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1.
Molecules ; 27(9)2022 May 08.
Artículo en Inglés | MEDLINE | ID: mdl-35566374

RESUMEN

Valorization of wild plants to obtain botanical ingredients could be a strategy for sustainable production of cosmetics. This study aimed to select the rosehip extract containing the greatest amounts of bioactive compounds and to encapsulate it in vesicular systems capable of protecting their own antioxidant activity. Chemical analysis of Rosa canina L. extracts was performed by LC-DAD-MS/MS and 1H-NMR and vitamins, phenolic compounds, sugars, and organic acids were detected as the main compounds of the extracts. Liposomes, prepared by the film hydration method, together with hyalurosomes and ethosomes, obtained by the ethanol injection method, were characterized in terms of vesicle size, polydispersity index, entrapment efficiency, zeta potential, in vitro release and biocompatibility on WS1 fibroblasts. Among all types of vesicular systems, ethosomes proved to be the most promising nanocarriers showing nanometric size (196 ± 1 nm), narrow polydispersity (0.20 ± 0.02), good entrapment efficiency (92.30 ± 0.02%), and negative zeta potential (-37.36 ± 0.55 mV). Moreover, ethosomes showed good stability over time, a slow release of polyphenols compared with free extract, and they were not cytotoxic. In conclusion, ethosomes could be innovative carriers for the encapsulation of rosehip extract.


Asunto(s)
Rosa , Antioxidantes/química , Lípidos , Liposomas/química , Polifenoles/farmacología , Rosa/química , Espectrometría de Masas en Tándem
2.
Molecules ; 25(11)2020 May 31.
Artículo en Inglés | MEDLINE | ID: mdl-32486398

RESUMEN

The focus of this work was to prepare Spanish Broom, flax, and hemp dressings impregnated with glycyrrhetinic acid (GA) liposomes or hyalurosomes to promote the healing process and protect the skin wounds. Vesicles were prepared by the film hydration method and characterized in terms of size, particle size distribution, ζ potential, encapsulation efficiency, in vitro release, and biocompatibility on 3T3 fibroblasts. Loaded liposomes and hyalurosomes showed nanometric size (355 ± 19 nm and 424 ± 32 nm, respectively), good size distribution (lower than 0.3), and appropriate encapsulation efficiency (58.62 ± 3.25% and 59.22 ± 8.18%, respectively). Hyalurosomes showed good stability during the storage period, which can be correlated to the negative ζ potential, and allowed a fast and complete release of GA. Preliminary biological studies revealed that both kinds of loaded vesicles were not cytotoxic and that hyalurosomes could exert a slight stimulating effect on fibroblast proliferation. Finally, in vitro release studies from the different dressings impregnated with the loaded vesicles demonstrated that a high amount of GA could be reached at the wound site after 60 min from application. In conclusion, the results suggested that the developed dressings, especially those impregnated with hyalurosomes, can be efficiently used to promote the healing process.


Asunto(s)
Cannabis/química , Lino/química , Ácido Glicirretínico/química , Ácido Hialurónico/química , Liposomas/química , Spartium/química , Cicatrización de Heridas/efectos de los fármacos , Células 3T3 , Animales , Materiales Biocompatibles , Ciclo Celular , Proliferación Celular , Supervivencia Celular , Portadores de Fármacos , Fibroblastos/efectos de los fármacos , Ratones , Tamaño de la Partícula , Piel/lesiones
3.
Drug Dev Ind Pharm ; 41(6): 1017-25, 2015 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-24918172

RESUMEN

The aim of this study was to evaluate the capacity of cellulose films enriched with oleic acid and polysorbate 80 to enhance the transdermal permeation of propranolol hydrochloride. Polymeric films were prepared by casting and drying aqueous solutions of hydroxypropylmethylcellulose or carboxymethylcellulose and characterized in chemical-physical properties, such as drug content, thickness, morphology and water uptake capacity. In vitro transport experiments were performed in order to evaluate the permeation enhancing ability of oleic acid and polysorbate 80. All carboxymethylcellulose films showed lower cumulative amounts of drug permeated than hydroxypropylmethylcellulose. Moreover, films containing both oleic acid and polysorbate 80 provided a greater permeation in comparison to film without permeation enhancers or only with one of these. The results obtained confirm that propranolol hydrochloride permeation can be easily modulated by varying the cellulose and enhancer type used for film preparation.


Asunto(s)
Antagonistas Adrenérgicos beta/administración & dosificación , Excipientes/química , Propranolol/administración & dosificación , Absorción Cutánea , Administración Cutánea , Antagonistas Adrenérgicos beta/química , Antagonistas Adrenérgicos beta/farmacocinética , Animales , Carboximetilcelulosa de Sodio/química , Química Farmacéutica/métodos , Preparaciones de Acción Retardada , Derivados de la Hipromelosa/química , Ácido Oléico/química , Polisorbatos/química , Propranolol/química , Propranolol/farmacocinética , Porcinos
4.
Gels ; 9(5)2023 Apr 25.
Artículo en Inglés | MEDLINE | ID: mdl-37232954

RESUMEN

Rising environmental awareness drives green consumers to purchase sustainable cosmetics based on natural bioactive compounds. The aim of this study was to deliver Rosa canina L. extract as a botanical ingredient in an anti-aging gel using an eco-friendly approach. Rosehip extract was first characterized in terms of its antioxidant activity through a DPPH assay and ROS reduction test and then encapsulated in ethosomal vesicles with different percentages of ethanol. All formulations were characterized in terms of size, polydispersity, zeta potential, and entrapment efficiency. Release and skin penetration/permeation data were obtained through in vitro studies, and cell viability was assessed using an MTT assay on WS1 fibroblasts. Finally, ethosomes were incorporated in hyaluronic gels (1% or 2% w/v) to facilitate skin application, and rheological properties were studied. Rosehip extract (1 mg/mL) revealed a high antioxidant activity and was successfully encapsulated in ethosomes containing 30% ethanol, having small sizes (225.4 ± 7.0 nm), low polydispersity (0.26 ± 0.02), and good entrapment efficiency (93.41 ± 5.30%). This formulation incorporated in a hyaluronic gel 1% w/v showed an optimal pH for skin application (5.6 ± 0.2), good spreadability, and stability over 60 days at 4 °C. Considering sustainable ingredients and eco-friendly manufacturing technology, the ethosomal gel of rosehip extract could be an innovative and green anti-aging skincare product.

5.
Antibiotics (Basel) ; 11(8)2022 Aug 02.
Artículo en Inglés | MEDLINE | ID: mdl-36009909

RESUMEN

In recent years, the treatment of bacterial skin infections has been considered a major healthcare issue due to the growing emergence of antibiotic-resistant strains of Staphylococcus aureus. The incorporation of antibiotics in appropriate nanosystems could represent a promising strategy, able to overcome several drawbacks of the topical treatment of infections, including poor drug retention within the skin. The present work aims to develop microemulsions containing azithromycin (AZT), a broad-spectrum macrolide antibiotic. Firstly, AZT solubility in various oils, surfactants and co-surfactants was assessed to select the main components. Subsequently, microemulsions composed of vitamin E acetate, Labrasol® and Transcutol® P were prepared and characterized for their pH, viscosity, droplet size, zeta potential and ability to release the drug and to promote its retention inside porcine skin. Antimicrobial activity against S. aureus methicillin-resistant strains (MRSA) and the biocompatibility of microemulsions were evaluated. Microemulsions showed an acceptable pH and were characterized by different droplet sizes and viscosities depending on their composition. Interestingly, they provided a prolonged release of AZT and promoted its accumulation inside the skin. Finally, microemulsions retained AZT efficacy on MRSA and were not cytotoxic. Hence, the developed AZT-loaded microemulsions could be considered as useful nanocarriers for the treatment of antibiotic-resistant infections of the skin.

6.
Pharmaceutics ; 14(3)2022 Feb 26.
Artículo en Inglés | MEDLINE | ID: mdl-35335901

RESUMEN

The inclusion of a chemical permeation enhancer in a dosage form is considered an effective approach to improve absorption across the nasal mucosa. Herein we evaluated the possibility of exploiting biosurfactants (BS) produced by Lactobacillus gasseri BC9 as innovative natural excipients to improve nasal delivery of hydrocortisone (HC). BC9-BS ability to improve HC solubility and the BS mucoadhesive potential were investigated using the surfactant at a concentration below and above the critical micelle concentration (CMC). In vitro diffusion studies through the biomimetic membrane PermeaPad® and the same synthetic barrier functionalized with a mucin layer were assessed to determine BC9-BS absorption enhancing properties in the absence and presence of the mucus layer. Lastly, the diffusion study was performed across the sheep nasal mucosa using BC9-BS at a concentration below the CMC. Results showed that BC9-BS was able to interact with the main component of the nasal mucosa, and that it allowed for a greater solubilization and also permeation of the drug when it was employed at a low concentration. Overall, it seems that BC9-BS could be a promising alternative to chemical surfactants in the nasal drug delivery field.

7.
Eur J Pharm Biopharm ; 180: 190-200, 2022 Nov.
Artículo en Inglés | MEDLINE | ID: mdl-36210035

RESUMEN

The aim of this work was to develop novel chitosan (CH) based nanoparticles (NPs) for rifampicin (RIF) delivery. RIF, a lipophilic molecule, was incorporated inside NPs as a complex with an anionic cyclodextrin, sulphobutyl-ether-ß-cyclodextrin (SBE-ß-CD). NPs were then prepared through the ionic gelation method by exploiting the interaction between CH and SBE-ß-CD-RIF complex (CH/SBE-ß-CD-RIF NPs), possibly in the presence of other crosslinkers, like carboxymethylcellulose (CH/SBE-ß-CD-RIF/CMC NPs) and pentasodium tripolyphosphate (CH/SBE-ß-CD-RIF/TPP NPs). NPs were then characterized for their size, ζ-potential, morphology, yield, drug loading, stability, mucoadhesion, in vitro drug release and antimicrobial activity. Results demonstrated that the functional properties of loaded NPs, like their size, ζ-potential, and stability, varied on the basis of the CH/crosslinker weight ratio. Interestingly, all the developed NPs had a round shape and were characterized by high yield values and mucoadhesive properties. Among them, NPs based on CH/SBE-ß-CD-RIF and CH/SBE-ß-CD-RIF/CMC have gained high drug loading, provided a sustained release of RIF and showed the best antimicrobial activity. Thus, both types of NPs may be considered as promising nanocarriers for the release of RIF.


Asunto(s)
Antiinfecciosos , Quitosano , Ciclodextrinas , Nanopartículas , Rifampin/farmacología , Polímeros , Portadores de Fármacos , Tamaño de la Partícula
8.
Eur J Pharm Sci ; 179: 106294, 2022 Dec 01.
Artículo en Inglés | MEDLINE | ID: mdl-36116696

RESUMEN

The objective of this work was to optimize a thermosensitive in situ gelling formulation to improve intranasal and nose-to-brain delivery of the antiepileptic drug carbamazepine (CBZ). A preliminary procedure of vehicles obtained just mixing different fractions of poloxamer 407 (P407) and poloxamer 188 (P188) revealed preparations with phase transition temperatures, times to gelation and pH values suitable for nasal delivery. Subsequently, the mucoadhesive properties of the most promising formulations were tuned by adding hydroxypropylmethylcellulose types of different viscosity grades, and the effect of the adhesive polymers was evaluated by testing in vitro time and strength of mucoadhesion on specimens of sheep nasal mucosa. The formulation that showed the greatest mucoadhesive potential in vitro, with a time and force of mucoadhesion equal to 1746,75 s and 3.66 × 10-4 N, respectively, was that composed of 22% P407, 5% P188 and 0.8% HPMC low-viscous and it was further investigated for its ability to increase drug solubility and to control the release of the drug. Lastly, the capability of the candidate vehicle to ensure drug permeation across the biomimetic membrane Permeapad®, an artificial phospholipid-based barrier with a stratified architecture, and the same barrier enriched with a mucin layer was verified. The final formulation was characterized by a pH value of 6.0, underwent gelation at 32.33°C in 37.85 s, thus showing all the features required by in situ gelling thermosensitive preparations designed for nasal delivery and, more notably, it conserved the ability to favor drug permeation in the presence of mucin. These findings suggest that the optimized gelling system could be a promising and easy to realize strategy to improve CBZ delivery to the brain exploiting both a direct and indirect pathway.


Asunto(s)
Mucinas , Poloxámero , Animales , Ovinos , Geles/química , Poloxámero/química , Mucosa Nasal/metabolismo , Administración Intranasal , Excipientes/metabolismo , Carbamazepina/metabolismo , Temperatura , Encéfalo/metabolismo , Sistemas de Liberación de Medicamentos/métodos
9.
Antibiotics (Basel) ; 10(1)2021 Jan 01.
Artículo en Inglés | MEDLINE | ID: mdl-33401413

RESUMEN

The emergence of resistance to antifungal drugs has made the treatment of vulvovaginal candidiasis (VVC) very challenging. Among natural substances, biosurfactants (BS) produced by Lactobacillus have gained increasing interest in counteracting Candida infections for their proven anti-adhesive properties and safety profile. In the present study, liposomes (LP-BS) or liposomes coated with hyaluronic acid (HY-LP-BS) were prepared in the presence of the BS isolated from the vaginal strain Lactobacillus crispatus BC1 and characterized in terms of size, ζ potential, stability and mucoadhesion. The anti-biofilm activity of free BS, LP-BS and HY-LP-BS was investigated against different Candida albicans and non-albicans strains (C. glabrata, C. lusitaniae, C. tropicalis, C. krusei and C. parapsilosis), clinically isolated from patients affected by VVC. The inhibition of biofilm formation and the dispersal of pre-formed biofilm were evaluated. The obtained phospholipid vesicles showed suitable size for vaginal application and good stability over the storage period. HY-LP-BS exhibited good mucoadhesive properties and the best anti-biofilm profile, both in preventing or limiting the surface colonization by a broad spectrum of Candida species. In conclusion, the formulation of a novel antifungal agent derived from the vaginal microbiota into mucoadhesive nanocarriers appears to be a promising biotherapeutic strategy to counteract vulvovaginal candidiasis.

10.
Pharmaceutics ; 13(8)2021 Aug 03.
Artículo en Inglés | MEDLINE | ID: mdl-34452153

RESUMEN

The selection of an appropriate dressing for each type of wound is a very important procedure for a faster and more accurate healing process. So, the aim of this study was to develop innovative Spanish Broom and flax wound dressings, as alternatives to cotton used as control, with polymeric films containing glycyrrhetinic acid (GA) to promote wound-exudate absorption and the healing process. The different wound dressings were prepared by a solvent casting method, and characterized in terms of drug loading, water uptake, and in vitro release. Moreover, biological studies were performed to evaluate their biocompatibility and wound-healing efficacy. Comparing the developed wound dressings, Spanish Broom dressings with GA-loaded sodium hyaluronate film had the best functional properties, in terms of hydration ability and GA release. Moreover, they showed a good biocompatibility, determining a moderate induction of cell proliferation and no cytotoxicity. In addition, the wound-healing test revealed that the Spanish Broom dressings promoted cell migration, further facilitating the closure of the wound.

11.
Pharmaceutics ; 13(6)2021 May 31.
Artículo en Inglés | MEDLINE | ID: mdl-34073138

RESUMEN

One of the most widely used strategies to improve drug diffusion through the skin is the use of permeation enhancers. The aim of this work was to investigate the effect of two biosurfactants (BS), produced by Lactobacillus crispatus BC1 and Lactobacillus gasseri BC9, on the skin permeation profile of hydrocortisone (HC, model drug). HC aqueous solubility and in vitro diffusion studies through porcine skin were performed in the presence of BC1-BS and BC9-BS at concentrations below and above critical micellar concentrations (CMC). Moreover, skin hydration tests and differential scanning calorimetry (DSC) analysis were performed to further investigate BS interaction with the outermost layer of the skin. Both BS increased HC solubility, especially at concentrations above their CMC. At concentrations below the CMC, drug permeation through the skin was improved, as the result of a dual effect: a) the formation of a superficial lipophilic environment, as confirmed by the reduction in skin hydration and b) the interaction between BS and the stratum corneum (SC), as demonstrated by the DSC curves. From the obtained data, it appears that BC1-BS and BC9-BS could represent new promising green excipients for drug permeation enhancement through the skin.

12.
J Pharm Sci ; 110(4): 1676-1686, 2021 04.
Artículo en Inglés | MEDLINE | ID: mdl-33164786

RESUMEN

Buccal matrices represent a widely accepted dosage form permitting a convenient, easy, reliable drug administration and reducing administration errors. The aim of this study was the development of mucoadhesive buccal matrices for propranolol administration in children. Matrices were obtained by freeze-drying of drug loaded polymeric solutions based on gum tragacanth (GT), pectin (PEC), hydroxypropylmethylcellulose (HPMC), sodium hyaluronate (HA), gelatin (GEL), chitosan (CH) or a mixture of CH and HPMC (CH/HPMC). Matrices were characterized for drug solid state, morphology, water-uptake, mucoadhesion ability, in vitro drug release and permeation through porcine epithelium. The most promising formulations were tested for in vitro biocompatibility in human dental pulp fibroblasts. The preparative method and the polymeric composition influenced the drug solid state, as a complete amorphization as well as different polymorphic forms were observed. GEL and PEC guaranteed a fast and complete drug release due to their rapid dissolution, while for the other matrices the release was influenced by drug diffusion through the viscous gelled matrix. Moreover, matrices based on CH and CH/HPMC showed the best mucoadhesive properties, favoured the drug permeation, in virtue of CH ability to interfere with the lipid organization of biological membrane, and were characterized by a good biocompatibility profile.


Asunto(s)
Mucosa Bucal , Propranolol , Administración Bucal , Animales , Niño , Sistemas de Liberación de Medicamentos , Liberación de Fármacos , Liofilización , Humanos , Mucosa Bucal/metabolismo , Propranolol/metabolismo , Porcinos
13.
Int J Pharm ; 580: 119228, 2020 Apr 30.
Artículo en Inglés | MEDLINE | ID: mdl-32184180

RESUMEN

The objective of this study was the development of different solid formulations, such as wafers and films, for buccal administration of ondansetron, a selective and potent antagonist of 5-hydroxytryptamine 3 receptors used in children for the treatment of nausea and vomiting. Wafers and films have been prepared drying an aqueous solution of pectin, hydroxypropyl methylcellulose, sodium hyaluronate, sodium carboxymethylcellulose, chitosan or gelatin, through lyophilization or oven. Formulations were characterized in terms of morphology, drug solid state and ability to hydrate, adhere to mucosa, release and favour the permeation of the drug through porcine esophageal epithelium, used as model of human buccal epithelium. The most promising formulations were tested for in vitro biocompatibility in human pulp fibroblasts. Films showed greater hydration and mucoadhesion abilities and allowed the release and the permeation of a greater amount of ondansetron with respect to wafers. Chitosan or hyaluronate provided films with the best mucoadhesion properties and good biocompatibility profile. Moreover, chitosan based film allowed to obtain the highest amount of permeated drug and could represent a novel child-appropriate dosage form able to combine the advantages of solid dosage form with the possibility to avoid the swallowing.


Asunto(s)
Ondansetrón/administración & dosificación , Ondansetrón/química , Adhesividad , Administración Bucal , Animales , Carboximetilcelulosa de Sodio/química , Química Farmacéutica/métodos , Quitosano/química , Formas de Dosificación , Composición de Medicamentos/métodos , Sistemas de Liberación de Medicamentos/métodos , Liofilización/métodos , Gelatina/administración & dosificación , Gelatina/química , Mucosa Bucal/metabolismo , Pediatría/métodos , Porcinos
14.
Pharmaceutics ; 12(3)2020 Mar 08.
Artículo en Inglés | MEDLINE | ID: mdl-32182651

RESUMEN

The aim of this work was to prepare mucoadhesive buccal films for local release of Lactobacillus brevis CD2, which shows interesting anti-inflammatory properties due to its high levels of arginine deiminase. Hydroxypropylmethylcellulose-based films were prepared by means of a modified casting method, which allowed L. brevis CD2 loading on one side of the film, before its complete drying. Three batches of films were prepared, stored at +2-8 °C and +23-25 °C for 48 weeks and characterized in terms of physico-chemical and functional properties. For each batch, the L. brevis viable count and arginine deiminase activity were evaluated at different time points in order to assess functional property maintenance over time. Moreover, the mucoadhesive properties and ability of the films to release L. brevis CD2 were evaluated. A good survival of L. brevis CD2 was observed, particularly at the storage temperature of +2-8 °C, while the activity of arginine deiminase was maintained at both temperature values. Films showed good mucoadhesive properties and guaranteed a prolonged release of viable lactobacilli, which can be directed towards the whole buccal cavity or specific mucosa lesions. In conclusion, the proposed preparative method can be successfully employed for the production of buccal films able to release viable L. brevis CD2 cells that maintain the anti-inflammatory enzymatic activity.

15.
J Pharm Pharmacol ; 61(1): 41-6, 2009 Jan.
Artículo en Inglés | MEDLINE | ID: mdl-19126295

RESUMEN

OBJECTIVES: The aim of this study was to describe a colon-specific delivery system based on pectin hydrogels formed by complexation with chitosan. METHODS: Hydrogels were prepared at different weight ratios (4:1, 7:1, 10:1; pectin/chitosan), loaded with vancomycin hydrochloride (2:1, 4:1; polymer/drug weight ratio) and collected by spray-drying. The microspheres obtained were characterized in terms of morphology, swelling behaviour, mucoadhesive properties and drug loading efficiency. The influence of different pectin/chitosan hydrogels on the release behaviour of microspheres at pH 2.0, 5.5 and 7.4 were evaluated in vitro with and without pectinolytic enzyme. KEY FINDINGS: The results showed that water uptake was increased by raising the environmental pH (from 2.0 to 7.4) and the pectin/chitosan weight ratio, while drug availability was increased by raising the environmental pH (from 2.0 to 7.4) and decreased by raising the pectin/chitosan weight ratio. In the presence of pectinase, the glycoside bonds of pectin were degraded and a considerable amount of drug was released in a short time. CONCLUSIONS: This study suggested that pectin/chitosan microspheres were able to limit the release of vancomycin under acidic conditions and release it under simulated colonic conditions, confirming their potential for a colon-specific drug delivery system.


Asunto(s)
Colon/metabolismo , Sistemas de Liberación de Medicamentos/métodos , Microesferas , Pectinas/química , Vancomicina/administración & dosificación , Animales , Antibacterianos/administración & dosificación , Antibacterianos/química , Antibacterianos/farmacocinética , Disponibilidad Biológica , Quitosano/química , Liofilización/métodos , Humanos , Hidrogeles/química , Concentración de Iones de Hidrógeno , Microscopía Electrónica de Rastreo , Poligalacturonasa/química , Poligalacturonasa/metabolismo , Espectroscopía Infrarroja por Transformada de Fourier , Tecnología Farmacéutica/métodos , Vancomicina/química , Vancomicina/farmacocinética , Agua/química , Agua/metabolismo
16.
J Pharm Pharmacol ; 61(2): 151-7, 2009 Feb.
Artículo en Inglés | MEDLINE | ID: mdl-19178761

RESUMEN

OBJECTIVES: The purpose of this study was the preparation and characterisation of mucoadhesive nasal inserts based on chitosan/hyaluronate polyelectrolyte complexes prepared at various pHs and at different molar ratios. METHODS: A suspension of chitosan/hyaluronate complexes with or without the model drugs (vancomycin or insulin) was lyophilised into small inserts. Complexation yield, FT-IR spectra and thermogravimetric analysis were used to study the degree of interactive strength between polyions. In-vitro swelling, mucoadhesion and release tests were performed in order to investigate delivery of vancomycin and insulin in the nasal cavity. KEY FINDINGS: The results indicated that the selection of complex preparative conditions allows modulation of insert swelling and mucoadhesion ability. Nasal inserts containing vancomycin or insulin had showed completely different drug release behaviour. CONCLUSIONS: Chitosan/hyaluronate polyelectrolyte complexes can be used for the formulation of mucoadhesive nasal inserts for the delivery of peptide and protein drugs.


Asunto(s)
Adhesivos/metabolismo , Quitosano/química , Sistemas de Liberación de Medicamentos/métodos , Ácido Hialurónico/química , Mucosa Nasal/metabolismo , Péptidos/administración & dosificación , Proteínas/administración & dosificación , Adhesivos/química , Administración Intranasal , Concentración de Iones de Hidrógeno , Insulina/farmacocinética , Mucosa Nasal/efectos de los fármacos , Péptidos/farmacocinética , Proteínas/farmacocinética , Espectroscopía Infrarroja por Transformada de Fourier , Termogravimetría , Vancomicina/farmacocinética , Viscosidad , Agua/química , Agua/metabolismo
17.
CNS Drugs ; 33(9): 849-865, 2019 09.
Artículo en Inglés | MEDLINE | ID: mdl-31493244

RESUMEN

The aim of this article is to provide the rationale for the development of transdermal formulations of antipsychotics by highlighting their main advantages, starting with an overview of the antipsychotic formulations that are currently available on the market. Progress regarding transdermal antipsychotic formulations was investigated by performing a search of papers, patents and clinical trials published in the last 10 years. Available data on antipsychotic transdermal formulations are reported and discussed, focusing on the characteristics of the dosage forms and their ability to promote drug absorption. Despite the current availability of a large number of antipsychotics, only a few of these drugs (e.g. aripiprazole, asenapine, blonanserin, chlorpromazine, haloperidol, olanzapine, prochlorperazine, quetiapine, and risperidone) have been developed as transdermal delivery systems. Several papers and patents show that transdermal formulations, such as creams, films, gels, nanosystems, patches, solutions, and sprays, have been evaluated with the aim of expanding the clinical utility of antipsychotic drugs. In particular, the employment of different strategies, such as the use of nanoparticles/vesicles, or permeation enhancers as well as microneedles with iontophoresis, may improve the absorption of antipsychotic drugs through the skin. However, few clinical trials on transdermal delivery of antipsychotic drugs are available and only delivery systems containing asenapine and blonanserin have shown interesting clinical results in terms of pharmacokinetic data, efficacy, and tolerability. Recently, the transdermal patch formulation of blonanserin was approved in Japan for the treatment of schizophrenia.


Asunto(s)
Antipsicóticos/farmacología , Antipsicóticos/uso terapéutico , Administración Cutánea , Animales , Ensayos Clínicos como Asunto , Sistemas de Liberación de Medicamentos , Humanos
18.
Eur J Pharm Sci ; 131: 136-145, 2019 Apr 01.
Artículo en Inglés | MEDLINE | ID: mdl-30771474

RESUMEN

The aim of this work was to prepare new mucoadhesive nasal decongestant nanoparticles obtained by direct crosslinking between the cationic polymer chitosan and the anionic drug cromolyn. Different chitosan/cromolyn molar ratios were used in order to obtain nanoparticles of suitable size, encapsulation efficiency/drug loading and mucoadhesion. Moreover, the ability of the nanoparticles to deliver cromolyn into and through the nasal mucosa was evaluated. The obtained positively charged nanoparticles, sized 180-400 nm, showed interesting properties in terms of yield, mucoadhesion, encapsulation efficiency and drug loading. Release and permeation/penetration data indicated the ability of the nanoparticles to retain a high amount of cromolyn inside the mucosa, which is rich in mast cells. These findings suggest developing decongestant nanoparticles for potential treatment of allergic rhinitis.


Asunto(s)
Antialérgicos/química , Quitosano/química , Cromolin Sódico/química , Nanopartículas/química , Adhesividad , Animales , Antialérgicos/administración & dosificación , Quitosano/administración & dosificación , Cromolin Sódico/administración & dosificación , Liberación de Fármacos , Nanopartículas/administración & dosificación , Mucosa Nasal/metabolismo , Permeabilidad , Rinitis Alérgica/tratamiento farmacológico , Ovinos
19.
J Pharm Sci ; 108(7): 2447-2457, 2019 07.
Artículo en Inglés | MEDLINE | ID: mdl-30853513

RESUMEN

Chlorhexidine (CLX) is a wide spectrum cationic antimicrobial used for prevention and treatment of infections of buccal and vaginal cavities. To increase the residence time of CLX-based formulations at the application site and consequently reduce the daily dose frequency, new formulations composed of mucoadhesive polymers should be designed. The objective of this work was the development of matrices based on polyanionic polymers, such as sodium alginate, carboxymethylcellulose, xanthan gum and sodium hyaluronate, aimed to prolong the local release of CLX into the buccal or vaginal cavity. Matrices were prepared by freeze-drying and comply with 2 different preparative methods and characterized in terms of resistance to compression, water uptake ability, mucoadhesion, in vitro drug release behavior and antimicrobial activity toward representative pathogens of buccal and vaginal cavities. Results showed that the selection of suitable polymers associated to the adequate preparative method allowed to modulate matrix ability to hydrate, adhere to the mucosa and release the drug as well as to exert antimicrobial activity. In particular, matrix based on sodium hyaluronate was found to be the best performing formulation and could represent a versatile system for local release of CLX with potential application in both buccal and vaginal cavities.


Asunto(s)
Clorhexidina/química , Polímeros/química , Adhesividad , Administración Bucal , Administración Intravaginal , Animales , Antiinfecciosos/química , Sistemas de Liberación de Medicamentos/métodos , Liberación de Fármacos , Femenino , Liofilización/métodos , Ácido Hialurónico/química , Mucosa Bucal/metabolismo , Polielectrolitos , Porcinos , Vagina/metabolismo
20.
Eur J Pharm Biopharm ; 139: 246-252, 2019 Jun.
Artículo en Inglés | MEDLINE | ID: mdl-30991089

RESUMEN

Staphylococcus aureus is the major causative agent of skin and soft tissue infections, whose prevention and treatment have become more difficult due to the emergence of antibiotic-resistant strains. In this regard, the development of an effective treatment represents a challenge that can be overcome by delivering new antibiofilm agents with appropriate nanocarriers. In this study, a biosurfactant (BS) isolated from Lactobacillus gasseri BC9 and subsequently loaded in liposomes (LP), was evaluated for its ability to prevent the development and to eradicate the biofilm of different methicillin resistant S. aureus (MRSA) strains. BS from L. gasseri BC9 was not cytotoxic and was able to prevent formation and to eradicate the biofilm of different MRSA strains. BS loaded liposomes (BS-LP) presented a mean diameter (lower than 200 nm) suitable for topical administration and a low polydispersity index (lower than 0.2) that were maintained over time for up 28 days. Notably, BS-LP showed higher ability than free BS to inhibit S. aureus biofilm formation and eradication. BS-LP were loaded in lyophilized matrices able to quickly dissolve (dissolution time lower than 5 s) upon contact with exudate, thus allowing vesicle reconstitution. In conclusion, in this work, we demonstrated the antibiofilm activity of Lactobacillus-derived BS and BS-LP against clinically relevant MRSA strains. Furthermore, the affordable production of lyophilized matrices containing BS-LP for local prevention of cutaneous infections was established.


Asunto(s)
Antibacterianos/administración & dosificación , Biopelículas/efectos de los fármacos , Productos Biológicos/administración & dosificación , Lactobacillus gasseri , Staphylococcus aureus Resistente a Meticilina/fisiología , Tensoactivos/administración & dosificación , Células 3T3 , Animales , Antibacterianos/aislamiento & purificación , Productos Biológicos/aislamiento & purificación , Evaluación Preclínica de Medicamentos , Humanos , Liposomas , Staphylococcus aureus Resistente a Meticilina/efectos de los fármacos , Ratones , Pruebas de Sensibilidad Microbiana , Infecciones Estafilocócicas/tratamiento farmacológico , Infecciones Estafilocócicas/microbiología , Infecciones Cutáneas Estafilocócicas/tratamiento farmacológico , Infecciones Cutáneas Estafilocócicas/microbiología , Tensoactivos/aislamiento & purificación
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