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1.
Int J Mol Sci ; 22(2)2021 Jan 17.
Article in English | MEDLINE | ID: mdl-33477393

ABSTRACT

The aim of this work was the development of microstructured lipid carriers (MLC) based on chitosan (CH) and containing N-acetylcysteine (NAC), a mucolytic and antioxidant agent, to inhibit the formation of Pseudomonas aeruginosa biofilm. MLC were prepared using the high shear homogenization technique. The MLC were characterized for morphology, particle size, Z potential, encapsulation efficiency and drug release. The antioxidant properties of NAC-loaded microstructured carriers were evaluated through an in vitro spectrophotometer assay. Finally, the activity of NAC-CH-MLC on biofilm production by Pseudomonas aeruginosa was also evaluated. Results obtained from this study highlighted that the use of chitosan into the inner aqueous phase permitted to obtain microstructured particles with a narrow size range and with good encapsulation efficiency. NAC-loaded MLC showed higher antioxidant activity than the free molecule, demonstrating how encapsulation increases the antioxidant effect of the molecule. Furthermore, the reduction of biofilm growth resulted extremely high with MLC being 64.74% Ā± 6.2% and 83.74% Ā± 9.95%, respectively, at 0.5 mg/mL and 2 mg/mL. In conclusion, this work represents a favorable technological strategy against diseases in which bacterial biofilm is relevant, such as cystic fibrosis.


Subject(s)
Acetylcysteine/pharmacology , Chitosan/pharmacology , Drug Delivery Systems/methods , Anti-Infective Agents/pharmacology , Biofilms/drug effects , Drug Liberation , Lipids/pharmacology , Microbial Sensitivity Tests , Nanoparticles , Particle Size , Pseudomonas Infections/drug therapy , Pseudomonas aeruginosa/drug effects , Pseudomonas aeruginosa/metabolism
2.
Skin Res Technol ; 26(3): 422-430, 2020 May.
Article in English | MEDLINE | ID: mdl-31802538

ABSTRACT

BACKGROUND: Nowadays, nail care products are extremely important both in medical and cosmetic fields. Actually, there are only a very few "in vivo" methods to evaluate the safety and the efficacy of nail products. METHODS: The new apparatus, based on a recently patented technology, is developed for the "in vivo" evaluation of nails in terms of thickness, structural firmness, flattening, and bending properties. The device analyzes nails by an "in vivo" non-invasive methodology in a timely way and with high accuracy. The assessment of the resistance to compression measures the cohesion of the nail matrix (nail firmness), while the evaluation of the resistance to transversal deformation detects the elasticity of the nail plate. Furthermore, the apparatus is able to assess the nail thickness and the flexibility of their distal edge. RESULTS: The instrument provides nail thickness and several parameters reflecting mechanical properties of nail plate: Viscoelasticity expressed as viscoelasticity index (VI), structural strength/ firmness expressed as Firmness Index (FI), and viscoelasticity of the distal edge expressed as Bending Index (BI). CONCLUSIONS: The instruments described in this work represent an innovative apparatus for the safety and efficacy evaluation of nail products in several fields: cosmetics, pharmaceuticals, and medical devices.


Subject(s)
Biomechanical Phenomena/physiology , Nail Diseases/psychology , Nails/anatomy & histology , Adult , Cosmetics , Elasticity/physiology , Extracellular Matrix , Female , Humans , Keratins/metabolism , Keratins/physiology , Middle Aged , Nail Diseases/epidemiology , Patents as Topic
3.
Drug Dev Ind Pharm ; 43(11): 1792-1800, 2017 Nov.
Article in English | MEDLINE | ID: mdl-28581831

ABSTRACT

N-Acetyl-d-glucosamine (NAG) has been recently considered for topical treatment of hyperpigmentation disorders due to its inhibitory effect on thyrosinase enzymes in melanocytes. NAG is a precursor of hyaluronic acid, increasing its amount in skin, and consequently, preserving the skin hydration and elasticity. It may also act as an emulsion stabilizer. Solid lipid nanoparticles (SLN) are advanced delivery systems successfully used in pharmaceutical and cosmetic formulations for the improvement of active molecules penetration into the skin. Therefore, this work aimed to develop and characterize stable and scalable topical formulations containing NAG-loaded SLN. NAG was incorporated in SLN which were prepared by two high shear homogenizers and characterized regarding its morphology and particle size by transmission electron microscopy and photon correlation spectroscopy, respectively. Oil emulgel and hydrogel were used as carriers of NAG-loaded SLN. Several parameters were evaluated, including the droplet size distribution, rheology, pH and topical delivery by different techniques. It was observed that SLN size was significantly dependent on NAG incorporation and homogenization process. Most tested SLN parameters appeared to be quite suitable, that is, spherical and well-defined SLN with approximately 258 nm and -30 mV. Hereafter, both gels containing SLN presented a pseudoplastic flow. Emulgel formulation containing NAG-loaded SLN allowed a higher NAG permeation through the SC compared to the respective control (about 0.8Ā Āµgcm-2 h-1). According to the results obtained, it can be suggested that NAG acts as an emulsion stabilizer. This stabilization was also particularly dependent on the homogenizer type which is quite important for scale-up process. This study demonstrated the potential of scalable SLN formulations to improve NAG topical delivery contributing to the improvement of skin properties on several skin disorders.


Subject(s)
Acetylglucosamine/chemistry , Calorimetry, Differential Scanning/methods , Cosmetics/chemistry , Gels/chemistry , Lipids/chemistry , Microscopy, Electron, Transmission/methods , Nanoparticles/chemistry , Acetylglucosamine/pharmacology , Administration, Topical , Chemistry, Pharmaceutical , Cosmetics/administration & dosage , Gels/pharmacology , Lipids/pharmacology , Particle Size
4.
Pharmaceuticals (Basel) ; 16(12)2023 Dec 08.
Article in English | MEDLINE | ID: mdl-38139830

ABSTRACT

Nowadays, acne vulgaris therapies are often unsuccessful. One of the responsible factors for the formation of comedones and inflammatory lesions could be the peroxidation of squalene, a hydrocarbon representing one of the major components of human sebum. This peroxidation is increased by solar irradiation. The purpose of this work was to set up an in vivo method for the extraction and quantification of squalene from acne skin and to correlate the results with biophysical skin parameters such as sebum amount, protein content and TEWL. Healthy volunteers were used as control. The results obtained demonstrated that acne-prone skin had a major quantity of squalene, and, in the stratum corneum area, its peroxide form is present. Moreover, Spearman's rank correlation showed a positive correlation between sebum content and peroxide squalene and between porphyrin intensity and peroxide squalene.

5.
J Cosmet Dermatol ; 22(2): 517-528, 2023 Feb.
Article in English | MEDLINE | ID: mdl-35796684

ABSTRACT

BACKGROUND: Actually, the use of chemical peels in cosmetics and dermatology continues to grow due to their versatility, clinical endpoint-directed predictability, and favorable risk profile in comparison to lasers. The chemical peel is a generally safe method for treatment of some skin disorders and to refresh and rejuvenate the skin. The major challenge of chemical peels is the tolerability, that is because of sensitive skin which is one of the most common skin disorders. AIM: The aim of this study was to evaluate the effectiveness of the new Miamo Renewal Peel Serum formulated with a pool of new generation acids (ELPA25™) on sensitive skin with respect to mandelic acid serum only and with respect to placebo comparison. MATERIALS AND METHODS: The "in vivo" study following the half-face experimental protocol active versus placebo involved 30 healthy Caucasian female volunteers between 25 and 64 years, with sensitive skin, who were divided into two different groups. ELPA25™ serum was applied in one group three times a week for 8 weeks. The other group, with the same protocol, applied an active serum containing mandelic acid, as control, versus placebo. In particular, skin moisturizing, skin viscoelastic properties, skin surface smoothness, wrinkle reduction, and stratum corneum renewal were evaluated. RESULTS: Renewal Peel Serum was very well tolerated from sensitive skin. A significant decrease in skin roughness and wrinkle breadth, and an improvement in firmness and in skin elasticity, was observed after 2Ā months of treatment with respect both to mandelic acid serum and to placebo comparison. CONCLUSIONS: Scientific protocol using self-controlled study methodology and noninvasive skin bioengineering techniques with adequate statistical methods were able to evaluate both the safety and the efficacy of the new Miamo Renewal Peel Serum. This study highlighted that the Miamo Renewal Peel Serum formulated with a patent-pending mixture of new generation acids (ELPA25™) exerts many beneficial effects and it can be successfully employed for sensitive skin.


Subject(s)
Chemexfoliation , Skin Aging , Skin Diseases , Female , Humans , Chemexfoliation/adverse effects , Chemexfoliation/methods , Mandelic Acids/adverse effects , Skin , Skin Diseases/chemically induced , Treatment Outcome
6.
J Cosmet Dermatol ; 22(12): 3329-3339, 2023 Dec.
Article in English | MEDLINE | ID: mdl-37803998

ABSTRACT

BACKGROUND: The cumulative oxidative damage causes an acceleration in the skin aging. OBJECTIVES: To evaluate the ability of a new patented matrix of lipid particles (SIREN CAPSULE TECHNOLOGY™) to have superior anti-aging properties due to its high sensitivity to reactive oxygen species (ROS), testing its efficacy versus free or encapsulated vitamins. METHODS: An inĀ vitro study was conducted to evaluate the protective effects of lipid particles using menadione as an enhancer of oxidative stress. Subsequently, inĀ vivo studies evaluated skin hydration, skin barrier function, and smoothness and wrinkle depth. For this purpose, gels containing free or encapsulated vitamins were used as controls. RESULTS: In vitro, the SIREN CAPSULE TECHNOLOGY™ gel shows inhibitory activity against ROS production through menadione induction. In fact, at both tested concentrations, ROS production is lower than in the control samples (placebo, free vitamins, encapsulated vitamins). In vivo, the net effect of SIREN CAPSULE TECHNOLOGY™ gel versus the others permitted to conclude that lipid particles exert a higher skin moisturizing effect (20.17%) and a stronger effect in reducing transepidermal water loss (-16.29%) after 4 weeks of treatment. As for surface analysis, a gel based on SIREN CAPSULE TECHNOLOGY™ improves the skin texture in a similar way than gel containing encapsulated vitamins (Ra and Rz variations in 4 weeks). CONCLUSIONS: SIREN CAPSULE TECHNOLOGY™ represents an advance and a successful strategy to develop cosmetic products for the treatment of skin conditions associated with an accumulation of ROS. SIREN CAPSULE TECHNOLOGY™ represents a result-oriented breakthrough in the effective delivery of active ingredients to the skin.


Subject(s)
Cosmetics , Skin Aging , Humans , Aged , Reactive Oxygen Species , Vitamin K 3/pharmacology , Skin , Cosmetics/pharmacology , Vitamins/pharmacology , Vitamin A , Lipids/pharmacology
7.
Biomedicines ; 11(3)2023 Mar 21.
Article in English | MEDLINE | ID: mdl-36979945

ABSTRACT

The concept of skin microbiota is not really clear and more accurate approaches are necessary to explain how microbial flora can influence skin biophysical parameters in healthy individuals and in pathology patients with non-infectious skin disease. The aim of this work is to provide a suitable, fast and reproducible protocol to correlate skin parameters with the composition of skin microbiota. For this purpose, the work was split into two main phases. The first phase was focused on the selection of volunteers by the administration of a specific questionnaire. The skin microbiota was then collected from the forehead of selected volunteers as a test area and from the shoulder as control area. On the same skin area, the biophysical parameters, such as trans-epidermal water loss (TEWL), sebum level (SL), porphyrin intensity, keratin content and stratum corneum water content were taken. All parameters were taken at t0 and after 15 days without changes in the volunteers' lifestyle. A strong correlation was found between forehead and shoulder area for porphyrin intensity, pH and TEWL parameters, and between Cutibacterium acnes and some biophysical parameters both in the forehead and the shoulder area. The procedural setup in this work represents the starting point for evaluating problematic skins and the efficacy of cosmetic products or treatment against skin dysbiosis.

8.
Skin Res Technol ; 18(1): 45-54, 2012 Feb.
Article in English | MEDLINE | ID: mdl-21492243

ABSTRACT

BACKGROUND: There is a rising debate concerning the possible side effects arising from the use of particles at nanosize since the production of nanomaterials is increasing worldwide. Nanoparticles are able to enter the body through the skin, lungs or intestinal tract, depositing in several organs, and the risk associated with exposure to them, the routes of entry and the molecular mechanisms of any cytotoxicity need to be well understood. The aim of this work was to evaluate the suitability of skin replica as a method to study the colloidal systems visualization and distribution on skin surface. METHODS: Solid lipid nanoparticles (SLN) were used as carrier systems. Skin replicas on healthy volunteers, before and after SLN application, were prepared and visualized using profilometry and scanning electron microscopy (SEM). RESULTS: The results obtained in our study show that skin replica represents a suitable method to study the colloidal systems and their interaction with the skin surface. CONCLUSION: Profilometry enabled us to observe the systems distribution on a cutaneous texture. In addition, SEM, thanks to its high magnifications and field depth, allowed us to evaluate particles' distribution on the skin texture and the interaction between particles of different compositions and replica silicone.


Subject(s)
Biomimetic Materials/analysis , Hardness Tests/methods , Microscopy, Electron/methods , Nanoparticles/ultrastructure , Skin/chemistry , Skin/ultrastructure , Adolescent , Child , Female , Humans , Male , Pilot Projects , Surface Properties , Young Adult
9.
Biomedicines ; 10(10)2022 Oct 09.
Article in English | MEDLINE | ID: mdl-36289784

ABSTRACT

The skin harbors a huge number of different microorganisms such as bacteria, fungi and viruses, and it acts as a protective shield to prevent the invasion of pathogens and to maintain the health of the commensal microbiota. Several studies, in fact, have shown the importance of the skin microbiota for healthy skin. However, this balance can be altered by intrinsic and extrinsic factors, leading to the development of skin disease, such as acne vulgaris (AV), atopic dermatitis (AD) and rosacea(RS). Although these diseases are widespread and affect both adolescents and adults, the scientific correlation between these disorders and the skin microbiota and physiological parameters (TEWL, hydration and lipid composition) is still unclear. This review aims to investigate the current literature regarding the correlation between the skin microbiota and its imbalance underlying microbiological aspects, how the skin microbiota changes over the course of the disease and the current possible treatments. The following reported studies show a general imbalance of the bacterial flora. For this reason, more in-depth studies are necessary to explore the different subspecies and strains involved in all three diseases.

10.
Pharmaceutics ; 14(1)2022 Jan 12.
Article in English | MEDLINE | ID: mdl-35057065

ABSTRACT

Different mucoadhesive systems have been studied in recent years to increase the residence time of the delivery systems and to prolong the release of the drug. The aim of this work was to evaluate the mucoadhesive properties of chitosan-based Microstructured Lipid Carrier (CH-MLC) with a new approach which requires chitosan and mucin to be compacted into a tablet and mucoadhesion to be assessed on a non-mucoadhesive substrate. This type of test showed that chitosan maintains a close bond with mucin even in the presence of a fluid and even encapsulated in microparticles. After this, using a bioreactor, the release of N-acetylcysteine (NAC) from the microparticles (NA-CH-MLC) through a layer of mucus mimicking the pathological conditions of a patient with cystic fibrosis was tested. The release of the active from NAC-CH-MLC demonstrated how the chitosan inside the microparticles acts as a penetration enhancer and how the microparticles can impart a prolonged release over time.

11.
Pharmaceuticals (Basel) ; 15(2)2022 Feb 11.
Article in English | MEDLINE | ID: mdl-35215328

ABSTRACT

N-acetylcysteine is the acetylated form of the amino acid L-cysteine and a precursor to glutathione (GSH). It has been known for a long time as a powerful antioxidant and as an antidote for paracetamol overdose. However, other activities related to this molecule have been discovered over the years, making it a promising drug for diseases such as cystic fibrosis (CF). Its antioxidant activity plays a key role in CF airway inflammation and redox imbalance. Furthermore, this molecule appears to play an important role in the prevention and eradication of biofilms resulting from CF airway infections, in particular that of Pseudomonas aeruginosa. The aim of this review is to provide an overview of CF and the role that NAC could play in preventing and eliminating biofilms, as a modulator of inflammation and as an antioxidant, restoring the redox balance within the airways in CF patients. To do this, NAC can act alone, but it can also be used as an adjuvant molecule to known drugs (antibiotics/anti-inflammatories) to increase their activity.

12.
J Fungi (Basel) ; 8(11)2022 Oct 27.
Article in English | MEDLINE | ID: mdl-36354900

ABSTRACT

Onychomycosis is a fungal infection caused by different etiologic agents, including dermatophytes that specifically colonize keratin-rich substrates. The aim of this work was to investigate mechanical modifications of bovine membranes (used as an in vitro nail model) placed in contact with Trichophyton species. Trichophyton strains were isolated from toenails specimens. The procedure was set up by spreading T. rubrum,T. interdigitale, and T. mentagrophytes strains on Petri dishes with minimal and rich media; after that, bovine membranes were placed in the center. After 27 days, T. interdigitale and T. mentagrophytes significantly reduced the thickness of the colonized membranes, whereas two T. rubrum strains showed the highest degradation limited to the small colonized area. These results were confirmed by SEM images of the colonization profile on membranes. Mechanical analyses performed on membranes were used as an innovative method to evaluate the thickness and structural integrity of membranes variation following fungal colonization. In conclusion, mechanical analyses of substrate may be used as a procedure for the development of a new onychomycosis diagnosis test in order to develop personalized and strain-specific treatment.

13.
Int J Pharm ; 600: 120409, 2021 May 01.
Article in English | MEDLINE | ID: mdl-33639225

ABSTRACT

Several studies can be found using bovine hoof membranes as a nail in vitro model. Most of them are actually permeability studies, while it is very hard to find reference in literature related to the use of those membranes to evaluate safety and efficacy of products. In facts, some effects, both desirable or not, are not strongly related to the penetration of the products thru all of the nail plate keratin layers. There are morphological characteristics and properties such as mechanical ones which could be affected even by a product acting on the surface of the nail. Moreover, hoof membranes production is not a standardized procedure, as well as membranes characterization which is a critical step to deal with when we are looking for a specific in vitro model. In this work, hoof membranes production is described in detail, along with the characterization techniques and parameters chosen for studying the model, such as contact angle measurement and mechanical properties assessment. The production method developed in this work has shown to be effective, making it possible to obtain membranes with desirable thickness, homogenous morphology and suitable mechanical properties. Mechanical properties were the most challenging to be assessed, also for the poor coverage of the topic by scientific literature. In particular the mechanical assessment has never been used before with this specific aim thus this research could be considered as a feasibility protocol in order to obtain a suitable nail model for further studies concerning drug permeability or safety and efficacy of final products .


Subject(s)
Hoof and Claw , Animals , Antifungal Agents , Cattle , Keratins , Membranes , Nails , Permeability
14.
Open Vet J ; 11(3): 471-482, 2021.
Article in English | MEDLINE | ID: mdl-34722213

ABSTRACT

Background: Furosemide is a potent diuretic drug widely used to treat congestive heart failure in dogs and cats, but it shows remarkable variability in bioavailability and efficacy when administered orally. In particular, a different diuretic effect can be detected after repeated administrations of the same medicinal product in the same animal. For this reason, we investigate the possible reasons for this peculiar behavior. Drug products for veterinary andhuman use are compared in terms of variability for tablet splitting, in vitro dissolution profiles (in different fluids that could simulate the gastrointestinal environment of pets), and drug distribution uniformity. Aim: To study the in vitro performances of drug products in terms of variability. Methods: Five veterinary products and five products for human use, containing different furosemide doses, are characterized. Tablets splitting uniformity, in vitro dissolution profiles in different fluids that could simulate the gastrointestinal environment of the different species, and drug content distribution, were tested. Results: The in vitro dissolution profiles of the different medicines are comparable but confirm a different dissolution rate as a function of the medium pH and volume. Many of the products considered show wide variability in the division performances of the scored tablets, and this problem could lead to the detected fluctuations in the diuretic effect. The four-leaf clover shape of a veterinary product appears to give rise to more uniform fractions. A uniform distribution of the drug in the tablets and their fractions is confirmed for all the products considered. Conclusion: The possibility of tablets splitting allows considerable dosage flexibility, but a non-uniform break of the tablets to obtain the dosage suitable for the pet's weight, can cause dangerous over-or sub-dosing condition, especially in critical pathologies and in small breed pets.


Subject(s)
Cat Diseases , Dog Diseases , Veterinary Drugs , Animals , Cats , Dogs , Furosemide , Tablets
15.
J Cosmet Dermatol ; 19(3): 725-735, 2020 Mar.
Article in English | MEDLINE | ID: mdl-31301106

ABSTRACT

BACKGROUND: In recent years, bacterial cellulose (BC), or biocellulose, a natural polymer synthesized by certain bacteria, has attracted great interest in dermatology and cosmetic applications. Several bioactive ingredients are currently loaded into BC masks. However, only a few studies have reported the effectiveness of such delivery systems. AIM: The aim of this study was to evaluate the effect on skin parameters of three biocellulose masks formulated to have different cosmetic effects (anti-aging, lifting, and cell renewal). In particular, skin moisturizing, skin color, skin viscoelastic properties, skin surface smoothness, wrinkle reduction, dermal homogeneity, and stratum corneum renewal were evaluated. MATERIALS AND METHODS: The study involved 69 healthy Caucasian female volunteers between 25 and 64Ā years, who were divided into three different studies. Biocellulose facial masks were applied using the split-face method three times a week for 4-8Ā weeks depending on the study. RESULTS: The results obtained from this work highlight that biocellulose masks are very well tolerated. A significant decrease in skin roughness and wrinkle breadth, and an improvement in dermal homogeneity and firmness, was observed after 2Ā months of treatment with "anti-aging" masks. A significant improvement in skin firmness and elasticity was observed after 1Ā month of treatment with "lifting" masks. Furthermore, a 1-month treatment with "cell renewal" masks promoted the production of new skin cells through a mild exfoliating action. CONCLUSIONS: This study highlights that biocellulose masks are effective delivery systems to successfully release into the skin several types of active compounds exerting many beneficial effects.


Subject(s)
Cellulose/chemistry , Cosmeceuticals/administration & dosage , Drug Carriers/chemistry , Polysaccharides, Bacterial/chemistry , Skin/drug effects , Administration, Cutaneous , Adult , Cellulose/adverse effects , Drug Carriers/adverse effects , Elasticity/drug effects , Face , Female , Gluconacetobacter xylinus/chemistry , Healthy Volunteers , Humans , Middle Aged , Polysaccharides, Bacterial/adverse effects , Regeneration/drug effects , Skin Aging/drug effects
16.
Skin Appendage Disord ; 6(2): 108-114, 2020 Mar.
Article in English | MEDLINE | ID: mdl-32258054

ABSTRACT

INTRODUCTION: Brittle nail syndrome is characterized by dry, weak, easily breakable nails that show inelasticity, splitting and overall nail plate fragility. OBJECTIVE: This paper describes in vitro and clinical studies using bovine hooves designed to assess the efficacy, compatibility and acceptability of a water-soluble nail strengthener (WSNS), containing Pistacia lentiscus and hyaluronic acid, for the treatment of patients affected by brittle nails. METHODS: In the in vitro study, the WSNS was tested versus placebo and a marketed product on bovine hoof membranes, applied once daily for 14 days for evaluation of firmness, viscoelasticity and thickness before and after applications. In a clinical study, 23 female subjects affected by brittle nails were included, and the WSNS was applied once daily for 3 months. Signs and symptoms were rated by the investigators and by the participants during treatment at 28 and 84 days with different methods and dermoscopic images. Subjective efficacy was evaluated by specific questionnaires. RESULTS: In the in vitro study, the daily application of the WSNS and marketed product led to a significant increase in firmness index. In the clinical study, the nails on the treated hand presented an improvement in nail appearance and weakness, after 28 and 84 days of WSNS application, respectively. The nails not treated showed no improvement. The WSNS was well tolerated. CONCLUSIONS: The WSNS containing Pistacia lentiscus and hyaluronic acid was shown to significantly increase nail firmness in the in vitro study. In the clinical study, WSNS significantly improved brittle nail appearance. The hydrosolubility and easy-to-apply format of WSNS were reported to be factors of a good compliance. We consider this product as an important tool to improve and reinforce the aspect of brittle nails.

17.
J Microencapsul ; 26(6): 535-43, 2009 Sep.
Article in English | MEDLINE | ID: mdl-18855198

ABSTRACT

A novel formulation based on chondroitin sulphate/chitosan microspheres (CS/CH) has been investigated for oral delivery of macromolecules using ovalbumin as the model protein (OVA). The microspheres were prepared by a new emulsion-complex coacervation method. Physico-chemical properties of the polymers constituting microparticulate matrix were investigated by IR, DSC, TGA and X-ray diffraction analyses. In vitro tests were performed to evaluate the drug delivery system degradation and the protein release under conditions simulating the intestinal fluids. The ability of colonic enzymes to degrade the microparticulate systems was simulated employing the chondroitinase ABC enzyme. Results showed that the different CS/CH compositions influenced both microparticles stability and the protein release rate. Only the microspheres composed by 1:1 chondroitin sulphate-chitosan ratio achieved an OVA release profile suitable to a possible colon targeting. These microspheres released approximately 30% of ovalbumin encapsulated in 24 h in the different aqueous media tested, while they released 100% of protein in the presence of chondroitinase. The preliminary results demonstrated that chondroitin sulphate-chitosan microspheres can be a suitable delivery system for protein drug envisaged to oral administration.


Subject(s)
Chitosan , Chondroitin , Microspheres , Proteins/administration & dosage , Administration, Oral , Animals , Chickens , Chitosan/chemistry , Chondroitin/chemistry , Chondroitin ABC Lyase/administration & dosage , Drug Carriers/chemistry , Ovalbumin/administration & dosage , Proteus vulgaris/enzymology , Solubility
18.
Eur J Pharm Biopharm ; 70(1): 58-65, 2008 Sep.
Article in English | MEDLINE | ID: mdl-18547793

ABSTRACT

Prolidase loaded chitosan nanoparticles were set up in order to suggest an innovative therapeutic approach for Prolidase Deficiency (PD), a rare autosomal inherited disorder of the connective tissue. The satisfactory drug loading efficiency (42.6+/-2.1%) as well as the suitable physical characteristics (mean diameter of 365.5+/-35.1 nm and a positive zeta-potential of 17.94+/-0.12 mV) was achieved. In order to verify the compatibility of the chitosan nanoparticles with cells, the influence of the nanoparticles on the growth and the viability (MTT assay) of cultured skin fibroblasts were determined: the nanoparticles showed a good biocompatibility up to 5 microg of chitosan/10,000 fibroblasts. Uptake of chitosan nanoparticles by fibroblasts was verified by confocal microscopy using FITC-labelled chitosan nanoparticles. The ex vivo experiments were performed by incubating different amounts of prolidase loaded chitosan nanoparticles with skin human fibroblasts from PD patients for scheduled times. The restored prolidase activity was quantitatively monitored by a capillary electrophoretic method and confirmed by cells morphological observations. Standing from the nanoparticles internalization, the enzymatic activity was progressively restored reaching the best value (about 66%) after 5 days of co-incubation. Moreover, prolidase loaded chitosan nanoparticles permitted to restore prolidase activity in PD fibroblasts for a prolonged period of time (8 days).


Subject(s)
Amino Acid Metabolism, Inborn Errors/drug therapy , Chitosan/chemistry , Dipeptidases/pharmacology , Drug Carriers , Fibroblasts/drug effects , Nanoparticles , Amino Acid Metabolism, Inborn Errors/enzymology , Cell Proliferation/drug effects , Cell Survival/drug effects , Cells, Cultured , Chemistry, Pharmaceutical , Chitosan/toxicity , Dipeptidases/chemistry , Dipeptidases/deficiency , Dipeptidases/therapeutic use , Dose-Response Relationship, Drug , Electrophoresis, Capillary , Endocytosis , Enzyme Stability , Fibroblasts/enzymology , Humans , Microscopy, Confocal , Particle Size , Solubility , Time Factors
19.
Eur J Pharm Sci ; 121: 309-318, 2018 08 30.
Article in English | MEDLINE | ID: mdl-29874551

ABSTRACT

BACKGROUND: The growing incidence of photodamaging effects caused by UV radiation (e.g. sunburn, skin cancer) has increased the attention from health authorities which recommend the topical application of sunscreens to prevent these skin damages. The economic stakes for those companies involved in this international market are to develop new UV filters and innovative technologies to provide the most efficient, flexible and robust sunscreen products. Today the development of innovative and competitive sunscreen products is a complex formulation challenge. Indeed, the current sunscreens must protect against skin damages, while also being safe for the skin and being sensory and visually pleasant for the customers when applied on the skin. Organic UV filters, while proposing great advantages, also present the risk to penetrate the stratum corneum and diffuse into underlying structures with unknown consequences; moreover, their photo-stability are noted thorny outcomes in sunscreen development and subsequent performance. In recent years, the evaluation of the interaction between skin and sunscreen in terms of penetration after topical application has been considered from European authority but still its testing as their photo-stability assessment are not mandatory in most countries. OBJECTIVE: This study, based on in-vitro approaches, was performed to evaluate and compare the retention and the penetration of organic UV filters in free or encapsulated form inside the skin as well as their respective photo-stability. METHODS: Sunscreen formulation with a combination of Avobenzone and Octocrylene in "free form" and a formulation using the same UV filters but encapsulated in a sol-gel silica capsule, were analyzed and compared by FTIR Imaging Spectroscopy. Tape stripping method was used to investigate the penetration of these UV filters inside the stratum corneum. Their photo-stabilities were evaluated by spectroscopic measurements (FTIR, UV/Vis) and standard measurements were calculated: AUC (Area Under the Curve) and SPF (Sun Protection Factor). RESULT: With traditional formulation, the organic UV filters penetrated significantly into the stratum corneum while the same UV filters combined with encapsulation technology remained on the skin surface. The encapsulation technology also improved significantly their stability. CONCLUSION: Encapsulation technology is a promising strategy to improve the efficacy of sunscreen product using organic UV filters and to reduce safety problem. On the other hand, this study highlighted the pertinence of the FTIR Spectroscopy to test, compare and investigate sunscreen formulations.


Subject(s)
Acrylates/administration & dosage , Propiophenones/administration & dosage , Sunscreening Agents/administration & dosage , Acrylates/chemistry , Acrylates/radiation effects , Animals , Drug Compounding , Drug Stability , Propiophenones/chemistry , Propiophenones/radiation effects , Skin/metabolism , Skin Absorption , Sunscreening Agents/chemistry , Sunscreening Agents/radiation effects , Swine , Ultraviolet Rays
20.
Pharmaceutics ; 10(3)2018 Aug 02.
Article in English | MEDLINE | ID: mdl-30072665

ABSTRACT

Plastic material is used for a wide variety of commercial packaging due to being inexpensive, lightweight, and due to its resistance. In pharmaceutics, container-content compatibility studies are required for product authorization. Many guidelines and publications are available; however, the information is often only related to the raw materials used to produce packaging. During the manufacturing process, substances can be added to improve the product characteristics and performance, resulting in a processed material that is considerably different from the unprocessed material. In this study, the mechanical properties of low-density polyethylene (LDPE) and linear low-density polyethylene (LLDPE) specimens fabricated according to standard ISO 527 and specimens fabricated with the same materials, but obtained from final packaging, were evaluated. Furthermore, we examined the interaction between a semisolid formulation and LLDPE and LDPE as a final packaging, by subjecting two samples to accelerated degradation testing. Then, mechanical properties and volatile organic extractable were evaluated. Simulated solar radiation did not induce changes in the packaging mechanical properties and no extracts were detectable. The thermal shock strongly influenced the mechanical behavior, and interactions between packaging contents were identified. The present work underlines the difference between analyzing the standard ISO specimens versus samples obtained from final packaging in order to evaluate the packaging under real use conditions. An evaluation on the final packaging, instead on standard specimens, can provide information about the plastic material after the manufacturing process and the interaction between packaging and content.

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