Release Of Active Principle Research Articles

Rutin encapsulated decellularized earthworm granulation hydrogel promotes angiogenesis in wound healing of diabetic rabbit model by inhibiting TRAF1/NF-κB pathway

Diabetic micro-vasculopathy is induced by accumulation of Reactive Oxygen Species (ROS) which results in delayed wound healing under hyperglycemic conditions. The classical practice of treating diabetic wound includes surgical debridement, hyperbaric oxygen therapy and use of antibiotics to control infection. The therapeutic interventions based on these classical practices have been found ineffective in management of diabetic wound healing and diabetic vasculopathy. Henceforth, engineered biomaterials with anti-oxidant activity have become research hotspots for their high biological activity, due to sustained release of active principles and weak immunogenicity. Based on these postulates, current study was conducted to evaluate diabetic wound healing potential of Rutin encapsulated decellularized earthworm granulation tissue (RdECM) with special reference on angiogenesis. The angiogenetic activity of RdECM was evaluated on cell line under hyperglycemic conditions and we found significant decline in ROS induced Deoxyribonucleic acid (DNA) damage and inhibition of Nuclear factor kappa B (NF-Kβ) pathway with subsequent aggregation of cells in tubular structure. Application of RdECM on diabetic wound resulted in accelerated wound healing, reduction in ROS induced DNA damage and down regulation of TNF receptor associated factor 1 (TRAF1). These changes results in inhibition of TRAF1-mediated NF-κB signal activation and subsequently angiogenesis in hyperglycemic conditions of diabetic wound. These findings support therapeutic utility of RdECM as angiogenetic agent and its potential use against diabetic wound healing.

Synthesis of Bio-Based Polyester from Microbial Lipidic Residue Intended for Biomedical Application.

In the last decade, selectively tuned bio-based polyesters have been increasingly used for their clinical potential in several biomedical applications, such as tissue engineering, wound healing, and drug delivery. With a biomedical application in mind, a flexible polyester was produced by melt polycondensation using the microbial oil residue collected after the distillation of β-farnesene (FDR) produced industrially by genetically modified yeast, Saccharomyces cerevisiae. After characterization, the polyester exhibited elongation up to 150% and presented Tg of -51.2 °C and Tm of 169.8 °C. In vitro degradation revealed a mass loss of about 87% after storage in PBS solution for 11 weeks under accelerated conditions (40 °C, RH = 75%). The water contact angle revealed a hydrophilic character, and biocompatibility with skin cells was demonstrated. 3D and 2D scaffolds were produced by salt-leaching, and a controlled release study at 30 °C was performed with Rhodamine B base (RBB, 3D) and curcumin (CRC, 2D), showing a diffusion-controlled mechanism with about 29.3% of RBB released after 48 h and 50.4% of CRC after 7 h. This polymer offers a sustainable and eco-friendly alternative for the potential use of the controlled release of active principles for wound dressing applications.

Oral disintegration films: applications and production methods.

The use of orally disintegrating films (ODF) as a vehicle for the release of active compounds has drawn attention due to the advantages such as ease of swallowing, precise dosage, low thickness, flexibility, greater comfort and acceptability by the patient in relation to oral tablets, for do not require water for administration, it is ideal for people with difficulty in swallowing. In this review, recent advances in ODFs, their applications and production methods will be presented. The production of ODFs uses polymers, plasticizers and active compounds. Among the compounds added to the film that can affect its properties, the polymer used has a strong influence on the disintegration time and on the controlled release of active principles. Polymers used for the production of oral films must be non-toxic, have good wettability and spreadability, and may be of synthetic or natural origin. Regarding the methods used in the production of ODFs, those currently used are solvent evaporation and hot extrusion. However, one of the great challenges for the production of oral films is the scale up, from laboratory to industrial scale, as factors such as heating, mixing speed and temperatures can lead to changes in film quality. Recently, ODFs have been developed as carriers of natural compounds such as vitamins, phenolic compounds, antioxidant and antimicrobial activity. Thus, it was found that orally disintegrating films are an alternative for the release of active compounds, different from those already existing, which justifies the growing interest in this type of film.

Solventless Crosslinking of Chitosan, Xanthan, and Locust Bean Gum Networks Functionalized with β-Cyclodextrin.

The incorporation of cyclodextrins into polymeric crosslinked gels of hydrophilic nature can be useful for promoting the sorption of hydrophobic molecules and/or modulating the release of active principles. The covalent addition of these excipients to the matrix integrates their solubilizing effect that can contribute to increase the capacity of retention of hydrophobic substances. In this study, three diverse polysaccharides, chitosan, xanthan gum, and locust bean gum, were crosslinked with or without β-cyclodextrin, using citric acid in different ratios, to create hydrogel matrices. Through a green synthetic path, the efficient production of soluble and insoluble (hydrogel) networks functionalized with β-cyclodextrin was achieved by means of a solventless procedure. The characterization of their chemical composition, swelling in water, and their sorption and release behavior were also carried out in this work.

Nanoemulsions and dermatological diseases: contributions and therapeutic advances.

Skin disease is one of the most common human diseases and affects between 30% and 70% of individuals, which requires a lot of attention to their treatments. The delivery of active pharmacological ingredients at the topical level is a challenge because of the difficulties in overcoming the mechanical barrier created by the skin and reaching greater depths, since delivery specificities are decisive for the degree of effectiveness. In this way, the nanoemulsions emerge as a potential system for the incorporation of active substances in the cells and for the controlled release of active principles. The present article intends to review the main treatments for which the nanoemulsions were used in the field of dermatology. In addition, it discusses the results and advantages over the other dermatological therapies that are being used. The results showed that the particle size in nanoemulsions increased the contact surface area, resulting in increased drug efficacy, even in comparison with other existing pharmaceutical formulations. In conclusion, it has been shown that nanoemulsions have a better performance in efficacy, safety, permeability profile, and bioavailability compared with other formulations studied.

Transdermal skin patch based on reduced graphene oxide: A new approach for photothermal triggered permeation of ondansetron across porcine skin

The development of a skin-mounted patch capable of controlled transcutaneous delivery of therapeutics through thermal activation provides a unique solution for the controlled release of active principles over long-term periods. Here, we report on a flexible transdermal patch for photothermal triggered release of ondansetron (ODS), a commonly used drug for the treatment of chemotherapy-induced nausea and vomiting and used as model compound here. To achieve this, a dispersion of ODS-loaded reduced graphene oxide (rGO-ODS) nanosheets were deposited onto Kapton to produce a flexible polyimide-based patch. It is demonstrated that ODS loaded Kapton/rGO patches have a high drug delivery performance upon irradiation with a continuous laser beam at 980nm for 10min due to an induced photothermal heating effect. The ability of ODS impregnated Kapton/rGO patches as transdermal delivery scaffolds for ODS across the skin is in addition investigated using porcine ear skin as a model. We show that the cumulative quantity and flux of ODS passing the skin are highly depending on the laser power density used. At 5Wcm−2 irradiation, the ODS flux across pig skin was determined to be 1.6μgcm−2h−1 comparable to other approaches. The use of tween 20 as skin enhancer could significantly increase the ODS flux to 13.2μgcm−2h−1. While the skin penetration enhancement is comparable to that obtained using other well-known permeation enhancers, the actual superiority and interest of the proposed approach is that the Kapton/rGO photoactivatable skin patch can be loaded with any drugs and therapeutics of interest, making the approach extremely versatile. The on demand delivery of drugs upon local laser irradiation and the possibility to reload the interface with the drug makes this new drug administration route very appealing.

Modeling of the controlled release of betacarotene into anhydrous ethanol from microcapsules

In this paper several models of the mass transfer process are described with the aim of simulating the release of active principles from matrix-type polymeric microcapsules. The following mathematical models, which are available in the literature, are applied in this study: Fick's second law (CDMASSA), the linear drive force (LDF), an analytical model and other semi-empirical models. The release of the active principle (betacarotene) contained in microcapsules (PHBV) into a solvent (ethanol) was investigated. It was observed that the model obtained with Fick's second law provided a better fit with the literature data compared with the LDF model, the analytical model and the semi-empirical models. It can be concluded from this finding that the most complete model, based on the phenomenology of the problem, provided the best result.

Drug release system of ibuprofen in PCL-microspheres

Today, the technology of microencapsulation of active principles is on top of biomedical advances, because through it we can solve many of the problems caused by current methods of taking medication. Active principle microencapsulation not only solves the problems of drug intake but also controls its dosage. In this study was carried out the development of a protocol for the microencapsulation of ibuprofen by solvent evaporation method. A subsequent application of those microencapsulates to biofunctional textile substrates (cotton, polyamide, acrylic, and polyester) using a finishing process, and finally a study of the release of active principle in two different media (deionized water and physiological serum) has been carried out using samples of the treated fabrics that were submerged into a thermostatized vessel at semi-infinite bath conditions. The determination of active principles released to the bath was determined by a UV spectrophotometer. These experimental results have been analyzed and evaluated, and have therefore allowed to define a controlled drug release system by Fickian diffusion in different media.

Drug Delivery Properties of Macroporous Polystyrene Solid Foams

Polymeric porous foams have been evaluated as possible new pharmaceutical dosage forms. These materials were obtained by polymerization in the continuous phase of highly concentrated emulsions prepared by the phase inversion temperature method. Their porosity, specific surface and surface topography were characterized, and the incorporation and release of active principles was studied using ketoprofen as model lipophilic molecule. Solid foams with very high pore volume, mainly inside macropores, were obtained by this method. The pore morphology of the materials was characterized, and very rough topography was observed, which contributed to their nearly superhydrophobic properties. These solid foams could be used as delivery systems for active principles with pharmaceutical interest, and in the present work ketoprofen was used as a model lipophilic molecule. Drug incorporation and release was studied from solid foam disks, using different concentrations of the loading solutions, achieving a delayed release with short lag-time.

Alternativa con gel de Papaver somniferum (amapola) y Cannabis sativa (marihuana), como tratamiento de artritis reumatoide

En la elaboración del presente producto farmacéutico (una formulación galénica entre el gel y la emulsión fluida), se utilizaron dos principios activos naturales considerados psicotrópicos o narcóticos: extracto alcohólico de amapola (Papaver somni-ferum) y extracto alcohólico de marihuana (Cannabis sativa); éstos tienen actividad biológica conocida dentro del organismo. Son excelentes analgésicos para pacientes con cáncer terminal pero también tienen propiedades antieméticas, estimulantes del apetito, relajantes oculares, bronquíticos, ansiolíticos. Se conoce que para tener una liberación prolongada de un principio activo es muy útil el uso de liposomas; por esta razón se utilizaron liposomas de extracto alcohólico de amapola, considerando que esta planta tiene mejores propiedades analgésicas que la marihuana, por lo cual el extracto de esta última integra un 40% de la formulación. Los resultados obtenidos después de la elaboración del producto fueron favorables en lo relacionado al control de calidad. El presente trabajo comprende un gel, para el uso tópico; esta composición farmacéutica es un reservorio de ingredientes activos en un sistema de liberación transdérmico, además tiene una notable estabilidad y características orga- lépticas óptimas.

In vitro evaluation of the permeation through reconstructed human epidermis of essentials oils from cosmetic formulations

The permeation of essential oils through SkinEthic ® reconstructed human epidermis, (RHE), was studied in vitro to establish a convenient tool to monitor the kinetics of release of active principles from cosmetic formulations. Twelve days old human epidermis held on polycarbonate disks was revitalized by addition of growth medium and incubated at 37 °C in 5% CO 2 atmosphere for five days prior to investigation. A system of six custom designed glass Franz-type diffusion cells were used for the permeation studies at 34 °C. The diffusion kinetic for 8 selected terpenes (camphor, carvone, 1,8-cineole, linalool, menthol, α-thujone, menthone, t-anethole), chosen as analytical markers of a mixture of plant essential oils contained in a cosmetic formulation, was probed by HS/SPME–GC–MS analysis and elaborated according to Fick's first law to obtain skin permeability coefficients ( P S = 1.51, 1.47, 1.36, 0.80, 0.62, 0.40 and 0.14 × 10 −3 cm/h, respectively). The method proved to be sensitive, simple and reproducible, and RHE represents a convenient model for safety/quality assessment of cosmetic formulations.

Preparation, Rheological Study, and Characterization of an Organogel as a System for Transdermal Release of Active Principles

The use of formulations containing Pluronic® gel as a vehicle and permeabilizing agent for transdermal preparations has increased in recent years. We prepared and compared two transdermal formulations for drug administration as an alternative to oral or parenteral administration. In formulations containing Pluronic® F127 gel or pluronic lecithin organogel (PLO), rheological, structural (transmission electron microscopy) and physicochemical characteristics were studied under different conditions of composition, temperature, and time from 24 hr to 3 months after preparation. Rheological studies at 20–25°C and at 4°C to study the influence of refrigeration on viscosity and pH showed that both formulas were thermoreversible. Unilamellar vesicles smaller than 1 μm in diameter were seen in the PLO formulation on TEM observation. The characteristics of these excipients may facilitate the application and may avoid the gastrointestinal tract and the first-pass effect.

Modeling the controlled release of microencapsulated drugs: theory and experimental validation

The release of active principles from microencapsulated drugs has been studied and treated extensively in the literature. However, only empirical or semiempirical models have been proposed. Often, such models are not able to describe correctly the articulated behavior of the release phenomenon. This paper, based on a first principles approach, defines a fully theoretical model of the release process within the human body. The key point of this work is the penetration theory that describes the experimental evidence of release dependency from square root of time. In addition, the paper deals with the observed lead-lag time characterizing the release dynamics of active principle that diffuses towards the external solution. A detailed analysis of the transport phenomena involved, focuses the attention on the diffusive mechanism, which is strictly related to the existing affinity between active principle and polymer coating. Finally, the good agreement between experimental release data, for different active principles, and corresponding simulated curves allows the proposed model to be considered of real value for predictive design purposes.

Nanoparticle systems for the targeted release of active principles of proteic nature.

The preparation and characterization of nanoparticles based on biodegradable/bioerodible polymers is reported. They have been designed for the controlled-targeted release of proteic drugs such as alpha-interferon and for the release of active principles in tissue engineering. The amenability of some of the prepared polymeric matrices to be used in the fabrication of micro and nano patterned scaffolds is also described.

COMPREHENSIVE EVALUATION OF DIFFERENT SOLIDAGINIS HERBA EXTRACTS

COMPREHENSIVE EVALUATION OF DIFFERENT SOLIDAGINIS HERBA EXTRACTS