scholarly journals Supramolecular and Macromolecular Matrix Nanocarriers for Drug Delivery in Inflammation-Associated Skin Diseases

Pharmaceutics ◽  
2020 ◽  
Vol 12 (12) ◽  
pp. 1224
Author(s):  
Ranime Jebbawi ◽  
Séverine Fruchon ◽  
Cédric-Olivier Turrin ◽  
Muriel Blanzat ◽  
Rémy Poupot

Skin is our biggest organ. It interfaces our body with its environment. It is an efficient barrier to control the loss of water, the regulation of temperature, and infections by skin-resident and environmental pathogens. The barrier function of the skin is played by the stratum corneum (SC). It is a lipid barrier associating corneocytes (the terminally differentiated keratinocytes) and multilamellar lipid bilayers. This intricate association constitutes a very cohesive system, fully adapted to its role. One consequence of this efficient organization is the virtual impossibility for active pharmaceutical ingredients (API) to cross the SC to reach the inner layers of the skin after topical deposition. There are several ways to help a drug to cross the SC. Physical methods and chemical enhancers of permeation are a possibility. These are invasive and irritating methods. Vectorization of the drugs through nanocarriers is another way to circumvent the SC. This mini-review focuses on supramolecular and macromolecular matrices designed and implemented for skin permeation, excluding vesicular nanocarriers. Examples highlight the entrapment of anti-inflammatory API to treat inflammatory disorders of the skin.

2020 ◽  
Vol 21 (14) ◽  
pp. 5016
Author(s):  
Roxana Popescu ◽  
Mihaela Violeta Ghica ◽  
Cristina-Elena Dinu-Pîrvu ◽  
Valentina Anuța ◽  
Dumitru Lupuliasa ◽  
...  

In an attempt to develop drug delivery systems that bypass the blood–brain barrier (BBB) and prevent liver and intestinal degradation, it was concluded that nasal medication meets these criteria and can be used for drugs that have these drawbacks. The aim of this review is to present the influence of the properties of chitosan and its derivatives (mucoadhesion, permeability enhancement, surface tension, and zeta potential) on the development of suitable nasal drug delivery systems and on the nasal bioavailability of various active pharmaceutical ingredients. Interactions between chitosan and proteins, lipids, antigens, and other molecules lead to complexes that have their own applications or to changing characteristics of the substances involved in the bond (conformational changes, increased stability or solubility, etc.). Chitosan and its derivatives have their own actions (antibacterial, antifungal, immunostimulant, antioxidant, etc.) and can be used as such or in combination with other molecules from the same class to achieve a synergistic effect. The applicability of the properties is set out in the second part of the paper, where nasal formulations based on chitosan are described (vaccines, hydrogels, nanoparticles, nanostructured lipid carriers (NLC), powders, emulsions, etc.).


2021 ◽  
Vol 22 (18) ◽  
pp. 9743
Author(s):  
Eliana B. Souto ◽  
Ana S. Macedo ◽  
João Dias-Ferreira ◽  
Amanda Cano ◽  
Aleksandra Zielińska ◽  
...  

Administration of active pharmaceutical ingredients (APIs) through the skin, by means of topical drug delivery systems, is an advanced therapeutic approach. As the skin is the largest organ of the human body, primarily acting as a natural protective barrier against permeation of xenobiotics, specific strategies to overcome this barrier are needed. Liposomes are nanometric-sized delivery systems composed of phospholipids, which are key components of cell membranes, making liposomes well tolerated and devoid of toxicity. As their lipid compositions are similar to those of the skin, liposomes are used as topical, dermal, and transdermal delivery systems. However, permeation of the first generation of liposomes through the skin posed some limitations; thus, a second generation of liposomes has emerged, overcoming permeability problems. Various mechanisms of permeation/penetration of elastic/ultra-deformable liposomes into the skin have been proposed; however, debate continues on their extent/mechanisms of permeation/penetration. In vivo bioavailability of an API administered in the form of ultra-deformable liposomes is similar to the bioavailability achieved when the same API is administered in the form of a solution by subcutaneous or epi-cutaneous injection, which demonstrates their applicability in transdermal drug delivery.


Nanoscale ◽  
2021 ◽  
Author(s):  
Jiyeon Kim ◽  
Chanuk Choi ◽  
Seonki Hong

Co-crystallization of active pharmaceutical ingredients (APIs) with pharmaceutically acceptable additives has emerged as an alternative to current drug delivery systems for hydrophobic drugs, due to the high drug loading efficiency....


The Analyst ◽  
2014 ◽  
Vol 139 (5) ◽  
pp. 1000-1006 ◽  
Author(s):  
D. Fitzpatrick ◽  
R. Evans-Hurson ◽  
Y. Fu ◽  
T. Burke ◽  
J. Krüse ◽  
...  

There is an increased trend towards the use of drug and enteric coated sugar spheres for controlled oral delivery of active pharmaceutical ingredients (API).


2021 ◽  
Vol 22 (4) ◽  
pp. 1535
Author(s):  
Parinbhai Shah ◽  
Benjamin Goodyear ◽  
Nirali Dholaria ◽  
Vinam Puri ◽  
Bozena Michniak-Kohn

Psoriasis is a chronic autoimmune skin disease impacting the population globally. Pharmaceutical products developed to combat this condition commonly used in clinical settings are IV bolus or oral drug delivery routes. There are some major challenges for effectively developing new dosage forms for topical use: API physicochemical nature, the severity of the disease state, and low bioavailability present challenges for pharmaceutical product developers. For non-severe cases of psoriasis, topical drug delivery systems may be preferred or used in conjunction with oral or parenteral therapy to address local symptoms. Elastic vesicular systems, termed “niosomes”, are promising drug delivery vehicles developed to achieve improved drug delivery into biological membranes. This study aimed to effectively incorporate a corticosteroid into the niosomes for improving the drug bioavailability of desoximetasone, used to treat skin conditions via topical delivery. Niosomes characterization measurements were drug content, pH, spreadability, specific gravity, content uniformity, rheology, and physicochemical properties. Formulations used a topical gelling agent, Carbomer 980 to test for in vitro skin permeation testing (IVPT) and accelerated stability studies. The developed niosomal test gel provided approximately 93.03 ± 0.23% to 101.84 ± 0.11% drug content with yield stresses ranging from 16.12 to 225.54 Pa. The permeated amount of desoximetasone from the niosomal gel after 24 h was 9.75 ± 0.44 µg/cm2 compared to 24.22 ± 4.29 µg/cm2 released from the reference gel tested. Furthermore, a drug retention study compared the test gel to a reference gel, demonstrating that the skin retained 30.88 ng/mg of desoximetasone while the reference product retained 26.01 ng/mg. A controlled drug release profile was obtained with a niosomal formulation containing desoximetasone for use in a topical gel formulation showing promise for potential use to treat skin diseases like psoriasis.


Encyclopedia ◽  
2021 ◽  
Vol 1 (3) ◽  
pp. 942-963
Author(s):  
Sónia N. Pedro ◽  
Carmen S. R. Freire ◽  
Armando J. D. Silvestre ◽  
Mara G. Freire

Deep eutectic solvents (DES) are eutectic mixtures that present a deviation from the ideal thermodynamic solid–liquid phase behavior, where a significant depression in the melting temperature occurs. If properly designed and chosen, DES may be liquid at room and the human body’s temperatures and display a biocompatible character, thus representing relevant options in the pharmaceutical field. Accordingly, DES have been studied as alternative solvents or in formulations of pharmaceuticals to improve their solubility and stability. Depending on the DES components, these mixtures might exhibit interesting biological activities compatible with several applications. The use of DES as functional agents or as novel liquid forms of active pharmaceutical ingredients (API-DES) with the goal of improving bioavailability, permeability and therapeutic efficacy of a given API stands as alternative strategies in the pharmaceutical field for drug delivery purposes.


Author(s):  
A. S. Koval ◽  
S. V. Birukova ◽  
Y. V. Voyda

The aim of the work is to determine the spectrum and strenght of antimicrobial activity of the studied compositions, to compare them with the activity of substancesand to select the most optimal concentration for further combination with each other. Topicality. Nowadays, one of the most common skin diseases is acne and demodicosis, the manifestations of which can be mild (comedones in seborrheic areas), more noticeable (papules-pustular rash) and severe (large cyanotic infiltrative elements in the back, prone to abscessing and scarring). The prevalence of acne and demodicosis currently reaches 90%. With these skin pathologies, it is desirable to use safe and effective drugs for external therapy, which provide rapid improvement of the skin (reduction of inflammation without side effects) to obtain a rapid and high-quality therapeutic effect. In the course of our research, we selected 3 active pharmaceutical ingredients (APIs): metronidazole, benzyl benzoate and benzoyl peroxide - according to the purpose of ICD-10 and their effectiveness in these pathologies. Mild medicines have an advantage over dermatological diseases such as acne and demodicosis because the use of soft medicines is local, namely a targeted effect on the microbial microflora. At present for production of soft medicines for local application such substances as macromolecular compounds are widely used, plasticizers, surfactants,etc. When creating a drug composition, a study was conducted aimed at obtaining soft medicines with certain consumer properties, in particular physicochemical (pH, osmotic activity, homogeneity,etc.) , physical and mechanical properties (rheological parameters). Materials for the study – soft medicines based on cetyl alcohol, Emulgade Sucro Plus, Polyvinylpyrrolidone, Carboxymethylcellulose, Tween 80, Triethanolamine, Propylene glycol, vaseline oil, which as (API) contains metronidazole, benzoyl peroxide, benzylbenzene. The specific antimicrobial activity of the samples was tested in accordance with Order № 167 of the Ministry of Health of Ukraine dated 05.04.2007 by the standard macromethod of serial dilutions in liquid nutrient medium and by the method of diffusion into agar. The minimum inhibitory concentration (MIC) of API (substrates) was determined. Results. The studied compositions of soft medicines and substrates revealed to presence of antibacterial (bacteriostatic) action against the test strains of microorganisms. Conclusions. The test of the compositions of soft medicines and the substance revealed the presence of a slight antibacterial (bacteriostatic) effect against the test strains of microorganisms. Key words: antimicrobial activity; active pharmaceutical ingredients (API); excipients; soft dosage form


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