanocarriers as novel drug delivery systems could overcome limitations of conventional dosage forms, owing to increment of poorly soluble drug' solubility, then its thermodynamic activity and, consequently, its skin permeation. Also, side effects of the drug substances on the skin could be reduced by the nano-sized drug delivery systems due to encapsulation of the drug in the nanocarriers and targeted drug delivery of drug substances to the inflammated skin areas. Thereby, there have been available numerous research studies and patents regarding the use of nanocarriers in the management of atopic dermatitis. This review focuses on the mechanism of disease and development of nanocarrier based on novel drug release systems in the management of atopic dermatitis.


Assuntos
Corticosteroides/administração & dosagem , Inibidores de Calcineurina/administração & dosagem , Dermatite Atópica/tratamento farmacológico , Fármacos Dermatológicos/administração & dosagem , Portadores de Fármacos , Nanopartículas , Pele/efeitos dos fármacos , Administração Cutânea , Corticosteroides/química , Corticosteroides/farmacocinética , Animais , Disponibilidade Biológica , Inibidores de Calcineurina/química , Inibidores de Calcineurina/farmacocinética , Dermatite Atópica/diagnóstico , Dermatite Atópica/metabolismo , Fármacos Dermatológicos/química , Fármacos Dermatológicos/farmacocinética , Composição de Medicamentos , Humanos , Nanomedicina , Permeabilidade , Pele/metabolismo , Absorção Cutânea
10.
Pharmaceuticals (Basel) ; 13(8)2020 Jul 24.
Artigo em Inglês | MEDLINE | ID: mdl-32722238

RESUMO

The research work was designed to develop a solid self-nanoemulsifying drug delivery system (S-SNEDDS) of deferasirox (DFX). According to the solubility studies of DFX in different components, Peceol, Kolliphor EL, and Transcutol were selected as excipients. Pseudo-ternary phase diagrams were constructed, and then SNEDDS formation assessment studies and solubility of DFX in selected SNEDDSs formulations were performed. DFX loaded SNEDDS were prepared and characterized. The optimum DFX-SNEDDS formulations were developed. The relative safety of the optimized SNEDDS formulation was examined in a human immortalized myelogenous leukemia cell line, K562 cells, using the MTT cell viability test. Cytotoxicity studies revealed more cell viability (71.44%) of DFX loaded SNEDDS compared to pure DFX (3.99%) at 40 µM. The selected DFX-SNEDDS formulation was converted into S-SNEDDS by adsorbing into porous carriers, in order to study its dissolution behavior. The in vitro drug release studies indicated that DFX release (Q5%) from S-SNEDDS solidified with Neusilin UFL2 was significantly higher (93.6 ± 0.7% within 5 min) compared with the marketed product (81.65 ± 2.10%). The overall results indicated that the S-SNEDDS formulation of DFX could have the potential to enhance the solubility of DFX, which would in turn have the potential to improve its oral bioavailability as a safe novel delivery system.

11.
Turk J Pharm Sci ; 17(1): 43-48, 2020 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-32454759

RESUMO

OBJECTIVES: Microemulsions are fluid, isotropic, colloidal systems that have been widely studied as drug delivery systems. The percutaneous transport of active agents can be enhanced by their microemulsion formulation when compared to conventional formulations. The purpose of this study was to evaluate naftifine-loaded microemulsions with the objective of improving the skin permeation of the drug. MATERIALS AND METHODS: Microemulsions comprising oleic acid (oil phase), Kolliphor EL or Kolliphor RH40 (surfactant), Transcutol (co-surfactant), and water were prepared and physicochemical characterization was performed. In vitro skin permeation of naftifine from microemulsions was investigated and compared with that of its conventional commercial formulation. Attenuated total reflectance-Fourier transform infrared (ATR-FTIR) spectroscopy was used to evaluate the interaction between the microemulsions and the stratum corneum lipids. Candida albicans American Type Culture Collection (ATCC) 10231 and Candida parapsilosis were used to evaluate the antifungal susceptibility of the naftifine-loaded microemulsions. RESULTS: The microemulsion formulation containing Kolliphor RH40 as co-surfactant increased naftifine permeation through pig skin significantly when compared with the commercial topical formulation (p<0.05). ATR-FTIR spectroscopy showed that microemulsions increased the fluidity of the stratum corneum lipid bilayers. Drug-loaded microemulsions possessed superior antifungal activity against Candida albicans ATCC 10231 and Candida parapsilosis. CONCLUSION: This study demonstrated that microemulsions could be suggested as an alternative topical carrier with potential for enhanced skin delivery of naftifine.

12.
J Ocul Pharmacol Ther ; 36(6): 323-341, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32310723

RESUMO

Micelles have been studied in the targeting of drug substances to different tissues as a nano-sized delivery system for many years. Sustained drug release, ease of production, increased solubility, and bioavailability of drugs with low water solubility are the most important superiorites of micellar carriers. These advantages paved the way for the use of micelles as a drug delivery system in the ocular tissues. The unique anatomical structure of the eye as well as its natural barriers and physiology affect ocular bioavailability of the drugs negatively. Conventional dosage forms can only reach the anterior segment of the eye and are used for the treatment of diseases of this segment. In the treatment of posterior segment diseases, conventional dosage forms are administered sclerally, via an intravitreal injection, or systemically. However, ocular irritation, low patient compliance, and high side effects are also observed. Micellar ocular drug delivery systems have significant promise for the treatment of ocular diseases. The potential of micellar systems ocular drug delivery has been demonstrated by in vivo animal experiments and clinical studies, and they are continuing extensively. In this review, the recent research studies, in which the positive outcomes of micelles for ocular targeting of drugs for both anterior and posterior segment diseases as well as glaucoma has been demonstrated by in vitro, ex vivo, or in vivo studies, are highlighted.


Assuntos
Preparações de Ação Retardada/farmacocinética , Sistemas de Liberação de Medicamentos/métodos , Oftalmopatias/tratamento farmacológico , Soluções Oftálmicas/farmacocinética , Administração Oftálmica , Segmento Anterior do Olho/efeitos dos fármacos , Segmento Anterior do Olho/patologia , Disponibilidade Biológica , Preparações de Ação Retardada/administração & dosagem , Portadores de Fármacos/química , Humanos , Injeções Intravítreas , Micelas , Soluções Oftálmicas/administração & dosagem , Soluções Oftálmicas/efeitos adversos , Segmento Posterior do Olho/efeitos dos fármacos , Segmento Posterior do Olho/patologia , Solubilidade/efeitos dos fármacos , Propriedades de Superfície/efeitos dos fármacos
13.
Curr Pharm Des ; 26(14): 1543-1555, 2020.
Artigo em Inglês | MEDLINE | ID: mdl-32167423

RESUMO

BACKGROUND: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. OBJECTIVE: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. METHODS: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. RESULTS: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. CONCLUSION: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.


Assuntos
Antifúngicos , Micelas , Polietilenoglicóis/química , Triazóis/química , Portadores de Fármacos , Tamanho da Partícula
14.
Turk J Pharm Sci ; 17(6): 638-644, 2020 Dec 23.
Artigo em Inglês | MEDLINE | ID: mdl-33389954

RESUMO

OBJECTIVES: Polyurethanes (PUs) are a popular choice for composing nanofibers due to their spinnability, biocompatibility, high chemical stability, and good mechanical and elasticity properties. The desired release behaviors are also achieved by using combinations of PUs and various polymers. In this study, we investigated effects of polyvinylpyrrolidone (PVP) and ethyl cellulose (EC) on PU electrospun nanofibers in terms of morphological structures and drug release characteristics. MATERIALS AND METHODS: Nanofibers were prepared using blends of PU with either EC or PVP in different ratios by electrospinning. The effects of PVP or EC on the morphology and diameter of the prepared nanofibers were examined with scanning electron microscope (SEM). The compatibility of the components used in the formulations of nanofibers was determined by attenuated total reflection (ATR)-fourier-transform infrared (FTIR). Donepezil hydrochloride (DNP), a water soluble compound, was selected as a model drug to examine its release characteristics from both PU/PVP and PU/EC electrospun nanofibers. In vitro drug release studies from electrospun nanofibers were performed according to the method defined in the monograph as the "paddle over disk method" of United States Pharmacopeia 38. RESULTS: The SEM images showed that addition of EC or PVP to PU solutions did not affect the generation of nanofibers, and those formed had a smooth surface without beads in nanoscale. The ATR-FTIR spectra disclosed that EC and PVP were separately incorporated into the PU matrix. The in vitro release data indicated that the presence of EC or PVP in PU nanofibers dramatically changed the release behavior of DNP. PU/EC nanofibers (F4) provided sustained drug release with the Korsmeyer-Peppas drug release kinetic mechanism, in which the release rate was controlled by diffusion of the drug, while all of the PU/PVP nanofibers exhibited fast drug release. CONCLUSION: Overall, these characteristics of PU/EC (10/8) electrospun nanofibers has suggested their potential use as a drug carrier from which water-soluble drug release may occur in a sustained fashion.

15.
Pharm Dev Technol ; 25(4): 440-453, 2020 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-31851857

RESUMO

In this study, voriconazole (VCZ) incorporated polyvinyl alcohol/sodium alginate electrospun nanofibers were produced and, then crosslinked with glutaraldehyde for topical antifungal treatment. The nanofibers were characterized in terms of fiber size, surface morphology, and compatibility between drug-polymer and polymer-polymer using scanning electron microscopy, atomic force microscopy, attenuated total reflection-Fourier transform infrared spectroscopy, and high pressure liquid chromatography. After optimization studies, in vitro drug release, skin penetration, and deposition studies were performed using Franz diffusion cells. Antifungal activities of the nanofiber formulations against Candida albicans, Candida tropicalis, and Candida parapysilosis strains were evaluated using susceptibility test and subsequently time-kill study was performed against C. albicans. The cytotoxicity study was performed using 4-succinate dehydrogenase viability assay on mouse fibroblast cell line. The release rate of VCZ from crosslinked nanofibers was slower than that of non-crosslinked nanofibers and Higuchi kinetic model best fitted to the in vitro release data of both of formulations. VCZ deposited in deeper skin layers from nanofiber formulations was higher than that of the control formulation (VCZ solution in propylene glycol (1% (w/v)). According to the susceptibility and time-kill studies, all of the nanofiber formulations showed antifungal activity against C. albicans with confirming no cytotoxicity on mouse fibroblast cells.


Assuntos
Antifúngicos/administração & dosagem , Candida/efeitos dos fármacos , Sistemas de Liberação de Medicamentos , Nanofibras/química , Voriconazol/administração & dosagem , Administração Tópica , Alginatos/química , Animais , Antifúngicos/farmacocinética , Antifúngicos/farmacologia , Candidíase/tratamento farmacológico , Linhagem Celular , Liberação Controlada de Fármacos , Humanos , Camundongos , Álcool de Polivinil/química , Absorção Cutânea , Suínos , Voriconazol/farmacocinética , Voriconazol/farmacologia
16.
Braz. J. Pharm. Sci. (Online) ; 56: e18440, 2020. tab, graf
Artigo em Inglês | LILACS | ID: biblio-1249159

RESUMO

In this study, naftifine (a topical antifungal drug) loaded poly(vinyl) alcohol (PVA)/sodium alginate (SA) nanofibrous mats were prepared using the single-needle electrospinning technique. The produced nanofibers were crosslinked with glutaraldehyde (GTA) vapor. The morphology and diameter of the electrospun nanofibers were studied by scanning electron microscopy (SEM). SEM images showed the smoothness of the nanofibers and indicated that the fiber diameter increased with crosslinking and drug loading. Atomic force microscopy (AFM) images confirmed the uniform production of the scaffolds, and elemental mapping via energy dispersive X-ray spectroscopy (EDS) showed the uniform distribution of the drug within the nanofibers. An attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy study demonstrated that naftifine has sufficient secondary interactions with the polymer blend. The crosslinking treatment decreased the burst drug release effectively and the release mechanism followed Korsmeyer-Peppas Super Case-II transport. Overall, these findings suggest the potential use of naftifine-loaded PVA/SA nanofibers as a topical antifungal drug delivery system.


Assuntos
Administração Tópica , Nanofibras/análise , Espectrometria por Raios X/instrumentação , Análise Espectral/instrumentação , Preparações Farmacêuticas/administração & dosagem , Sistemas de Liberação de Medicamentos , Espectroscopia de Infravermelho com Transformada de Fourier/métodos , Microscopia de Força Atômica/instrumentação , Alginatos/efeitos adversos , Liberação Controlada de Fármacos
17.
Int J Pharm ; 551(1-2): 133-140, 2018 Nov 15.
Artigo em Inglês | MEDLINE | ID: mdl-30171899

RESUMO

The nanomicelles have recently drawn a great deal of attention for drug delivery into the skin. However, these carriers have only deposited in hair follicles and furrows, and drug in the micelles may not therapeutically reach into viable skin layers. The aim of this study was to formulate a combination of nanomicelles with terpenes to overcome this challenge and evaluate their potential for topical drug delivery into the skin. The nanomicelles were characterised with respect to size, size distribution (PDI), zeta potential, morphology and encapsulation efficiency (%). The drug accumulation and penetration were examined by tape stripping method in the skin. The colloidal stability of nanomicelles was followed with respect to size and PDI values. The nanomicelles were about 25-30 nm in size with narrow distribution. All of them had slightly negative surface charge, spherical shapes and high encapsulation efficiency (%). The tape stripping data revealed that nanomicelles consisting of terpinolene led to accumulation of more drug in the stripped skin as compared with commercial product and nanomicelles without terpene. Also, micelle formulations consisting of terpinolene (2.0%) had the highest colloidal stability. Consequently, combination of nanomicelles with terpinolene could be a feasible approach for enhancement of skin drug delivery.


Assuntos
Sistemas de Liberação de Medicamentos , Micelas , Nanoestruturas/administração & dosagem , Terpenos/administração & dosagem , Administração Cutânea , Animais , Poloxâmero/administração & dosagem , Pele/metabolismo , Suínos , Tacrolimo/administração & dosagem
18.
Ther Deliv ; 8(11): 967-985, 2017 11.
Artigo em Inglês | MEDLINE | ID: mdl-29061106

RESUMO

Nanocarriers used for alternative drug-delivery strategies have gained interest due to improved penetration and delivery of drugs into specific regions of the skin in recent years. Dermal drug delivery via polymeric-based nanocarriers (polymeric nanoparticles, micelles, dendrimers) and lipid-based nanocarriers (solid-lipid nanoparticles and nanostructured lipid carriers, vesicular nanocarriers including liposomes, niosomes, transfersomes and ethosomes) has been widely investigated. Although penetration of nanocarriers through the intact skin could be restricted, these carriers are particularly considered as feasible for the treatment of dermatological diseases in which the skin barrier is disrupted and also for follicular delivery of drugs for management of skin disorders such as acne. This review mainly highlights the recent approaches on potential penetration enhancement and targeting mechanisms of these nanocarriers.


Assuntos
Portadores de Fármacos/química , Lipídeos/química , Nanoestruturas/química , Polímeros/química , Pele/metabolismo , Administração Cutânea , Animais , Dendrímeros/química , Humanos , Lipossomos/química
19.
Curr Drug Metab ; 18(5): 454-468, 2017.
Artigo em Inglês | MEDLINE | ID: mdl-28228078

RESUMO

BACKGROUND: Psoriasis is a chronic autoimmune inflammatory skin disease affecting 2 to 3% of people worldwide. Topical therapy as first option in the management of psoriasis is an attractive strategy by delivering drugs efficiently into target sites of disease, minimizing systemic side effects of drugs and ensuring high patient compliance. However, the delivery of antipsoriatic agents via conventional topical formulations is limited due to their poor percutaneous penetration and targeting into deeper layers of the skin. METHOD: In this review, an overview of skin structure and psoriatic skin as well as different approaches used for the treatment are provided. We discussed the topical nanocarriers including solid lipid nanoparticles, nanostructured lipid carriers, liposomes, niosomes, ethosomes, transfersomes, dendrimers and micelles used to deliver antipsoriatic drugs. We also summarized the 2011 onward research studies dealing with the application of nanocarriers for psoriasis treatment. RESULT: In the last decades, numerous types of nanocarriers have been widely investigated as a novel delivery approach to reach effective antipsoriatic drug concentrations. These nanocarriers can enhance the therapeutic efficacy and minimize the toxicity of the drugs by lowering the dose. They also improve drug localization in the skin and achieve site-specific drug targeting. But, most of the available studies have lack of clinical outcome in psoriasis and required more focus on the clinical evaluation. CONCLUSION: Nanocarriers could enhance deposition of antipsoriatic drugs in targeted sites of the skin. Nevertheless, still there is a need to develop more effective simulated models that provide realistic model for psoriasis.


Assuntos
Administração Tópica , Sistemas de Liberação de Medicamentos , Nanoestruturas , Psoríase/tratamento farmacológico , Humanos , Absorção Cutânea
20.
Colloids Surf B Biointerfaces ; 146: 692-9, 2016 Oct 01.
Artigo em Inglês | MEDLINE | ID: mdl-27434156

RESUMO

The aim of this work was to optimize polymeric nano-sized micellar carriers of the anti-acne compound benzoyl peroxide (BPO) and to examine the ability of these carriers to deposit into hair follicles with the objective of improving skin delivery of BPO. BPO loaded polymeric micelles composed of Pluronic(®) F127 were prepared by the thin film hydration method and characterized in terms of size, loading capacity, morphology and physical stability. The optimized micelle formulation was then selected for skin delivery studies. The penetration of BPO loaded micellar carriers into skin and skin appendages across full thickness porcine skin was examined in vitro. Confocal microscopy images confirmed the penetration of Nile Red into hair follicles, which was loaded into micellar carriers as a model fluorescent compound. The relative safety of the polymeric micelles was evaluated with the MTT viability test using mouse embryonic fibroblasts. The results indicated that nano-sized polymeric micelles of BPO composed of Pluronic(®) F127 offer a potential approach to enhance skin delivery of BPO and that targeting of micelles into hair follicles may be an effective and safe acne treatment.


Assuntos
Peróxido de Benzoíla/química , Peróxido de Benzoíla/uso terapêutico , Portadores de Fármacos/química , Nanopartículas/química , Polímeros/química , Acne Vulgar/tratamento farmacológico , Animais , Linhagem Celular , Camundongos , Micelas
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